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Full Agenda Adhesion GPCR workshop 2024 CINVESTAV, Mexico City, Mexico October 23-25 Download PDF Program HERE < Back to Full Agenda Session III Molecular tools and biosensors directed at AGPCR signaling and function The NTF Release Sensor Approach for Drug Discovery for Human Adhesion GPCRs Stephanie Häfner bioSens-All: A Multiparametric BRET-Based Platform for Comprehensive Profiling of adhesion GPCR Signaling and Pharmacology-Enabling Drug Discovery Laurent Sabbagh Characterizing hADGRE5/CD97 Activation and Signaling: A Mechanical Stimulation BRET-Based Approach (MS-BRET) Ana Lilia Moreno Salinas The NTF Release Sensor Approach for Drug Discovery for Human Adhesion GPCRs Stephanie Häfner Abstract "G Protein-coupled receptors (GPCRs) are common drug targets, yet no approved drugs exist for the Adhesion G Protein-coupled receptors (aGPCRs or ADGRs). This gap is due to their unique autoproteolytic cleavage in the GAIN domain, creating a heterodimer of an N-terminal fragment (NTF) and a C-terminal fragment (CTF), posing challenges for traditional drug discovery. To address this, we developed the NTF release sensor (NRS), a genetically encoded reporter that facilitates visualization and quantification of aGPCR NTF-CTF separation events both in vitro and in vivo. The NRS fuses the extracellular region of any given aGPCR with a cleavage module from a Notch receptor. Upon NTF dissociation, an intracellular transcription factor (reporter module) is released, generating a specific, measurable biochemical signal. The NRS system has recently been validated in vivo by targeting the latrophilin-type aGPCR Cirl/ADGRL in Drosophila, revealing NTF release and receptor dissociation within the developing nervous system. It was then adapted for the human aGPCRs CD97/ADGRE5 and Latrophilin/ADGRL3 and tested in HEK293T cells using a luciferase assay to detect NTF release events. After validating the functionality of the NRS and demonstrating its utility for monitoring aGPCR dissociation across different species, we plan to adapt this technology for high-throughput screening of pharmacological compound libraries to identify potential therapeutic substances for aGPCRs. By leveraging self-cleavage and NTF release, the NRS technology offers a novel approach distinct from conventional GPCR drug discovery methods. This tailored system aims to expedite the identification of drugs targeting the unique aGPCR receptor family and customize the method for disease-relevant human aGPCRs." Authors & Affiliations "Dahse, Anne-Kristin; Annadurai, Prabakaran; Demirbaş, Berkay; Kemkemer, Marguerite; Langenhan, Tobias; Scholz, Nicole Rudolf Schönheimer Institute of Biochemistry, Divison of General Biochemistry, Medical Faculty, Leipzig University, Leipzig, Germany" About Stephanie Häfner "I am a trained chemist with extensive biochemical experience. After earning my Master of Science in Chemistry, I pursued my PhD in Dr. Michael Schaefer’s group at Leipzig University, Germany, focusing on drug screening and utilizing electrophysiological and imaging techniques to study TRP ion channels. Immediately following my PhD, I joined Dr. Guillaume Sandoz's group in 2019 as a postdoctoral research scientist at Université Côte d‘Azur, France. There, I investigated Two-Pore-Potassium channels using electrophysiology, molecular and chemical biology techniques, and fluorescence imaging. In 2021, I joined Dr. Tobias Langenhan's group, where I currently manage a project to establish a drug screening assay for Adhesion GPCRs using a specialized sensor system and mentor PhD students." Stephanie Häfner on the web LinkedIn Scholz Lab Langenhan Lab bioSens-All: A Multiparametric BRET-Based Platform for Comprehensive Profiling of adhesion GPCR Signaling and Pharmacology-Enabling Drug Discovery Laurent Sabbagh Abstract "The 3rd generation bioSens-All platform combines BRET-based biosensors that are highly adaptable to the needs of discovery projects for small molecules, peptides, and antibodies. The platform has been successfully used internally to identify biased small molecule negative allosteric modulators for protease-activated receptor 2 (PAR2). The platform revealed different mechanisms-of-action of our lead compound when benchmarked against other antagonists of PAR2. In addition, the platform was used to develop assays for high-throughput screening for challenging adhesion GPCRs. These examples will demonstrate how the bioSens-All platform was used to advance projects from discovery to preclinical candidate nomination and to provide the tools to advance adhesion GPCR biology." Authors & Affiliations "Ana Lilia Moreno Salinas (2), Arturo Mancini (1), Raida Jallouli (2), Richard Leduc (2) (1)Domain Therapeutics North America Inc, Montréal, Québec, Canada (2) Department of Pharmacology-Physiology, Université de Sherbrooke, Québec, Canada" About Laurent Sabbagh "Laurent holds a Ph.D. in immunology from McGill University. Following his doctoral degree Dr. Sabbagh undertook post-doctoral fellowships at the Ontario Cancer Institute and the University of Toronto before being recruited by University of Montreal as an assistant professor working on the role of TNF receptors in immunological memory, inflammation and hematological malignancies. In the fall of 2013, Dr. Sabbagh was recruited by Vertex Pharmaceuticals (Canada) where he worked on biomarker discovery for inflammatory bowel disease and small molecules drug discovery for polycystic kidney disease. Subsequently, Dr. Sabbagh led research projects aimed on drug discovery of small molecules for the treatment of inflammatory disorders and cancer at Paraza Pharma Inc. in Montreal. Laurent is currently leading DTNA discovery group working on GPCRs in immuno-oncology to discover new molecules and antibodies." Laurent Sabbagh on the web Domain Therapeutics Characterizing hADGRE5/CD97 Activation and Signaling: A Mechanical Stimulation BRET-Based Approach (MS-BRET) Ana Lilia Moreno Salinas Abstract Only available for AGPCR 24 Attendees Authors & Affiliations "Arturo Mancini (2), Samya Aouad (2,3), Herthana Kandasamy (2), Sandra Morrissette (2), Arhamatoulaye Maiga (4), Michel Bouvier (4), Richard Leduc (1), Laurent Sabbagh (2) 1. Department of Pharmacology-Physiology, Université de Sherbrooke, Sherbrooke, Quebec, Canada 2. Domain Therapeutics North America Inc., Montreal, Quebec, Canada 3. Université Claude Bernard - Lyon, Faculté de Pharmacie, Lyon, France 4. Department of Biochemistry and Molecular Medicine, Institute for Research in Immunology and Cancer (IRIC), Université de Montréal, Montreal, Quebec, Canada " About Ana Lilia Moreno Salinas "I am currently part of a dynamic research team dedicated to advancing the understanding of G protein-coupled receptors (GPCRs), with a particular focus on the adhesion GPCRs (aGPCRs) family. My expertise lies in exploring the biological properties and signaling pathways activated by aGPCRs, investigating their roles in both normal physiological and pathological conditions. Our research aims to leverage this knowledge to identify novel pharmacological targets and contribute to the development of innovative treatments for a range of diseases, including psychiatric disorders and cancer." Ana Lilia Moreno Salinas on the web ResearchGate LinkedIn < Previous Session Next Session >

Showcase your creativity in the AGPCR24 Logo Contest! Submit your design to represent the Adhesion GPCR Workshop and inspire our global community. LOGO CONTEST Adhesion GPCR workshop 2024 CINVESTAV, Mexico City, Mexico October 23-25 Register Rules for the logo contest Design must be based on “Alebrijes” [ah-leh-bree-hez], which are chimeric creatures from Mexican folklore AND contain adhesion GPCRs Avoid copyrighted material unless a CC BY / open-use license has been acquired or generated (Adobe Stock, etc). The Consortium must be free to use the design. Requirements: Resolution 300 ppi max, JPEG/TIFF/EPS/PNG/PDF formats, 5MB max Open to all adhesion GPCR community members. Artist-scientists must be registered to attend the adhesion GPCR workshop 2024 in Mexico City. The contest deadline is August 15th, 2024, 11:59 PM CST (designs received after the deadline will not be considered) Designs or inquiries should be sent to this email The prize for the selected design will include free registration and more! Register for the Adhesion GPCR 2024 Learn more about the Adhesion GPCR workshop 2024 Up About the event Learn more about the Adhesion GPCR workshop 2024 and its preliminary program. Up About the venue Discover Cinvestav, the host venue for the upcoming workshop. Up Abstract Submission Submit your research abstracts following our guidelines to present at the conference. Up Traveling Tips Find essential tips about Mexico City, including transportation options and local insights.

Full Agenda Adhesion GPCR workshop 2024 CINVESTAV, Mexico City, Mexico October 23-25 Download PDF Program HERE < Back to Full Agenda Session V Structural mechanisms of AGPCR signaling and function Structural Determinants Of GAIN Domain Autoproteolysis And Cleavage Resistance Of Adhesion G Protein-Coupled Receptors Fabian Pohl Structural studies of the CELSR1 extracellular region reveal a compact multidomain module of fourteen domains which regulates signaling Sumit Bandekar Unveiling the GPS Cleavage Mechanism in ADGRL1 with QM/MM Florian Seufert Structural Determinants Of GAIN Domain Autoproteolysis And Cleavage Resistance Of Adhesion G Protein-Coupled Receptors Fabian Pohl Abstract "The GPCR autoproteolysis-inducing (GAIN) domain is a hallmark feature of adhe-sion G-protein coupled receptors (ADGRs), as this extracellular domain contains an integral agonistic sequence (Stachel) for activation via binding to the 7-transmembrane (7TM) helical domain of the receptor. Many ADGRs are autoproteo-lytically cleaved at the GPCR proteolysis site (GPS), an HXS/T motif within the GAIN domain. However, several ADGRs can be activated without GPS cleavage. We de-termined the crystal structure of the human ADGRB2/BAI2 hormone receptor (HormR) and GAIN domains and found that this ADGR is resistant to autoproteolysis despite the presence of a canonical HLS sequence at the GPS. By structural com-parison and with the help of molecular dynamics (MD) simulations we identified several unique structural features that are important for autoproteolytic cleavage, beyond the canonical HXS/T motif. Disruption of these features reduced autoproteo-lytic activity in ADGRL1/LPHN1 and restored cleavage competence of AD-GRB3/BAI3. Furthermore, conservation analysis indicates that wild type ADGRB2 and ADGRB3 are GPS cleavage-incompetent receptors." Authors & Affiliations "Fabian Pohl1, Florian Seufert2, Yin Kwan Chung3, Daniela Volke1, Ralf Hoffmann1, Torsten Schöneberg4, Tobias Langenhan3, Peter W. Hildebrand2, Norbert Sträter1 1 Institute of Bioanalytical Chemistry, Leipzig University, Deutscher Platz 5, 04103 Leipzig, Germany 2 Institute of Medical Physics and Biophysics, Leipzig University, Härtelstr. 16-18, D-04107 Leipzig 3 Rudolf-Schönheimer-Institute of Biochemistry, Division of General Biochemistry, Leipzig University, Johannisallee 30, D-04103 Leipzig 4 Rudolf-Schönheimer-Institute of Biochemistry, Division of Molecular Biochemis-try, Leipzig University, Johannisallee 30, D-04103 Leipzig" About Fabian Pohl "Mar 2023 – Today Postdoc, University Leipzig, Group of Prof. Langenhan Apr 2016 – Nov 2022 PhD candidate, University Leipzig, Group of Prof. Sträter Oct 2011 – Mar 2016 Master of Science in chemistry, University Leipzig Oct 2008 – Sep 2011 Bachelor of Science in chemistry, University Leipzig" Fabian Pohl on the web Langenhan Lab Structural studies of the CELSR1 extracellular region reveal a compact multidomain module of fourteen domains which regulates signaling Sumit Bandekar Abstract "Cadherin EGF Laminin G seven-pass G-type receptors (CELSRs) are conserved adhesion G protein-coupled receptors; they are essential for embryogenesis and neural development. CELSRs have large and enigmatic extracellular regions (ECRs) with nine cadherin repeats and a variety of adhesion domains which couple cell adhesion to signaling. CELSRs regulate planar cell polarity, including the closure of the neural tube. Despite numerous cell and animal studies, molecular details on CELSR proteins are sparsely available, precluding an integrative understanding of CELSR biology. Here, we report the 3.8 Å cryo-EM reconstruction of the CELSR1 ECR which enables unambiguous assignment of the 14 domains within the structure. These domains form a compact module mediated by robust and evolutionarily conserved interdomain interactions. This compact module provides a plethora of potential ligand binding sites for the various adhesion domains within the structure and hints at a model where the compact module could be pulled apart by robust mechanical force. We present biophysical evidence that the CELSR1 ECR forms an extended dimer in the presence of Ca2+, which we propose represents the cadherin repeats dimerizing in a configuration similar to protocadherins. We employ cellular assays with full-length CELSR1 and truncation constructs to assess the adhesive and signaling functions of this protein. We assign the N-terminal CADH1-8 module as necessary for cell adhesion and we show the C-terminal CAHD9-GAIN module regulates signaling. Our work provides molecular context to the literature on CELSR function and lays the groundwork for further elucidation of structure/function relationships." Authors & Affiliations "Garbett, Krassimira, Kordon, Szymon P., Shearer, Tanner, Sando, Richard C.*, and Araç, Demet* Department of Biochemistry and Molecular Biology, The University of Chicago Neuroscience Institute, Institute for Biophysical Dynamics, and the Center for Mechanical Excitability, The University of Chicago, Chicago, IL, 60637, USA. Department of Pharmacology, Vanderbilt Brain Institute, Vanderbilt University, Nashville, TN 37240, USA." About Sumit Bandekar "I am an NIH F32 postdoctoral fellow in the Araç Laboratory at the University of Chicago. I study adhesion GPCRs using structural biology perspective and I am interested in how the large multidomain extracellular region regulates receptor function. In my free time, I enjoy biking around Chicago and trying new breweries and restaurants." Sumit Bandekar on the web Araç Laboratory at UChicago X (Twitter) LinkedIn Unveiling the GPS Cleavage Mechanism in ADGRL1 with QM/MM Florian Seufert Abstract "Adhesion G-protein coupled receptors (aGPCR) are a family of 32 mammalian proteins with a defining conserved GPCR autoproteolysis inducing (GAIN) domain that catalyzes receptor self-cleavage at a GPCR proteolysis site (GPS). The autoproteolytic mechanism has been previously proposed, but remains to be validated.⁠ A previous computational study has uncovered variable flexible protein regions, whose dynamics mediate solvent-accessibility of the catalytically active GPS triad HL|S/T, however classical molecular dynamics approaches fall short of explaining the chemical reaction.⁠ Using a multiscale QM/MM approach - combining computational quantum mechanics with classical molecular dynamics - to study the GAIN domain cleavage mechanism of ADGRL1 reveals the sequence of events at the electronic level, suggesting relative energies for the individual states during the reaction, and provides insight into the structural determinants for a successful GPS cleavage exceeding the catalytically active GPS triad. By directly scanning and comparing energetic sequences of reaction steps, the most likely pathway and the individual contribution of surrounding protein residues can be elucidated. A stable π-edge contact with a conserved phenylalanine and a protonated glutamate side-chain catalyze the reactant conformation. MD simulations with the parameterized ester intermediate reveal a protonation-dependent dynamic desolvation of the GPS for subsequent ester hydrolysis by restricting water conformations. Mutational experiments on residues of interest showed that restoring the Phe-His interaction in the uncleaving ADGRB3 GAIN domain partially re-instates cleavage, while its deletion reduces cleavage in the ADGRL1 GAIN domain.⁠ We present a two-step GPS cleavage model and respective determinants of the reaction." Authors & Affiliations "Chung, Yin Kwan2, Pohl, Fabian2, Batebi, Hossein1 Sträter, Norbert3 , Langenhan, Tobias2 & Hildebrand, Peter Werner1 1 Institute of Medical Physics and Biophysics, Medical Faculty, Leipzig University, Germany 2 Rudolf Schönheimer Institute of Biochemistry, Division of General Biochemistry, Medical Faculty, Leipzig University, Germany 3 Institute of Bioanalytical Chemistry, Leipzig University, Germany" About Florian Seufert "Florian Seufert has studied Biochemistry in Leipzig, before joining the Hildebrand Lab in Leipzig for his PhD." Florian Seufert on the web LinkedIn ResearchGate < Previous Session Next Session >

Full Agenda Adhesion GPCR workshop 2024 CINVESTAV, Mexico City, Mexico October 23-25 Download PDF Program HERE < Back to Full Agenda Session I Tethered agonist - dependent/independent activation mechanism in AGPCRs Signaling Properties of ADGRL3 Signe Mathiasen An ECR-Mediated and TA-independent Mechanism of aGPCR Activation: Direct Communication of Extracellular Region with Transmembrane Domain in a Holo-Adhesion GPCR Demet Araç Heterogeneity of Tethered Agonist Signaling in Adhesion G Protein-Coupled Receptors Andrew Dates Discriminating between the extracellular scaffolding and G protein signaling roles of GPR56/ADGRG1 via the characterization of a non-cleavable point mutant knock-in mouse, H381S Frank Kwarcinski Tethered Peptide Activation Mechanism of Adhesion GPCRs Peng Xiao Signaling Properties of ADGRL3 Signe Mathiasen Abstract Only available for AGPCR 24 Workshop Attendees Authors & Affiliations "Rosell, Júlia (1) Holmkvist, Jesper L. (1) Arastoo, Mohammad Reza (1) Vejre, Phillip C. (1) Regmi, Rajesh (1) Perry-Hauser, Nicole A. (2) Bendix, Poul Martin (3) Javitch, Jonathan A. (2) Mathiasen, Signe (1) 1. Department of Biomedical Sciences, Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen, Denmark. 2. Departments of Psychiatry and Molecular Pharmacology and Therapeutics, Columbia University Vagelos College of Physicians and Surgeons, New York, New York, USA; Division of Molecular Therapeutics, New York State Psychiatric Institute, New York, New York, USA 3. Niels Bohr Institute, Faculty of Natural Sciences, University of Copenhagen, Copenhagen, Denmark" About Signe Mathiasen "2022-present Assistant Professor (Tenure Track) and Group Leader Department of Biomedical Sciences, University of Copenhagen. 2020 – 2022: Assistant Professor Department of Biomedical Sciences, University of Copenhagen. 2014-2021: Postdoc / Assistant Professor Department of Psychiatry, Columbia University, New York, USA. New York State Psychiatric Institute, Research Foundation for Mental Hygiene, New York, USA. Postdoc Supervisor Professor Jonathan Javitch 2013: PhD in Nanoscience/Biophysics. Department of Chemistry, University of Copenhagen, Copenhagen Denmark. PhD Supervisor Professor Dimitrios Stamou." Signe Mathiasen on the web University of Copenhagen Mathiasen Group An ECR-Mediated and TA-independent Mechanism of aGPCR Activation: Direct Communication of Extracellular Region with Transmembrane Domain in a Holo-Adhesion GPCR Demet Araç Abstract "According to the Tethered Agonist (TA)-mediated model of aGPCR activation, the ECR acts as a protective cap for the TA peptide to hide it within the GAIN domain. However, several recent observations suggest that other mechanisms of aGPCR activation are possible. For example, some aGPCRs do not undergo autoproteolysis, which is required for TA release. Even the aGPCRs that are cleaved do not always require cleavage for mediating some aspects of wild type functions. It has been suggested that the TA can regulate receptor signaling without coming out of the GAIN domain or by being partially exposed, however the recent TA-bound 7TM structures of multiple aGPCRs showed that the critical phenylalanine residue and other important TA residues have to reach deep into the 7TM orthosteric pocket for receptor activation, suggesting that non-release or partial release of the TA is unlikely to activate the receptor. In this talk, I summarize accumulating data from our lab and the aGPCR field that suggests an additional model in which the conformation of the Extracellular Region (ECR) has a direct role in modulating the 7TM signaling, independently of TA-mediated activation. Our results provide evidence for the ECR-mediated activation of aGPCR as a complementary mechanism for the TA-mediated activation of aGPCRs. Many biological forces are smaller than 200 pN, the force that is needed to separate the TA from the GAIN domain. To sense these smaller forces, and to regulate aGPCR function on and off, a mechanism that does not depend on ECR dissociation and TA exposure might be at work. At low force or no force conditions, aGPCR may be reversibly regulated by binding and dissociation of a ligand to the ECR without ECR shedding and TA exposure. In this ECR-mediated mechanism of activation, the ECR-7TM communication is altered by transient interactions between ECR and 7TM. The TA peptide remains at its original position and is not involved in signaling. Because the TA-mediated mechanism is a “one and done” mechanism that is irreversible and prevents the receptor from going back to its inactive resting state, the ECR-mediated mechanism may operate in situations where a reversible regulation is needed. The ECR-mediated mechanism may also enable responding to compressing forces on the receptor, that directly “push” on the protein. In cases where a large “pulling” force is executed on the ECR, the ECR may be removed from the 7TM releasing the tethered agonist and activating the aGPCR irreversibly but acutely. ECR-mediated mechanism opens new possibilities for drugging aGPCRs. Future work that dissects different activation mechanisms of aGPCRs in different physiological contexts will shed light on this fascinating family of receptors. " Authors & Affiliations "Kordon Szymon P.1, 2, Cechova Kristina3, Bandekar Sumit J.1, 2, Ethan Dintzner1, 2, Leon Katherine1, 2, Dutka Przemysław1, Siffer Gracie3, Kossiakoff Anthony A.1, Sando Richard 4, Vafabakhsh Reza3, Araç Demet1, 2 1. Department of Biochemistry and Molecular Biology, The University of Chicago, Chicago; 2. Neuroscience Institute, Institute for Biophysical Dynamics, and Center for Mechanical Excitability, The University of Chicago, 3. Department of Molecular Biosciences, Northwestern University; 4. Vanderbilt University" About Demet Araç "Demet was an undergraduate at Bilkent University in Turkey, where she majored in Molecular Biology and Genetics. She moved to the University of Texas Southwestern Medical Center at Dallas in 2000 to work with Dr. Jose Rizo-Rey as a graduate student to elucidate the mechanisms of neurotransmitter release. After finishing her graduate training, she joined Dr. Axel Brunger’s lab at Stanford University to study the structure and function of cell-adhesion proteins at the synapse. In 2013, Demet began her independent research career at the University of Chicago within the Department of Biochemistry and Molecular Biology." Demet Araç on the web Araç Laboratory at UChicago X (Twitter) Heterogeneity of Tethered Agonist Signaling in Adhesion G Protein-Coupled Receptors Andrew Dates Abstract Only available for AGPCR 24 Workshop Attendees Authors & Affiliations "Daniel T.D. Jones (Harvard Medical School); Jeffrey S. Smith (Harvard Medical School, Brigham and Women's Hospital); Meredith A. Skiba (Harvard Medical School); Maria F. Rich (University of Cincinnati School of Medicine); Maggie M. Burruss (Harvard Medical School); Andrew Kruse (Harvard Medical School); Stephen C. Blacklow (Harvard Medical School)" About Andrew Dates "Drew Dates received his B.S. in Biological Chemistry from Carnegie Mellon University in 2018. As an undergraduate, he studied opioid receptor trafficking and G protein conformational dynamics in the laboratories of Manojkumar Puthenveedu and Roger Sunahara, respectively. As part of his doctoral work in the Blacklow laboratory at Harvard Medical School, Drew studied structure-function relationships in the Adhesion Family of GPCRs." Andrew Dates on the web Harvard Medical School Discriminating between the extracellular scaffolding and G protein signaling roles of GPR56/ADGRG1 via the characterization of a non-cleavable point mutant knock-in mouse, H381S Frank Kwarcinski Abstract Only available for AGPCR 24 Workshop Attendees Authors & Affiliations ""Tyler F. Bernadyn, Mariane Nascimento, Xinyi Lu, Pauline L. Pan, Michael Holinstat and Gregory G. Tall Department of Pharmacology, University of Michigan "" About Frank Kwarcinski "I am research faculty within the department of Pharmacology at the University of Michigan. I work under the supervision of Dr. Gregory Tall and our research primarily focuses on the structural and biochemical characterization of adhesion GPCRs (AGPCR) for mechanism of action and pathogenesis studies. We utilize several genetically modified mouse models to investigate requirements for receptor activator and continuously work to identify novel chemical modulators of AGPCRs through assay development and high-throughput screening efforts. I have previous work experience at two separate contract research organizations centered on assay development, and I am formally trained as a chemical biologist." Frank Kwarcinski on the web LinkedIn Tethered Peptide Activation Mechanism of Adhesion GPCRs Peng Xiao Abstract Only available for AGPCR 24 Workshop Attendees About Peng Xiao "I joined Prof. Jin-Peng Sun’s Lab since I graduated from Shandong University in 2012, and worked under the guidance of Prof. Sun as a postdoc/research associate/assistant professor. Since then, I have been working on dissecting the three-dimensional architecture and underlying molecular signaling mechanism of GPCR using cryo-electron microscopy (cryo-EM). So far, I have published 20 peer-reviewed papers as correspondence (or co- correspondence) or first (or co-first) authors, among which, four papers were published in Nature (2022a, 2022b, 2021, 2020); one paper was published in Cell (2021); on paper was published in Science (2023); two papers were published in Nat Chem Biol. (2022, 2018)." Peng Xiao on the web ResearchGate < Previous Session Next Session >

Your go-to guide for attending AGPCR24. Find essential travel information, from transportation and accommodation tips to local insights, to help you make the most of your trip and enjoy a smooth, stress-free conference experience. TRAVELING TIPS Adhesion GPCR workshop 2024 CINVESTAV, Mexico City, Mexico October 23-25 Register DO's and DONT's for travelers in Mexico Mexico travel advice *Travelers are encouraged to consult their country's embassy advisories as they may differ from the one posted above. The Canadian embassy provides a comprehensive list. We highly suggest reserving accommodations in the city's center as the housing around the venue is scarce, and some may not be suitable for a convenient stay. Do not hesitate to contact us if you have inquiries regarding the neighborhood of your choice. We suggest the following neighborhoods: Roma Norte, Juárez, Zona Rosa, Condesa, Cuauhtémoc, San Rafael Apart from the numerous Airbnb options in these neighborhoods, here are our recommendations for affordable hotels in order of preference: 1. Hotel Carlota : An industrial chic experience at economical pricing. It can include breakfasts. 2. Hotel Exe Suites Reforma 3. Hotel Maria Cristina : Old School “hacienda”-type hotel. 4. Hotel Laila 5. City Express by Marriott EBC Reforma 6. Hoteles PF Zona Rosa MAP AIR TRAVEL Mexico City is accessible by two major airports. Transportation options, approximate travel times, and approximate fares to and from the airports are listed. Fares are subject to change. Airfare and other travel arrangements are the full responsibility of aGPCR Workshop 2024 attendees. Aeropuerto Internacional de la Ciudad de México (AICM) Benito Juárez is located 15 km from the “Angel de la Independencia” and 13 km from Cinvestav. This airport is the best option for international travel. Time/Distance : Approximate 35-minute drive. Taxis : Taxis are available at the lower levels (outside of baggage claim) at each terminal. Fares are based on traffic conditions, but an average fare is $20-$30. Subway : The subway is only available at Terminal 1. If your flight arrives at Terminal 2, there is a shuttle to Terminal 1. At the subway station you can purchase a “Movilidad Integrada” card in order to access public transportation (subway, metrobus, bikes, bus, etc). Information from public transportation can be followed through Google Maps or City Mapper apps. Uber and Didi apps : Uber type applications are available in Mexico City and a safe option for transportation. Aeropuerto Internacional Felipe Ángeles (AIFA) is located 53 km from the “Angel de la Independencia” and 33 km from Cinvestav. Time/Distance : Approximate 60-minute drive. Taxis : Taxis are available at the lower levels (outside of baggage claim) at each terminal. Fares are based on traffic conditions, but an average fare is $30-$50. Public Transportation : We recommend taking a shuttle (available for travelers) from AIFA to AICM Terminal 1. TRAVEL & VISA INFORMATION We look forward to welcoming attendees. Please check if you need a visa or permit to enter Mexico. After identifying that a visa or permit is needed, foreign travelers should contact their country's Mexican Embassy Consular Section. To request a Letter of Invitation for visa purposes, contact us. MONEY EXCHANGE Mexican pesos are the currency of Mexico. Reliable exchange booths are available at airports, banks, and hotels. However, many businesses accept credit/debit cards. POSTER PRINTING Poster printing is the full responsibility of aGPCR Workshop 2024 attendees. Office Depot and Office Max offer services for poster printing. Close to Cinvestav, on “Instituto Politécnico Nacional” avenue, there are several small local businesses offering poster printing services. The average fare for poster printing is $10-$12. SIM CARD AND WIFI SIM cards can be easily purchased at the airport and Oxxo stores around the city. The average fare is $10-$12. Public Wi-Fi is available around the city, including at airports and subway stations, and just outside of Cinvestav. FOOD RESTRICTIONS Please share any food restrictions you might have (allergies, dietary, etc). We will try to accommodate you as best we can. GETTING TO THE VENUE UBER is the most recommended as it is a highly economical and safe way to reach Cinvestav from your housing accommodation. We recommend carpooling with others to reduce individual costs and to be environmentally friendly. Typical costs are $8 USD one way ($2 USD / person carpooling with four people). Register for the Adhesion GPCR 2024 Learn more about the Adhesion GPCR workshop 2024 Up About the event Learn more about the Adhesion GPCR workshop 2024 and its preliminary program. Up About the venue Discover Cinvestav, the host venue for the upcoming workshop. Up Abstract Submission Submit your research abstracts following our guidelines to present at the conference. Up Logo Contest Enter our logo contest for a chance to have your design represent the upcoming event.

Full Agenda Adhesion GPCR workshop 2024 CINVESTAV, Mexico City, Mexico October 23-25 Download PDF Program HERE < Back to Full Agenda Session VI AGPCRs shaping the nervous system ADGRCs in glutamatergic synapse formation, maintenance and degeneration Yimin Zou Antibody-drug conjugates targeting CD97 in glioblastoma Dimitris Placantonakis Adhesion G protein-coupled receptor latrophilin-3 (ADGRL3) modulation of dopaminergic neurotransmission Nicole Perry-Hauser ADGRCs in glutamatergic synapse formation, maintenance and degeneration Yimin Zou Abstract "ADGRCs (Celsr1-3) are components of the conserved planar cell polarity (PCP) pathway, which establishes and maintains cell and tissue polarity along the tissue plane in all tissues. Work from our lab showed that the PCP components, including ADGRC2 and ADGRC3, are localized in the developing and adult synapses and interact with synaptic scaffold proteins and glutamate receptors and are responsible for the formation and stability of the vast majority of glutamatergic synapses in the mammalian brain. Initial impairment of synaptic functions, which occurs early in Alzheimer’s disease, and subsequent massive loss of synapses are closely correlated with the decline of cognitive function. We showed that oligomeric Aβ binds to ADGRC3 on the same domain required for the interaction with Frizzled3, weakens their interaction and assists Vangl2 in disassembling synapses. Conditionally knocking out Ryk, required for Vangl2 function, protected synapses and preserved cognitive function in a mouse model for Alzheimer’s. Massive synapse loss in the prefrontal cortex is a hallmark of massive depressive disorder. Injection of low-dose ketamine, an antidepressant, can lead to acute (in several hours) and sustained (up to several weeks) antidepressive effects. Restoration of synaptic connections induced by low-dose ketamine has been found associated with the sustained antidepressive effects. We showed that ADGRC2 and ADGRC3 are required for the restoration of glutamatergic synapses in prefrontal cortical neurons of chronically stressed animals and their behavioral remission induced by low-dose ketamine. I will also present ongoing work on the signaling mechanisms of how ADGRCs regulate synapse formation, maintenance and plasticity." About Yimin Zou "I received Ph.D from University of California at Davis and San Diego in 1995 and then postdoctoral training from University of California, San Francisco in 2000. I was an assistant and then associate professor with tenure at the University of Chicago from 2000 to 2006 and moved to University of California San Diego as an Associate Professor in 2006. I became full professor in 2011 and Vice Chair of the Neurobiology Department at UC San Diego in 2012. I served as the Chair of the Neurobiology Department at UC San Diego from 2014 to 2017. My research focus is the mechanisms of neural circuit development, function and disease." Yimin Zou on the web UC San Diego Antibody-drug conjugates targeting CD97 in glioblastoma Dimitris Placantonakis Abstract "Glioblastoma (GBM) is the most common and aggressive primary brain malignancy. Several adhesion G protein-coupled receptors (aGPCRs) have recently been shown to play critical roles in GBM biology. We showed that CD97 (ADGRE5), in particular, drives tumor growth via effects on GBM stem cell self-renewal and metabolism, but also has a therapeutically favorable expression pattern: it is highly expressed in all GBM specimens, but is absent from healthy brain tissue. To exploit this expression profile, we have developed antibody-drug conjugates (ADCs) targeting CD97, by screening a synthetic human antibody library. We initially tested the ADC using in vitro WST-8 viability assays in human GBM cell lines and cell types that lack CD97. We observed significantly lower LD50 values in patient-derived and U87 GBM cell cultures vs. CD97-lacking cells. We also found significantly lower LD50 values when treating human GBM cells with the ADC (0.6788 nM), as compared to control ADC targeting RSV glycoprotein F (19.964 nM). In vivo intratumoral administration of the ADC in patient-derived GBM xenografts in the brain of immunodeficient mice resulted in significant reduction of tumor growth and prolongation of survival of host mice. Collectively, these data suggest that ADCs targeting CD97 impair tumor growth in preclinical GBM models and are promising candidates for future clinical trials." Authors & Affiliations "Groff, Karenna; Donaldson, Hayley; Anderson, Sebastian; Pitti, Kiran; Wang, Shuai; Park, Christopher; Hattori, Takamitsu; Koide, Shohei; Placantonakis, Dimitris New York University Grossman School of Medicine" About Dimitris Placantonakis "Dimitris Placantonakis is a neurosurgeon-scientist at NYU Grossman School of Medicine in New York. As a clinician, he specializes in surgical treatment of brain tumors. His laboratory studies oncogenesis in glioblastoma, the most common brain malignancy, and chromatin organization in human neural development. His group has been particularly interested in the role adhesion GPCRs play in glioblastoma biology and their therapeutic targeting." Dimitris Placantonakis on the web Placantonakis Lab Google Scholar LinkedIn Adhesion G protein-coupled receptor latrophilin-3 (ADGRL3) modulation of dopaminergic neurotransmission Nicole Perry-Hauser Abstract Only available for AGPCR 24 Attendees Authors & Affiliations "Nicole A. Perry-Hauser1,2, Arturo Torres Herraez1,2, Dan Lowes1,2, Ying Zhu1,2, Siham Boumhaouad1,3, Eugene V. Mosharov1,2,4, David Sulzer1,2,4, Christoph Kellendonk1,2, and Jonathan A. Javitch1,2 1Departments of Psychiatry and Molecular Pharmacology and Therapeutics, Columbia University, New York, NY 10032; 2Division of Molecular Therapeutics, New York State Psychiatric Institute, New York, NY 10032; 3 Physiology and Physiopathology, Faculty of Sciences, Mohammed V University, Rabat 1014, Morocco; 4Department of Neurology, Columbia University, New York, NY 10032" About Nicole Perry-Hauser "I am an associate research scientist endeavoring to build a productive, independent scientific research career in adhesion G protein-coupled receptor (aGPCR) biology. My long-term research interests involve resolving signaling pathways downstream of aGPCRs and establishing how/if these receptors’ adhesive properties influence signaling events, and in turn whether signaling impacts synapse formation and neuronal wiring. I initially became interested in GPCR signal transduction during my graduate training in the Department of Pharmacology at Vanderbilt University where I studied under the co-mentorship of Dr. Vsevolod V. Gurevich and Dr. Tina M. Iverson. I then pursued a postdoctoral research position under the mentorship of Dr. Jonathan A. Javitch in the Department of Psychiatry at Columbia University Irving Medical Center." Nicole Perry-Hauser on the web LinkedIn Research Gate Pubmed Dr. GPCR < Previous Session Next Session >

Full Agenda Adhesion GPCR workshop 2024 CINVESTAV, Mexico City, Mexico October 23-25 Download PDF Program HERE < Back to Full Agenda Complimentary Lunch < Previous Session Next Session >

Full Agenda Adhesion GPCR workshop 2024 CINVESTAV, Mexico City, Mexico October 23-25 Download PDF Program HERE < Back to Full Agenda Plenary Lecture Identification and Functional Characterization of Adhesion GPCRs As Steroid Hormone Receptors and Hearing and Balance Receptors Abstract Only Available for AGPCR24 Attendees About Jin-Peng Sun "Since starting my laboratory in 2011, I has focused on G protein coupled receptors, in particular, the ligand identification, physiological functions and molecular mechanism of biased signaling of GPCRs. Our first main research aspect is the identification of endogenous ligand of GPCRs. We have identified the receptor subfamily to sense the steroid hormones. For instance, membrane receptor GPR97 is able to sense glucocorticoid to mediate its rapid actions, the progesterone and 17-hydroxyprogesterone membrane receptor are GPR126. We also identified DHEA, DHEAS and DOC are endogenous ligands of GPR64 etc (Nature, 2021a, Nat Chem Biol 2022, PNAS 2022b). Our second main research aspect is dissecting the molecular mechanism underlying sensation of force, ordor, itch and taste by GPCRs. We have elucidated the mechanism of receptors' perception of itch, olfactory and force (Nature 2021b, 2022a, 2022b, 2023a, 2024). Our third main research aspect is working mechanism of GPCR. For arrestin mediated biased signaling, we have proposed the “flute model” and “poly proline region docking theory” etc. to explain the arrestin mediated GPCR functions (Nature communications, 2015, 2021, 2022; PNAS 2021, Molecular Pharmacology, 2017; Recommended by Faculty 1000, Nature Chemical Biology 2018). We identified that arrestin can mediated AT1R/TRPC3 or M3R/TRPC3 coupling by forming a complex of AT1R/β-arrestin-1/PLCγ/TRPC3 or M3R//β-arrestin-1/TRPC3 (Nature communications, 2017, Nature communications, 2018). We also identified that orphan receptor GPR64 forms complex with β-arrestin-1 and CFTR at apical membrane of efferent ductulus to regulate the salt/water metabolism (eLife 2018, Faculty 1000 recommendation). Our fourth main research aspect is ligand coding mechanisms and structural aided drug discovery of GPCR. We have decoded the mechanisms underlying recognition of fish oil (unsaturated fatty acids) and other lipids by GPCRs (Science 2023, Science Advance 2021, PNAS 2023, Nature Metabolism 2023), recognition of amine containing hormones by GPCRs (Cell 2021, 2023, Nature 2023b), bile acids or its derivatives by GPCRs (Nature 2020)." Jin-Peng Sun on the web Google Scholar LinkedIn < Previous Session Next Session >

Submit your abstract for the Adhesion GPCR Workshop 2024. Share your research, connect with experts, and be part of the leading GPCR scientific community. ABSTRACT SUBMISSION Adhesion GPCR workshop 2024 CINVESTAV, Mexico City, Mexico October 23-25 Submit your Abstract Here Abstracts configuration 1. Abstract category (oral presentations) 2. Title: Capitalize each word, 20 words max, Bold 3. Authors’ names in full: Last name, First name 4. Institutions 5. Abstract body 6. Funding source Oral presentations Extended deadline: August 1st Speaker name indicated in bold and underlined Indicate abstract category on top left corner (up to 2 categories max) Abstract categories Signaling Trafficking Metabolism Structure and Bioinformatics Health and Disease Immunology Nervous system Model Organism Phylogenetics and Evolution Aging Basic and Clinical Pharmacology Proteomic and Transcriptomics Biosensors and Molecular Tools Biomarkers Poster presentations Deadline: August 1 The presenter's name is indicated in bold and underlined Poster size Poster width: 90 cm max Poster height: 140 cm max Register for the Adhesion GPCR 2024 [ Registration extended until September 15th ] Learn more about the Adhesion GPCR workshop 2024 Up About the event Learn more about the Adhesion GPCR Workshop 2024 and its preliminary program. Up About the venue Discover Cinvestav, the host venue for the upcoming workshop. Up Traveling Tips Find essential tips about Mexico City, including transportation options and local insights. Up Logo Contest Enter our logo contest for a chance to have your design represent the upcoming event.

Full Agenda Adhesion GPCR workshop 2024 CINVESTAV, Mexico City, Mexico October 23-25 Download PDF Program HERE < Back to Full Agenda Session VII Physiological and pathological roles of AGPCRs in the nervous system Uncovering the signaling pathway of the ADGRA homolog Remoulade in Drosophila Beatriz Blanco Redondo The Adhesion GPCR Latrophilin Interacts With The Notch Pathway To Control Germ Cell Proliferation Willem Berend Post Uncovering the signaling pathway of the ADGRA homolog Remoulade in Drosophila Beatriz Blanco Redondo Abstract "The Drosophila genome contains five loci encoding adhesion G-protein coupled receptors (aGPCRs). Phylogenetic analysis revealed that the remoulade (remo) gene is a homologue of the vertebrate aGPCR ADGRA family, sharing the same overall receptor domain structure. In vivo expression profiling has shown Remo expression in the central (CNS) and peripheral nervous systems (PNS) of third-instar larvae (L3) and adults. In L3 PNS specimen Remo is expressed in a subset of neurons expressing the DEG/ENaC channel pickpocket (PPK), which is involved in transduction of sensory information like nociception. remoKO larvae and animals, in which remo was knocked down in ppk-neurons through RNA interference, show a higher nocifensive response compared to wildtype remorescue controls indicating that remo is required in PPK-neurons for this behaviour. Furthermore, with the aim to analyse the biochemical properties of Remo, we performed immunoprecipitation analysis. We found that the receptor is cleaved despite the lack of a consensus GPS sequence. Hence, Remo is proteolytically processed, either by the GAIN domain or an alternative protease that cleaved Remo near the GPS. We also aimed at identifying the signaling pathway that Remo is involved in. The mammalian Remo homolog ADGRA2/Gpr124 cooperates with other GPCRs of the Frizzled family, and the transmembrane proteins RECK and Lrp5/6. Collectively these proteins form a cell surface complex that acts as a recognition platform for Wnt ligands. Knowledge of the structural dynamics of this complex is limited and pharmacological and in vivo systems that would allow its characterization are scarce. Remo may serve a role in this peculiar signaling pathway and require further analysis." Authors & Affiliations "Auger, Genevieve Marie1, Bigl, Marina1, America, Michelle2, Vanhollebeke Benoit2, Langenhan Tobias1 1Rudolf Schönheimer Institute of Biochemistry, Division of General Biochemistry, Medical Faculty, Leipzig University, Johannisallee 30, 04103 Leipzig, Germany 2Laboratory of Neurovascular Signaling, Department of Molecular Biology, ULB Neuroscience Institute, Université libre de Bruxelles (ULB), Gosselies B-6041, Belgium" About Beatriz Blanco Redondo "I studied Biomedicine at the University of Barcelona. After my bachelors, I moved to Germany where I obtained my Master’s of Science and PhD degree in Dr. Buchner’s group at the University of Wuerzburg. Shortly after receiving my PhD, I joined Dr. Neil Shneider’s group as a postdoctoral research scientist at Columbia University, New York, where I studied the mechanisms of motor neuron degeneration in Amyotrophic Lateral Sclerosis (ALS). In 2017, I joined the group of Prof. Langenhan where I am studying and characterizing newly generated adhesion GPCR receptors in Drosophila as a model organism for future pharmacological applications." Beatriz Blanco Redondo on the web Blanco-Redondo Lab LinkedIn Google Scholar X (Twitter) The Adhesion GPCR Latrophilin Interacts With The Notch Pathway To Control Germ Cell Proliferation Willem Berend Post Abstract Only available for AGPCR 24 Attendees Authors & Affiliations "Groß Victoria Elisabeth 1, Matúš Daniel 2,3, Kaiser Anette 4, Ließmann Fabian 5, Meiler Jens 5, Schöneberg Torsten 2,6, Prömel Simone 1 1 Institute of Cell Biology, Department of Biology, Heinrich Heine University Düsseldorf, Düsseldorf, Germany 2 Rudolf Schönheimer Institute of Biochemistry, Medical Faculty, Leipzig University, Leipzig, Germany 3 Department of Molecular and Cellular Physiology, Stanford University, Stanford CA, USA 4 Department of Anaesthesiology and Intensive Care, Medical Faculty, Leipzig University, Leipzig, Germany 5 Institute for Drug Discovery, Faculty of Medicine, Leipzig University 6 School of Medicine, University of Global Health Equity, Kigali, Rwanda" About Willem Berend Post "Willem Berend Post is a PhD student in Cell Biology at Heinrich Heine University in Düsseldorf, Germany. His research focuses on the relevance of aGPCRs in physiology and signaling using both in vitro and in vivo approaches." Willem Berend Post on the web Cell Biology LinkedIn < Previous Session Next Session >

Full Agenda Adhesion GPCR workshop 2024 CINVESTAV, Mexico City, Mexico October 23-25 Download PDF Program HERE < Back to Full Agenda Welcoming Remarks < Previous Session Next Session >

Full Agenda Adhesion GPCR workshop 2024 CINVESTAV, Mexico City, Mexico October 23-25 Download PDF Program HERE < Back to Full Agenda Session IV AGPCRs signaling in the nervous system BAI1/ADGRB1-mediated Regulation of Mitochondrial Morphology in Axons Joseph Duman Bai1 Is A Novel Neuronal Substrate Of The Psychiatric Risk Kinase TNIK Simeon R. Mihaylov Intricacies Of Complex Assembly And Ligand Interaction In The Adhesion GPCR Latrophilin/Cirl Anne Bormann BAI1/ADGRB1-mediated Regulation of Mitochondrial Morphology in Axons Joseph Duman Abstract Only available for AGPCR 24 Attendees Authors & Affiliations "Tolias, Kimberley F., Departments of Neuroscience and Biochemistry & Molecular Biology, Baylor College of Medicine, Houston, TX 77030" About Joseph Duman "Joseph Duman is an Assistant Professor in the Department of Neuroscience at Baylor College of Medicine, where he studies BAI1's role in the brain and the radiobiology of treatments for brain cancer. He trained at the University of California at Berkeley with John Forte and the University of Washington with Bertil Hille, before joining Kim Tolias' lab at Baylor College of Medicine." Joseph Duman on the web Baylor College of Medicine Kimberley Tolias Lab Bai1 Is A Novel Neuronal Substrate Of The Psychiatric Risk Kinase TNIK Simeon R. Mihaylov Abstract Only available for AGPCR 24 Attendees Authors & Affiliations "Flynn, Helen R.2, Sampedro-Castaneda, Marisol1, Claxton, Suzanne1, Skehel, Mark2, Ultanir, Sila K.1 1Kinases and Brain Development Laboratory, The Francis Crick Institute, UK 2Proteomics Science Technology Platform, The Francis Crick Institute, UK" About Simeon R. Mihaylov " I am a postdoctoral researcher in the kinases and brain development laboratory led by Dr Sila Ultanir at the Francis Crick Institute in London, England. I undertook my BSc in Biochemistry and Genetics at the University of Sheffield followed up by obtaining a PhD in molecular neuroscience at the Sheffield Institute for Translational Neuroscience. I then moved to King's College London, where my interest and passion for kinases in brain health and disease developed. I initially worked on mTOR in the pathogenesis of Tuberous Sclerosis Complex and then moved to the Francis Crick Institute working on the psychiatric risk kinase TNIK. I also work on multiple other kinases in our laboratory implicated in various neurodevelopmental and neurodegenerative disorders. My expertise includes biochemical approaches, proteomics and transcriptomics to name a few. I have recently also developed a strong interest in adhesion GPCRs and in particular, Bai1. " Simeon R. Mihaylov on the web Crick LinkedIn X (Twitter) Google Scholar Intricacies Of Complex Assembly And Ligand Interaction In The Adhesion GPCR Latrophilin/Cirl Anne Bormann Abstract Only available for AGPCR 24 Attendees Authors & Affiliations "Körner, Marek Benjamin; Dahse, Anne-Kristin; Ljaschenko, Dmitrij; Scholz, Nicole (Rudolf Schönheimer Institute of Biochemistry, Division of General Biochemistry, Faculty of Medicine, Leipzig University)" About Anne Bormann "I am a biochemist by training and studied at Leipzig University from 2015 to 2020. During my Bachelor's in 2018, I sought practical lab experience and found a position as a student assistant in Dr. Nicole Scholz's lab. My main topics were protein biochemistry, Drosophila husbandry, and genetics. I was fortunate that Nicole offered me an opportunity to do my Master's and later on a PhD thesis in her group. Since then, I have broadened my horizons with many more techniques in vivo and in vitro, with a main emphasis on the Adhesion GPCR Latrophilin/Cirl. Currently, I am in the final stages of my PhD, and I am looking forward to new projects and ideas." Anne Bormann on the web Rudolf-Schönheimer-Institut für Biochemie Scholz Lab < Previous Session Next Session >

Full Agenda Adhesion GPCR workshop 2024 CINVESTAV, Mexico City, Mexico October 23-25 Download PDF Program HERE < Back to Full Agenda Closing remarks < Previous Session Next Session >

Full Agenda Adhesion GPCR workshop 2024 CINVESTAV, Mexico City, Mexico October 23-25 Download PDF Program HERE < Back to Full Agenda Session VIII Physiological and pathological roles of AGPCRs in the periphery ADGRG1/GPR56 regulates survival of terminally differentiated CD8+ T cells Cheng-Chih Hsiao Adhesion GPCR GPR116/Adgrf5 controls a lineage of anti-thermogenic adipocytes with implications for adaptive thermogenesis during prolonged cold exposure Anastasia Georgiadi ADGRF5-mediated regulation of cardiac health and disease Douglas Tilley ADGRG1/GPR56 regulates survival of terminally differentiated CD8+ T cells Cheng-Chih Hsiao Abstract Only available for AGPCR 24 Attendees Authors & Affiliations "Cheng-Chih Hsiao1,2, Hendrik J. Engelenburg1, Joost Smolders1,3, and Jörg Hamann1,2 1Department of Neuroimmunology, Netherlands Institute for Neuroscience, Amsterdam, The Netherlands; 2Department of Experimental Immunology, Amsterdam institute for Immunology and Infectious diseases, Amsterdam University Medical Center, Amsterdam, The Netherlands; 3MS center ErasMS, Departments of Neurology and Immunology, Erasmus Medical Center, Rotterdam, The Netherlands" About Cheng-Chih Hsiao "2012-2015: PhD in Immunology, University of Amsterdam; 2015-2019: Postdoctoral researcher, Amsterdam UMC; 2019-2022: Senior postdoctoral researcher, Netherlands Institute for Neuroscience; 2022 - present: Researcher associate, Netherlands Brain Bank" Cheng-Chih Hsiao on the web LinkedIn ReseachGate Adhesion GPCR GPR116/Adgrf5 controls a lineage of anti-thermogenic adipocytes with implications for adaptive thermogenesis during prolonged cold exposure Anastasia Georgiadi Abstract Only available for AGPCR 24 Attendees Authors & Affiliations "El Merabhi Rabih1*, Karagiannakou Vasiliki1*, Kardinal Ronja2, Jäckstein Michelle3 Yvonne, Kumar Jha Ankush1, Krokidi Sissy Thodou1, Wachten Dagmar2, Heeren Jörg3, Herzig Stephan1, Georgiadi Anastasia1 *equal contributions , Institutions : 1. Institute for Diabetes and Cancer, Helmholtz Centre Munich, Germany, 2. Institute of Innate Immunity, University Hospital Bonn, University of Bonn, 3. Centre for Experimental Medicine, Institute for Biocehmistry and Molecular Cell Biology, University Medical Center Hamburg-Eppendorf" About Anastasia Georgiadi "Head of Junior Group Endocrine Pharmacology, Institute of Diabetes and Cancer (IDC). Professional Background Since 2021 Group Leader, Institute for Diabetes and Cancer, Helmholtz Diabetes Centre, Munich 2018 - 2021 Project Team Leader, Institute for Diabetes and Cancer, Helmholtz Diabetes Centre, Munich 2015 - 2018 Postdoctoral fellow, Department of Adipose Tissue Biology, Institute for Diabetes and Cancer, Helmholtz Diabetes Centre, Munich 2012 - 2015 Postdoctoral fellow, Department of Cell and Molecular Biology, Karolinska Institute, Sweden" Anastasia Georgiadi on the web Endocrine Pharmacology Google Scholar ADGRF5-mediated regulation of cardiac health and disease Douglas Tilley Abstract Only available for AGPCR 24 Attendees About Douglas Tilley "Research in the Tilley laboratory focuses primarily upon aspects of GPCR regulation of cardiac function, inflammation and remodeling during HF or following acute cardiac injury. Much of this work centered on elucidating novel mechanisms by which β-adrenergic receptors impact cardiac structure and function, and has evolved to encompass their roles in regulating immune cell response to acute cardiac injury or chronic stress. Additionally, the lab has begun to investigate potential roles for previously unrecognized cardiac-expressed GPCRs in the regulation of physiologic/pathologic function in the heart in an effort to uncover novel therapeutic directions for HF, including adhesion GPCRs (AGPCRs). In all, research in the Tilley lab spans molecular pharmacology to pathophysiology studies focused primarily in the cardiovascular realm." Douglas Tilley on the web Lewis Katz School of Medicine at Temple University < Previous Session Next Session >

Meet the sponsors who make the Adhesion GPCR Workshop 2024 possible, supporting global collaboration and innovation in GPCR research. Home Registration Full Agenda Venue Travel Tips Sponsors Special Issue on Adhesion GPCRs OUR SPONSORS Adhesion GPCR workshop 2024 CINVESTAV, Mexico City, Mexico October 23-25 Sponsor Us Platinum Sponsors Bronze Sponsors Collaborating partners Contact us for sponsorship Register for the Adhesion GPCR 2024 Learn more about the Adhesion GPCR workshop 2024 Up About the event Learn more about the Adhesion GPCR workshop 2024 and its preliminary program. Up About the venue Discover Cinvestav, the host venue for the upcoming workshop. Up Abstract Submission Submit your research abstracts following our guidelines to present at the conference. Up Traveling Tips Find essential tips about Mexico City, including transportation options and local insights.

Full Agenda Adhesion GPCR workshop 2024 CINVESTAV, Mexico City, Mexico October 23-25 Download PDF Program HERE < Back to Full Agenda Session II AGPCR signaling pathways and trafficking Localization of putative ligands for adhesion G protein-coupled receptors in mouse tissues. Yuling Feng The ADGRF5/GPR116 receptor is a key regulator of lymphatic endothelial cell identity and function Monserrat Avila Zozaya Adhesion GPCR BAI1/ADGRB1 can block IGF1R-mediated growth signalling, increase radiosensitivity and augment survival in medulloblastoma. Erwin G. Van Meir Site Specific N-Glycosylation Of The N-Terminal Fragment Of ADGRG6 Drives Proteolytic Processing, Trafficking And Signalling Pal Kasturi Localization of putative ligands for adhesion G protein-coupled receptors in mouse tissues. Yuling Feng Abstract Only available for AGPCR 24 Workshop Attendees Authors & Affiliations "Shen,Tingzhen; Bernadyn,Tyler; Kwarcinski, Frank; Gandhi, Riya; Tall, Greg. University of Michigan." About Yuling Feng "I am currently a postdoctoral research fellow working with aGPCR pharmacology and physiology in rodents." Yuling Feng on the web LinkedIn The ADGRF5/GPR116 receptor is a key regulator of lymphatic endothelial cell identity and function Monserrat Avila Zozaya Abstract Only available for AGPCR 24 Workshop Attendees Authors & Affiliations "Serafin D. Stephen, Caron Kathleen M Department of Cell Biology and Physiology at UNC Chapel Hill 111 Mason Farm Road, MBRB, CB 7545. University of North Carolina at Chapel Hill, Chapel Hill, North Carolina, USA 27599" About Monserrat Avila Zozaya "My doctoral research was focused on investigating the cellular effects of missense lung cancer-mutations in the G-protein-coupled receptor Autoproteolysis-Inducing (GAIN) domain of Latrophilin 3 receptor under the mentorship of Dr. Antony Boucard. I am currently a postdoctoral researcher fellow in Dr. Kathleen Caron's laboratory at UNC. My research focuses on understanding the molecular mechanisms of adhesion GPCRs (aGPCRs) in lymphatic endothelial cells (LECs), a cellular model with unique junction arrangements where aGPCRs are mainly unexplored. " Monserrat Avila Zozaya on the web LinkedIn Caron Lab Antony Boucard Lab Dr. GPCR Adhesion GPCR BAI1/ADGRB1 can block IGF1R-mediated growth signalling, increase radiosensitivity and augment survival in medulloblastoma. Erwin G. Van Meir Abstract Only available for AGPCR 24 Attendees Authors & Affiliations "Yamamoto, Takahiro 1,2*, De Araujo Farias, Virginea 1, Zhu, Dan3; Kuranaga, Yuki1, Parag, Rashed Rezwan 1,4,, Osuka, Satoru1,5 1 Department of Neurosurgery, School of Medicine, University of Alabama at Birmingham, Birmingham, Alabama, USA. 2 Department of Neurosurgery, Kumamoto University, Kumamoto, Japan 3 Department of Neurosurgery, Emory University School of Medicine, Atlanta, Georgia, USA 4 Graduate Biomedical Sciences, University of Alabama at Birmingham (UAB), Birmingham, Alabama, USA 5 O'Neal Comprehensive Cancer Center, University of Alabama at Birmingham (UAB), Birmingham, Alabama, USA " About Erwin G. Van Meir "Dr. Erwin Van Meir is a professor in the UAB Department of Neurosurgery. He was trained in molecular biology at the Universities of Fribourg and Lausanne, Switzerland where he obtained his Ph.D. in 1989. Dr. Van Meir pursued postdoctoral work at the Ludwig Institute for Cancer Research in San Diego and joined the faculty of Emory University in 1998. His research interest lies in understanding the molecular basis for human tumor development and how to use this knowledge to devise new therapeutics that will improve patient survival. Van Meir’s research examines how genetic alterations and hypoxia induce changes in cell biology that promote tumor formation with particular emphasis on adhesion GPCRs ADGRB1 and ADGRB3. Van Meir has developed novel therapeutic approaches for cancer using oncolytic adenoviruses and anti-angiogenic molecules and is currently developing novel small molecule inhibitors of the hypoxia-inducible factor pathway and the epigenetic reader MBD2 (methyl CpG binding protein 2). His research aims to translate these novel agents to testing in clinical trials with the hope to develop novel medicines for cancer treatment." Erwin G. Van Meir on the web Google Scholar Site Specific N-Glycosylation Of The N-Terminal Fragment Of ADGRG6 Drives Proteolytic Processing, Trafficking And Signalling Pal Kasturi Abstract "ADGRG6 is a member of the adhesion G-protein-coupled receptor (aGPCR) family, known to play a role in myelination, placentation, blood vessel, and inner ear development. Like many other aGPCRs, ADGRG6 undergoes autoproteolysis at the GPCR-autoproteolysis site (GPS) enclosed within the larger GAIN domain to generate the N-terminal (NTF) and C-terminal fragments (CTF). These cleaved fragments join to form the heteromeric ADGRG6 receptor complex. ADGRG6 NTF has multiple extracellular domains like CUB, PTX, SEA, hormone binding domain, and the GAIN domain, which regulate G-protein signaling by binding to extracellular matrix proteins and mechanotransduction. The short stachel sequence at the extreme N-terminal end of the CTF functions as a tethered agonist to activate cAMP signaling. GPCR signaling and trafficking can be regulated by several different post-translational modifications (PTM). Stehlik et al. have reported that ADGRG6 expressed in lipopolysaccharide stimulated human umbilical vein endothelial cells is N-glycosylated. However, it is unclear which domains of ADGRG6 are N-glycosylated and how this might affect the overall molecular pharmacology of the receptor. Furthermore, are there spatial roles of N-glycosylation in ADGRG6 processing, trafficking, signalling and in-vivo functions? To address these gaps in knowledge, we used biochemical and cell-biological approaches using cell-lines overexpressing wild-type and N-glycosylation mutants of ADGRG6. We observed that N-glycosylation specifically takes place in the NTF and not the CTF of ADGRG6. Our results demonstrate that specific N-glycan residues in different domains of the extracellular NTF of ADGRG6 have distinct roles in ADGRG6 autoproteolysis, furin cleavage, membrane trafficking, and G-protein signalling. In the future, we plan to decipher the roles of N-glycosylation of ADGRG6 in organogenesis and tissue development using zebrafish models." Authors & Affiliations "Anandhu Jayaraman: Department of Biology, Ashoka University Prabakaran Annadurai: Department of Biology, Ashoka University. Currently: University of Leipzig Mansi Tiwari: Department of Biology, Ashoka University. Currently: University of Aberdeen Priyadatha Sajan: Department of Biology, Ashoka University, Currently: University of Groningen Nayonika Chatterjee: Department of Biology, Ashoka University Prateek Sibal: Department of Biology, Ashoka University" About Pal Kasturi "I received my bachelor’s degree in Physiology from Presidency College, University of Calcutta and went on to complete my masters from Madurai Kamaraj University. During my PhD training, I worked in the laboratory of Dr. Kathryn Defea at the University of California, Riverside. For my PhD thesis, I worked on non-canonical, scaffold driven signaling by protease activated receptor-2 (PAR2). I joined University of Texas Southwestern Medical Center, for my postdoctoral training. Here, I worked on the regulation of the Sonic Hedgehog pathway by GPCRs which localized to the primary cilia. I then joined the laboratory of Dr. Velia Fowler, at the Scripps Research Institute, as a Judith Graham Poole postdoctoral fellow to work on the role of cytoskeletal proteins in megakaryocyte to platelet differentiation. I joined the Department of Biology at Ashoka University in 2020 as an assistant professor." Pal Kasturi on the web Ashoka University < Previous Session Next Session >

Full Agenda Adhesion GPCR workshop 2024 CINVESTAV, Mexico City, Mexico October 23-25 Download PDF Program HERE < Back to Full Agenda Session VIII * Physiological and pathological roles of AGPCRs in the periphery The CELSR/ADGRC Homolog Flamingo Is Not Autoproteolytically Processed By The GAIN Domain Tobias Langenhan Characterization of Phenotypes Associated with GPR110 Deletion Hee-Yong Kim The Adhesion GPCR Cupidon Regulates Mating In The Closest Relatives Of Animals Alain Garcia De Las Bayonas Critical role for CD97/ADGRE5 in the induction of allergic airway inflammation Gabriela Aust The CELSR/ADGRC Homolog Flamingo Is Not Autoproteolytically Processed By The GAIN Domain Tobias Langenhan Abstract Only available for AGPCR 24 Attendees Authors & Affiliations "Tobias Langenhan, Nicole Scholz, Genevieve M. Auger, Helen Strutt, David Strutt" About Tobias Langenhan "1997-2004: Medical school and Dr. med. Neuroanatomy (Würzburg, Germany); 2004-2005: M.Sc. Neuroscience (Oxford, UK); 2005-2009: D.Phil. Neuroscience (Oxford, UK); 2009-2016: Group leader, Institute of Neurophysiology (Würzburg, Germany); 2016: Heisenberg professorship (Würzburg, Germany); 2016-to date: Professor and Chair in Biochemistry (Leipzig, Germany)" Tobias Langenhan on the web Langenhan Lab LinkedIn Characterization of Phenotypes Associated with GPR110 Deletion Hee-Yong Kim Abstract "G-protein coupled receptor 110 (ADGRF1, GPR110), an adhesion GPCR recently deorphanized, plays an important role in in the development of neurons and cognitive function. Synaptamide, an endogenous ligand for GPR110, binds to the N-terminal G-protein autoproteolysis-inducing (GAIN) domain of GPR110, and activates GPR110/cAMP signaling. This activation promotes neurogenic differentiation of neural stem cells, neurite growth, and synaptogenesis of developing neurons. In addition, a significant role of GPR110 in blood brain barrier (BBB) function has been discovered. GPR110 is highly expressed in mouse and human NPCs and neurons, while its expression was absent in astrocytes. GPR110 is also highly expressed in the kidney, however, little is known about the function of this receptor in renal physiology. To extend our understanding of the role of GPR110 signaling in kidney, we evaluated the urine albumin level in mice devoid of GPR110 gene (GPR110 KO) compared to the wild type (WT). To provide the molecular basis for the renal phenotype, we analyzed in parallel differential expression of kidney proteins in GPR110 KO and WT mice by label-free LC-MS/MS and pathway analysis. We found that the albumin to creatinine ratio was significantly elevated in urine samples obtained from GPR110 KO mice, indicating glomerular filtration dysfunction. The change in protein expression of key proteins including VEGFA is associated with the abnormal renal phenotype of albumin urea in GPR110 KO mice. In addition to the central nervous system phenotype such as learning and memory deficit and BBB dysfunction, our study revealed a new renal phenotype associated with lack of GPR110 signaling. " Authors & Affiliations "Laboratory of Molecular Signaling, National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, USA" About Hee-Yong Kim "Senior Investigator and Chief of the Laboratory of Molecular Signaling at NIAAA, NIH" Hee-Yong Kim on the web NIH The Adhesion GPCR Cupidon Regulates Mating In The Closest Relatives Of Animals Alain Garcia De Las Bayonas Abstract "All animals develop through the recognition, adhesion, and fusion of a differentiated sperm and egg. Although fundamental, the evolution of gametogenesis and fertilization in animals is poorly understood. Recently, evidence for sex has been described in choanoflagellates, the closest living relatives of animals. Under nutrient depletion, the model choanoflagellate Salpingoeca rosetta forms distinct cell types that aggregate, fuse, and undergo meiotic recombination. Additionally, the bacterium Vibrio fischeri also induces mating in S. rosetta cultures, suggesting that multiple environmental cues can trigger sex. Importantly, the signaling pathways underlying sexual reproduction in these different contexts have not been investigated. In this study, we report the discovery of an adhesion GPCR, named Cupidon, that regulates the switch from vegetative growth to sexual reproduction in S. rosetta. We found that the knock-out of cupidon induces a gain in cell adhesion and cell fusion, resembling the mating behavior of wild-type cells under nutrient depletion. Cupidon mutants, similar to starved wild-type cells, upregulate various extracellular matrix-related genes, including teneurins and metalloproteases. Finally, we showed that nutrient availability controls the dissociation of the N-terminal fragment in Cupidon. Together, our results suggest that Cupidon prevents sexual reproduction in S. rosetta under high nutrient availability, by inhibiting genes involved in gamete recognition. " Authors & Affiliations "King Nicole, Howard Hughes Medical Institute and Department of Molecular and Cell Biology, University of California Berkeley" About Alain Garcia De Las Bayonas "Hi everyone! I am currently finishing my postoc in the laboratory of Pr Nicole King at UC Berkeley where I am studying the evolution of GPCR families in choanoflagellates, the sister group of animals. I have a particular interest in understanding the premetazoan function of adhesion GPCRs." Alain Garcia De Las Bayonas on the web King Lab Critical role for CD97/ADGRE5 in the induction of allergic airway inflammation Gabriela Aust Abstract Only available for AGPCR 24 Attendees Authors & Affiliations Coming Soon About Gabriela Aust Coming Soon Gabriela Aust on the web Coming Soon < Previous Session Next Session >

GPCR ecosystem , GPCR online course , GPCR scientist network , GPCR drug discovery , GPCR training program

Guests on The Web Maria Majellaro LinkedIn ResearchGate Ecosystem Johannes Broichhagen LinkedIn Google

Biotech founder Ajay Yekkirala shares how AI, GPCRs, and bold questions are driving next-gen pain therapeutics and drug discovery innovation. << Back to podcast list Strategic Partner(s) From Curiosity to Breakthrough: Ajay Yekkirala on GPCR Innovation What if the key to safer, more effective drugs lies in asking the right questions — and daring to challenge what’s “not possible”? In this episode, Dr. Ajay Yekkirala shares the pivotal moments that transformed him from a curious PhD student into a GPCR drug developer and entrepreneur. Dr. Ajay Yekkirala is a GPCR pharmacologist, biotech entrepreneur, and co-founder of Superluminal Medicines, a company using machine learning to unlock new GPCR-targeted therapies. In this wide-ranging conversation, he reflects on the mentors, failures, and bold questions that shaped his journey from academia to AI-powered drug discovery. Why This Matters Translating basic GPCR science into actual medicines is broken. Ajay unpacks why—and what it takes to fix it. AI is reshaping how we understand protein dynamics , but only when driven by deep biological questions. Young scientists are hungry for alternate career paths. This episode is a playbook for thinking bigger. Innovation doesn’t happen in isolation. Ajay reveals how humility, curiosity, and collaboration fuel the future of drug discovery. What You’ll Learn in This Episode How Ajay’s failed MD/PhD application rerouted his path toward a breakthrough GPCR research career The inside story behind founding Blue Therapeutics and targeting supraspinal pain pathway What it means to “teach AI protein dynamics,” and how Superluminal is using it to predict signaling bias The entrepreneurial lessons no one tells postdocs: how to pitch, fail, and build a team Why asking “what if it can be done?” is the heart of scientific innovation Who Should Listen PhD students and postdocs exploring biotech careers GPCR scientists interested in translational innovation Biotech investors and strategic leaders seeking new drug development models Anyone curious about where AI meets molecular pharmacology About Ajay Yekkirala Dr. Ajay Yekkirala is a molecular pharmacologist, biotech founder, and scientist whose career has been defined by bold questions and even bolder moves. Originally on track to pursue an MD/PhD, a rejection letter pivoted him into a PhD program at the University of Iowa, where he studied opioid pharmacology under the legendary Dr. Philip Portoghese. That “failure” became a launchpad: Ajay later joined the lab of Dr. Clifford Woolf at Boston Children’s Hospital and Harvard Medical School, where he deepened his understanding of pain biology and began dreaming bigger. Driven by the opioid crisis and the lack of non-addictive pain treatments, Ajay co-founded Blue Therapeutics, a biotech startup focused on targeting supraspinal GPCRs for chronic pain. But he didn’t stop there. Seeing the limits of traditional drug discovery, he later co-founded Superluminal Medicines, a company using machine learning to explore GPCR structure-function relationships and predict biased signaling with precision. Ajay’s work sits at the intersection of GPCR biology, AI, and translational medicine. He’s a strong advocate for cross-disciplinary thinking, mentoring young scientists, and building companies that solve real, unmet needs in human health. His story is one of relentless curiosity, humility in the face of complexity, and an unshakable belief in science’s power to do better. Ajay Yekkirala on the web Superluminal Medicines LinkedIn Tune in now to hear how asking “what if?” led Ajay Yekkirala to reshape the future of GPCR-targeted medicine. Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Recent Podcast Articles Asking Better Questions in Science: A Practical Guide for Emerging Researchers When the Islet Lit Up: Advancing GPCR Imaging in Native Tissue How Collaboration Sparked a GPCR Imaging Breakthrough in Chemical Biology Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

Dr. Michelle Halls reveals how organized GPCR signaling drives assay innovation and new therapeutic insights. << Back to podcast list Strategic Partner(s) Leadership, Impact, and GPCR Signaling with Dr. Michelle Halls In this episode Dr.Michelle Halls shares how dissecting the spatial organization of GPCR signaling opens new doors in drug discovery. From early discoveries in cyclic AMP signaling to uncovering ultrasensitive receptor responses at femtomolar ligand concentrations, her work highlights why receptor localization and protein complex assembly matter for therapeutic targeting. This conversation is especially valuable for scientists developing functional assays, fluorescence-based tools, and high-throughput GPCR screens. ⸻ Inside This Episode How ultrasensitive GPCR signaling emerges from pre-assembled receptor–effector complexes at the plasma membrane. Why receptor localization and scaffolding dramatically shift functional readouts in disease models. What early cyclic AMP assays revealed about spatial signaling long before high-content technologies existed. The moment when femtomolar ligand concentrations uncovered unexpected receptor sensitivity. How an integrated training and lab structure at Monash Institute of Pharmaceutical Sciences fosters innovation in functional assay development and GPCR research. ⸻ Why It Might Hit Home If you’ve ever: Faced unexpected assay behavior at ultra-low ligand concentrations, Balanced innovation with robust validation under real experimental constraints, Tried to map signaling heterogeneity in disease-relevant models, Built assays that need to work in real biology—not just on paper, …this episode will resonate. ⸻ About the Guest Michelle Halls is an Associate Professor at Monash University and Deputy Theme Leader of Drug Discovery Biology at Monash Institute of Pharmaceutical Sciences. She leads the Spatial Organisation of Signalling Laboratory, where her team investigates how GPCRs orchestrate localized signaling events, how these mechanisms are hijacked in disease, and how they can be leveraged for therapeutic innovation. Michelle earned her PhD in Molecular Pharmacology at Monash University, then trained in single-cell biology as an NHMRC CJ Martin Fellow at University of Cambridge. She established her lab in 2011, and today she is a Viertel Senior Medical Research Fellow. Her recognitions include the 2024 ASCEPT Achievement Award, the 2023 BPS Geoffrey Burnstock Prize, and the 2019 Faculty Future Research Leader Award. ⸻ More about Michelle Halls Monash Institute of Pharmaceutical Sciences Bluesky LinkedIn ⸻ Articles about this Podcast Episode How GPCR Spatial Signaling Sparked a Scientific Journey From Pipettes to Platforms: The Evolution of GPCR Research How GPCR Collaboration Built an Innovation Engine ⸻ 🎓 Want more like this? Get behind-the-scenes conversations, advanced assay development strategies, and practical GPCR tools inside Dr. GPCR Premium . Join a global GPCR community of scientists and biotech leaders. 👉 Join now Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Recent Podcast Articles Asking Better Questions in Science: A Practical Guide for Emerging Researchers When the Islet Lit Up: Advancing GPCR Imaging in Native Tissue How Collaboration Sparked a GPCR Imaging Breakthrough in Chemical Biology Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Strategic Partner(s) The Role of Quantitative Sciences in GPCRs with Dr. Nagarajan Vaidehi About Dr. Nagarajan Vaidehi "Nagarajan Vaidehi, Ph.D., is professor and chair of the Department of Computational and Quantitative Medicine (DCQM) at the Beckman Research Institute of the City of Hope in Los Angeles, CA. She is also the Associate Director of the City of Hope Comprehensive Cancer Center. Dr. Vaidehi received her Ph.D. in quantum chemistry from the Indian Institute of Technology in India, where she was honored with the Distinguished Alumni Award in 2016. Following her postdoctoral studies on protein dynamics simulation methods at University of Southern California, and at Caltech, she became the director of biomolecular simulations at the Materials and Process Simulation Center, Beckman Institute at Caltech. Dr. Vaidehi joined the Beckman Research Institute of the City of Hope in 2006 as a Professor and became chair of DCQM in 2018. She has advanced the use of computational methods to meet the challenges of designing therapeutics with lower off target effects. She is an internationally recognized biophysicist for her contributions in developing constrained molecular dynamics simulation methods with emphasis on application to G-protein coupled receptors and drug design." Dr. Nagarajan Vaidehi on the web City of Hope Google Scholar LinkedIn Dr. GPCR Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Recent Podcast Articles Asking Better Questions in Science: A Practical Guide for Emerging Researchers When the Islet Lit Up: Advancing GPCR Imaging in Native Tissue How Collaboration Sparked a GPCR Imaging Breakthrough in Chemical Biology Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Strategic Partner(s) Re-cap of Endocrine Metabolic GPCR 2024 with the Organizers About Dr. Aylin Hanyaloglu Dr. Aylin Hanyaloglu has been a Principal Investigator at Imperial College London since 2007. She received her BSc in Human Biology from King’s College London in 1997, and while her Ph.D. commenced at the MRC Human Reproductive Sciences Centre, Edinburgh, a move to Perth, Australia resulted in her Ph.D. in Molecular Endocrinology being awarded in 2002 with Distinction from the University of Western Australia. Dr. Hanyaloglu undertook her postdoctoral training at the University of California, San Francisco with Professor Mark von Zastrow where she identified novel core cellular machinery critical for G protein-coupled receptor trafficking and signaling. Her research focuses on understanding the fundamental cell biological mechanisms regulating GPCR activity, including spatial control of GPCR signaling and receptor crosstalk, and applying these mechanisms for distinct GPCRs in diverse physiological and pathophysiological systems, with particular focus on women's health, pregnancy, and nutrient sensing in the gut. Her work is currently funded by Biotechnology and Biological Sciences Research Council (BBSRC), Diabetes UK, Wellcome Trust, and the Medical Research Council. Dr. Aylin Hanyaloglu on the web LinkedIn Endocrine Metabolic GPCRs Researchgate Twitter Imperial College London Elsevier Loop Dr. GPCR About Dr. Caroline Gorvin "Dr. Caroline Gorvin is a Wellcome Trust & Royal Society Sir Henry Dale Fellow at the Institute of Metabolism and Systems Research, University of Birmingham. She obtained her PhD in 2012 from the University of Oxford, where her research focused on the cellular mechanisms by which mutations in a chloride-proton antiporter cause the renal disorder Dent’s disease. Caroline continued to undertake postdoctoral research in Oxford, investigating the signalling and trafficking of the G protein-coupled receptor (GPCR), calcium-sensing receptor, and its role in calcium homeostasis. Caroline moved to the University of Birmingham in 2018 to establish her research group investigating metabolic GPCRs. Her current research focuses on how metabolic GPCRs cross-talk and interact to regulate appetite and bone metabolism." Dr. Caroline Gorvin on the web University of Birmingham Endocrine Metabolic GPCRs Society of Endocrinology Google Scholar ResearchGate Loop Twitter Dr. GPCR About Dr. Alejandra Tomas "Dr. Alejandra Tomas is a molecular cell biologist and Senior Lecturer at the Department of Metabolism, Digestion and Reproduction, Imperial College London. She obtained a PhD in Biochemistry from University College London and spent several years in Switzerland working on the study of membrane trafficking processes in pancreatic beta cells before returning to the UK, first to her Department at UCL and then to lead a laboratory at Imperial following the receipt of an MRC New Investigator Award in 2015." Dr. Alejandra Tomas on the web Imperial College London Endocrine Metabolic GPCRs ResearchGate Google Scholar LinkedIn Twitter Dr. GPCR Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Recent Podcast Articles Asking Better Questions in Science: A Practical Guide for Emerging Researchers When the Islet Lit Up: Advancing GPCR Imaging in Native Tissue How Collaboration Sparked a GPCR Imaging Breakthrough in Chemical Biology Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Strategic Partner(s) Dr. Khaled Abdelrahman, Victoria Rasmussen and Madelyn Moore About Dr. Khaled Abdelrahman " Dr. Khaled Abdelrahman graduated in 2006 with a BSc in Pharmaceutical Sciences from Alexandria University (Egypt) followed by MSc in Pharmacology in the same university that was conferred in 2009. He joined the laboratory of Dr. William Cole at the University of Calgary in 2010 for his Ph.D. where he studied the molecular basis underlying altered cerebrovascular function and blood flow in type 2 diabetes. In 2015, He joined Dr. Stephen Ferguson’s laboratory in the Departments of Cellular & Molecular Medicine and Neuroscience at the University of Ottawa as a Postdoctoral Fellow to explore novel G protein-coupled receptor (GPCR) candidates that can be targeted pharmacologically to slow neurodegeneration. He has been also studying what aspects of GPCR signaling are regulated in a sex-selective manner and how this can influence drug discovery in the area of neurodegenerative diseases. He is also a Registered Pharmacist in Canada and held two of the most prestigious Clinician Postdoctoral Fellowships offered by Alberta Innovates and Canadian Institutes of Health Research. He received the Canadian Society of Pharmacology and Therapeutics Postdoctoral and Publication awards along with many Young Scientist Awards from the American Society for Pharmacology and Experimental Therapeutics. " Dr. Khaled Abdelrahman on the web Twitter PubMed Google Scholar Dr. GPCR About Victoria Rasmussen "Victoria Rasmussen is a graduate fellow in Dr. Thomas Sakmar’s laboratory at The Rockefeller University, where she study’s the signaling and degradation of G protein-coupled receptors. She completed her undergraduate education at Providence College, receiving a B.S. in Biology and a B.A. in psychology. During her time at Providence College, she received the Walsh Grant Fellowship to develop novel methods of synthesizing 2 -imidazoline scaffolds to be used as proteasome modulators in the laboratory of Travis Bethel. Victoria started her Ph.D. at the Tri-Institutional Ph.D. program in Chemical Biology, where she joined the lab of Thomas Sakmar at The Rockefeller University. She is currently working to understand the signaling and degradation of GPCRs in disease states to help test the feasibility of using protein-targeted degradation as a therapeutic strategy. " Victoria Rasmussen on the web Tri-Institutional PhD Program in Chemical Biology Rockefeller University LinkedIn Dr. GPCR About Madelyn Moore "Madelyn (Maddi) earned her B.S. in Biochemistry from the University of Minnesota-Duluth in 2020. In her time as an undergraduate, Maddi was a researcher in Dr. Amanda Klein's lab where she helped to investigate the role of various ATP-sensitive potassium channels in pain and opioid tolerance. From there, she went on to be a research technologist in Dr. Richard Vile's lab at Mayo Clinic where she aided the evaluation of tumor-specific oncolytic viruses. Maddi is currently a second year Ph.D. student in the Molecular Pharmacology and Therapeutics (MPaT) Graduate Program at the University of Minnesota. Advised by Dr. Lauren Slosky, she is working to understand the mechanism by which a new class of biased allosteric modulators for the neurotensin receptor 1 (NTSR1) act to attenuate the behavioral effects of methamphetamine." Madelyn Moore on the web MPaT PubMed LinkedIn Dr. GPCR Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Recent Podcast Articles Asking Better Questions in Science: A Practical Guide for Emerging Researchers When the Islet Lit Up: Advancing GPCR Imaging in Native Tissue How Collaboration Sparked a GPCR Imaging Breakthrough in Chemical Biology Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

A conversation with Prof. David Hodson on visualizing GLP-1 and GIP receptors in pancreatic islets and brain circuits to advance GPCR-targeted therapies for diabetes and obesity. << Back to podcast list Strategic Partner(s) Visualizing GLP-1 & GIP Receptors in Islets and Brain In this episode, Professor David Hodson discusses how GLP-1 and GIP receptors regulate metabolism across the pancreas and brain, and why visualizing receptor localization and signaling in real tissues is essential for advancing GPCR drug discovery . His team develops fluorescence-based and chemically engineered tools to study gpcr internalization and ligand engagement in intact islets and neuronal circuits — insights that inform next-generation functional assay development and translational therapeutic design. The conversation also highlights the role of interdisciplinary collaboration in accelerating innovation in diabetes and obesity research. Why this matters How receptor distribution in islets and brain circuits shapes incretin hormone drug effects Why visualization tools changed our understanding of GPCR signaling in metabolic tissues What collaborative chemistry enabled in designing receptor-targeted fluorescent ligands The moment when structural and imaging evidence clarified unexpected glucagon-derived peptide behavior How future metabolic therapies may evolve based on receptor cross-talk and tissue-specific engagement Who should listen Navigated complex datasets where interpretation depended on biological context Balanced innovation with the need for reproducible, well-controlled functional assays Worked across disciplines where chemistry, pharmacology, and physiology converge Questioned how drug action differs in real tissues vs. recombinant cell lines …this episode will resonate. About David Hodson Prof. David Hodson is the Robert Turner Professor of Diabetic Medicine at the University of Oxford , working within the Oxford Centre for Diabetes, Endocrinology and Metabolism. Originally trained as a Veterinary Surgeon , he completed postdoctoral research at the CNRS in Montpellier before establishing his independent laboratory at Imperial College London as a Diabetes UK RD Lawrence Fellow. He later served as Professor of Cellular Metabolism and Institute Deputy Director at the University of Birmingham. His group develops imaging and chemical biology tools to reveal how GLP-1 and GIP receptors operate within complex tissues, with direct relevance to type 2 diabetes and obesity therapy . David Hodson on the Web Radcliffe Department of Medicine Islet Biology Lab University of Birmingham Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Recent Podcast Articles Asking Better Questions in Science: A Practical Guide for Emerging Researchers When the Islet Lit Up: Advancing GPCR Imaging in Native Tissue How Collaboration Sparked a GPCR Imaging Breakthrough in Chemical Biology Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Strategic Partner(s) A Brief History of allosteric modulation with Dr. Arthur Christopoulos About Dr. Arthur Christopoulos " Arthur Christopoulos is the Professor of Analytical Pharmacology and the Dean of the Faculty of Pharmacy & Pharmaceutical Sciences, Monash University, Australia. His research focuses on novel paradigms of drug action at GPCRs, particularly allosteric modulation and biased agonism, and incorporates computational and mathematical modelling, structural and chemical biology, molecular and cellular pharmacology, medicinal chemistry, and preclinical models of behaviour and disease. His work has been applied to studies encompassing neurological and psychiatric disorders, cardiovascular disease, obesity, diabetes, chronic pain and addiction. He has received substantial, long-term support from international and national competitive, charitable and commercial sources, as well as being academic co-founder of three GPCR-focussed biotechnology companies. Professor Christopoulos has over 360 publications, including in leading international journals such as Nature,Science and Cell, and has delivered over 180 invited presentations. He has served on the Editorial Board of 8 international journals and was a Councillor of the International Union of Basic and Clinical Pharmacology (IUPHAR). He has also been the recipient of multiple awards, including the John J. Abel Award and the Goodman and Gilman Award from the American Society for Pharmacology and Experimental Therapeutics; the Rand Medal from the Australasian Society of Clinical and Experimental Pharmacologists and Toxicologists; the British Pharmacological Society’s Gaddum Memorial Award; the IUPHAR Sir James Black Analytical Pharmacology Lecturer; the GSK Award for Research Excellence and a Doctor of Laws (Honoris Causa) from the University of Athens. Since 2014, Clarivate Analytics have annually named him a Highly Cited Researcher in ‘Pharmacology & Toxicology’, and in 2021 also named him a Highly Cited Researcher in the additional category of ‘Biology & Biochemistry’. In 2017, he was elected a Fellow of the Australian Academy of Health and Medical Sciences, in 2018 as a Fellow of the British Pharmacological Society, and in 2021 he was elected a Fellow of the Australian Academy of Science for his seminal contributions to drug discovery. In 2023, he was elected a Fellow of the Pharmaceutical Society of Australia. " Dr. Arthur Christopoulos on the web Monash University Wikipedia Google Scholar LinkedIn Dr. GPCR AI Summary Quick recap Yamina and Arthur discussed Arthur's career journey in pharmacology, including his mentors and significant discoveries related to allosteric receptors. They explored the evolution of the field, allosteric modulation concepts, and potential therapeutic approaches involving autoantibodies and allosteric modulators. Additionally, they covered the importance of target product profiles, reproducibility in experiments, and collaborative efforts such as a potential book on GPCR history. Next steps - Arthur will continue to collaborate with other researchers and drug companies to advance the understanding and application of allosteric modulation. - Arthur will work on designing ligands for specific receptors, aiming to create biased agonists for therapeutic use. Summary Arthur's Career Journey and Allosteric Receptors Yamina and Arthur discussed Arthur's career journey and his contributions to the field of pharmacology, with a focus on allosteric receptors and their modulation. Arthur highlighted his mentors' influence, such as Fred Mitchelson and Nigel Burch, and significant discoveries like the concept of synthetic allosteric modulators by Bruns and Fergus. He also discussed the evolution of the field, from biochemical radioligand binding assays to cell-based functional assays, and the influence of Terry Kenakin and chemical programs on his later work. The conversation ended with Arthur's ongoing research and his development of a new operational model. Yamina emphasized the importance of understanding the historical context of the field and the significance of Arthur's contributions. Allosteric Modulation and Hybrid Molecules Arthur and Yamina discussed the development of an operational model for allosteric modulation, emphasizing the balance between mechanism and empiricism. Arthur shared his career journey, including his collaboration with Patrick Sexton and Jim Burch, and the discovery of hybrid molecules with functional selectivity. They also discussed the re-emergence of interest in certain programs, the importance of connections across receptor families, and the potential of hybrid molecules. Arthur's strategy of consulting drug companies and targeting their posters at conferences was also shared with Yamina. Pharmaceutical Industry Experiences and GPCR History Arthur shared his experiences in the pharmaceutical industry, highlighting the differences between big pharma and biotech. They discussed strategies for analyzing large compound screening data, emphasizing robust assays and addressing issues like shifting curves. Arthur recounted a 2004 visit to a pharma company using replicates in assays. Yamina proposed compiling a book on GPCR history through collaborative interviews, considering a symposium to align terminology. For their upcoming project, Yamina favored a conversational approach, while Arthur suggested a kickoff meeting, with Yamina planning chapters and interviews. Bias Mitigation in Symposium Ideas Arthur and Yamina discussed the concept of bias in the context of the history of the Symposium idea. They reviewed significant early papers related to the topic, including work by Brian Roth, Terry Kenakin, Bill Clarke, and Kelly Burke. They also discussed their own research on chemokine receptors and the importance of understanding the natural environment in drug discovery. Lastly, they touched on a project with Nicola Smith that challenged their previous theories. Allosteric Modulation and Drug Discovery Yamina and Arthur delved into the complexities of protein-protein interactions, specifically allosteric modulation. They discussed various modulatory elements, such as RAMPs, G proteins, and GRKs, with Arthur recounting his initial collaboration with Patrick Sexton on RAMPs and amylin receptors. They also delved into the different signaling of Class B receptors and the potential for modulation at various levels. The discussion underscored the potential of allosteric modulators as drugs, despite challenges in the past due to a lack of understanding about the principles involved. They highlighted the importance of fine-tuning the approach to suit different diseases and interdisciplinary collaboration. The discussion also emphasized the need for a disease-specific approach, considering the clinical context and dialing in the desired effect, as well as the significance of rational drug design principles. Allosteric Modulation and Autoantibodies Discussion Arthur and Yamina discussed the potential of autoantibodies and allosteric modulation in the context of disease and therapeutic approaches. Arthur explained the concept of endogenous allosteric ligands and the possibility of using a neutral allosteric ligand as a preferred therapeutic approach, emphasizing the importance of looking for low level cooperativity factors. They also discussed the potential of certain drugs, like flumazenil, as 'nails' or compounds that could be developed into medicines. The conversation highlighted the importance of establishing the correct disease context, setting up appropriate assays, and understanding the models for their work. They both agreed on the necessity of understanding the target product for an allosteric modulator and working backwards from there. TPP, Allosteric Modulators, and Reproducibility Yamina and Arthur discussed the concept of a target product profile (TPP) in drug development, with Arthur explaining its application in other contexts as well. Yamina appreciated Arthur's expertise and indicated she would be creating an outline for an episode on allosteric modulators. They highlighted the importance of reproducibility in scientific experiments, sharing personal experiences and anecdotes. They also discussed their upcoming trips to the GPCR Colloquium in California and current research in their fields. Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Recent Podcast Articles Asking Better Questions in Science: A Practical Guide for Emerging Researchers When the Islet Lit Up: Advancing GPCR Imaging in Native Tissue How Collaboration Sparked a GPCR Imaging Breakthrough in Chemical Biology Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

Full Agenda Adhesion GPCR workshop 2024 CINVESTAV, Mexico City, Mexico October 23-25 Download PDF Program HERE < Back to Full Agenda Student Flash Presentations Health and Disease, Metabolism, Nervous System, Proteomics and Transcriptomics, Receptor Structure, Signaling and Activation Mechanism Adgrg6/Gpr126 is Required for Myocardial Notch Activity and N-cadherin Localization to Attain Trabecular Identity Abhishek Kumar Singh Investigating The Role of ADGRB3 Loss of Expression in Brain Tumor Formation in Li-Fraumeni Syndrome Alex Torrelli-Diljohn GPR124 Mediates Adhesion Of Leukemic Stem Cells To Their Niche And Leads To Myeloid Skewing Emmanouil Kyrloglou A single cell GPCR map of thermogenic fat Vasiliki Karagiannakou GAIN Domain Dynamics And Its Relevance For Adhesion GPCR Signaling In Vivo Lara-Sophie Brodmerkel Novel isoforms of adhesion G protein coupled receptor B1 (ADGRB1/BAI1) generated from an alternative promoter in intron 17 Rashed Rezwan Parag Identification of Differentially Expressed Gpr116 (Adgrf5) Transcript Variants in Mouse Kidney Hailey Steichen Elucidating The Role Of GPR97/ADGRG3 In Neutrophil Biology Tyler Bernadyn Next Generation MBD2 inhibitors for Brain Cancer Therapy Jesse Stillwell Adgrg6/Gpr126 is Required for Myocardial Notch Activity and N-cadherin Localization to Attain Trabecular Identity Abhishek Kumar Singh Abstract Only available for AGPCR 24 Workshop Attendees Authors & Affiliations "Srivastava, Swati1; Singh, Abhishek Kumar1; Gunawan, Felix2; Gentile, Alessandra2; Petersen, Sarah C.3; Stainier, Didier Y.R.2; Engel, Felix B.1 1 Experimental Renal and Cardiovascular Research, Department of Nephropathology, Institute of Pathology, Friedrich-Alexander-Universität Erlangen-Nürnberg, Kussmaulallee 12, 91054 Erlangen, Germany 2 Developmental Genetics, Max-Planck-Institute for Heart and Lung Research, Ludwigstrasse 43, 61231 Bad Nauheim, Germany 3 Department of Developmental Biology, Washington University in St. Louis, 660 S. Euclid Ave, St. Louis, MO 63108, USA. Present address: Department of Neuroscience, Kenyon College, 203 North College Road, Gambier, OH 43022, USA" About Abhishek Kumar Singh "I am a doctoral student in the lab of Prof. Felix B. Engel. Since my undergraduate studies, I became fascinated with the class of adhesion GPCRs, owing to their potential, scarcity of knowledge on them, diverse expression profile, and the complexity with which they seem to be working. This made me pursue my higher education in the field of adhesion GPCRs. Accordingly, I worked with Prof. Hsi-Hsien Lin as summer intern twice, and finally joined the lab of Prof. Engel. I hope to develop my skillsets so as to be able to establish my own lab in future to work on adhesion GPCRs employing highly interdisciplinary field." Abhishek Kumar Singh on the web Uniklinikum Erlangen Google Scholar X (Twitter) Investigating The Role of ADGRB3 Loss of Expression in Brain Tumor Formation in Li-Fraumeni Syndrome Alex Torrelli-Diljohn Abstract "Li-Fraumeni syndrome (LFS) is a rare cancer predisposition syndrome caused by a germline mutation in the TP53 tumor suppressor gene. Glioblastoma (GBM) is the most prevalent central nervous system tumor in LFS, with TP53 mutations detected in 30% of sporadic GBMs. GBM is the most aggressive primary brain neoplasm that affects adults, with a median survival of 12-15 months. Recent studies implicate the dysregulation of adhesion G-Protein coupled receptors (GPCRs) in GBM development. Brain angiogenesis inhibitor 3 (BAI3/ADGRB3), a member of the BAI1-3 subfamily of adhesion GPCRS, has been observed to have low expression in brain tumors according to TCGA data, but the significance of this observation has not been explored. However, while its sister protein BAI1 has demonstrated tumor suppressor functions in the brain, it remains unclear whether BAI3 shares this role. To test this, an LFS mouse model (germline Tp53 deletion) with a second floxed allele under the control of Nestin-Cre was crossed to Bai3-/- mice. Preliminary findings indicate that the simultaneous loss of Bai3 and Tp53 expression in our mouse model increased spontaneous brain tumor formation incidence from 34% to 71%, in contrast to the loss of p53 alone. These observations lead me to hypothesize that ADGRB3 functions as a tumor suppressor in the brain, and its silencing, in the context of p53 mutation, facilitates GBM formation. Isolated GBM stem cells were collected for further genomic analyses and to test whether overexpression of BAI3 will save the tumor phenotype." Authors & Affiliations "Vukadin L, Park B, Mohamed M, Li H, Elkholy A, Torrelli-Diljohn A, Kim JH, Jeong K, Murphy JM, Harvey CA, Dunlap S, Gehrs L, Lee H, Kim HG, Sah JP, Lee SN, Stanford D, Barrington RA, Foote JB, Sorace AG, Welner RS, Hildreth BE 3rd, Lim SS, Ahn EE. A mouse model of Zhu-Tokita-Takenouchi-Kim syndrome reveals indispensable SON functions in organ development and hematopoiesis. JCI Insight. 2024 Mar 8;9(5):e175053. doi: 10.1172/jci.insight.175053. PMID: 38290089; PMCID: PMC10972584. University of Alabama at Birmingham" About Alex Torrelli-Diljohn "Alex completed his undergraduate & master’s degrees in Neurobiology & Cognitive sciences from the University of South Florida, where he researched early-onset Alzheimer’s disease in the lab of Dr. Angele Parent. He is interested in working on Li-Fraumeni syndrome and helping patients afflicted with this condition. He is also interested in working on Glioma Brain Organoid models." Alex Torrelli-Diljohn on the web The University of Alabama at Birmingham LinkedIn GPR124 Mediates Adhesion Of Leukemic Stem Cells To Their Niche And Leads To Myeloid Skewing Emmanouil Kyrloglou Abstract Only available for AGPCR 24 Workshop Attendees About Emmanouil Kyrloglou "Studied medicine at the University of Groningen. Now PhD-candidate at the Experimental Hematology lab of the University Medical Center Groningen (UMCG)." Emmanouil Kyrloglou on the web Adhesion GPCR Consortium LinkedIn A single cell GPCR map of thermogenic fat Vasiliki Karagiannakou Abstract Only available for AGPCR 24 Workshop Attendees Authors & Affiliations "Karagiannakou Vasiliki, El Merahbi Rabih, Herzig Stephan , Georgiadi A , Helmholtz Center Munich, Institute of Diabetes and Cancer" About Vasiliki Karagiannakou "MSc in Bioinformatics, PhD student since 2022 in the Institute for Diabetes and Cancer IDC, Helmholtz Centre Munich" Vasiliki Karagiannakou on the web Helmholtz Centre Munich GAIN Domain Dynamics And Its Relevance For Adhesion GPCR Signaling In Vivo Lara-Sophie Brodmerkel Abstract "Over the last years, Adhesion G Protein-coupled receptors (aGPCR) have been shown to play a crucial role in the perception of mechanical signals. However, the molecular details underlying their activation and how mechanical forces are translated into an intracellular response remains largely unknown. Recent Molecular Dynamics (MD) simulations of several aGPCRs predicted two flexible regions, termed flaps, located within the GPCR autoproteolysis inducing (GAIN) domain. These flaps could theoretically enable partial decryption of the Stachel through lateral movement and affect activation of the receptor independent of NTF-CTF dissociation. However, the physiological relevance of flap flexibility on receptor activation and signaling remains unclear. To investigate whether flexibility of GAIN flaps affects aGPCR function under native conditions, we strategically inserted specific mutations into the GAIN domain of the Latrophilin homologue Cirl in Drosophila melanogaster, with the intention to alter flap dynamics. Our goal is to understand if and how flap dynamics influence Cirl function and consequently the mechanosensory faculty of neurons in vivo. To this end, we combine behavioral, biochemical, immunohistochemical and functional readouts, with the overarching ambition to expand our knowledge on the mechanistic details underlying aGPCR activation in mechanosensation." Authors & Affiliations "Brodmerkel Lara-Sophie 1, Bormann Anne 1, Seufert Florian 2, Hildebrand Peter 2,3 ´, Ljaschenko Dmitrij 1´, Scholz Nicole 1´ 1Rudolf Schönheimer Institute of Biochemistry, Division of General Biochemistry, Medical Faculty, Leipzig University, Leipzig, Germany 2Institute for Medical Physics and Biophysics, Medical Faculty, Leipzig University, Leipzig, Germany 3Institute of Medical Physics and Biophysics, Charité – Universitätsmedizin Berlin, Berlin, Germany ´ correspondence: scholzlab@gmail.com , Dmitrij.Ljaschenko@medizin.uni-leipzig.de , peter.hildebrand@medizin.uni-leipzig.de *contributed equally" About Lara-Sophie Brodmerkel "I am a medical student and I´m currently working on my MD thesis in the lab of Dr. Nicole Scholz. We are investigating the relevance of GAIN domain dynamics for aGPCR signaling in Drosophila melanogaster." Lara-Sophie Brodmerkel on the web University of Leipzig Novel isoforms of adhesion GPCR B1 (ADGRB1/BAI1) generated from an alternative promoter in intron 17 Rashed Rezwan Parag Abstract "Brain-specific angiogenesis inhibitor 1 (BAI1) belongs to the adhesion G-protein-coupled receptors, which exhibit large multi-domain extracellular N-termini that mediate cell-cell and cell-matrix interactions. To explore the existence of BAI1 isoforms, we queried genomic datasets for markers of active chromatin and new transcript variants in the ADGRB1 (adhesion G protein-coupled receptor B1) gene. Two major types of mRNAs were identified in human/mouse brain, those with a start codon in exon 2 encoding a full-length protein of a predicted size of 173.5/173.3 kDa and shorter transcripts starting from alternative exons at the intron 17/exon 18 boundary with new or exon 19 start codons, predicting shorter isoforms of 76.9/76.4 and 70.8/70.5 kDa, respectively. Immunoblots on wild-type and Adgrb1 exon 2-deleted mice, reverse transcription PCR and promoter-luciferase reporters confirmed that the shorter isoforms originate from an alternative promoter in intron 17. The shorter BAI1 isoforms lack most of the N-terminus and are very close in structure to the truncated BAI1 isoform generated through GPS processing from the full-length receptor. The cleaved BAI1 isoform has a 19 amino acid extracellular stalk that can serve as a receptor agonist, while the alternative transcripts generate BAI1 isoforms with extracellular N-termini of 5 or 60 amino acids. Further studies are warranted to compare the functions of these isoforms and examine the distinct roles they play in different tissues and cell types." About Rashed Rezwan Parag "Rashed is from Bangladesh. He has received his BSc and MS degree from the Department of Biochemistry and Molecular Biology, University of Chittagong, Bangladesh. Before joining UAB as a graduate student, he worked in the EuGEF Research Group to identify novel prognostic biomarkers and therapeutic options for Metastatic Breast Cancer (BC) and Head and Neck Squamous Cell Carcinoma (HNSCC). Currently, he is working to elucidate the role of ADGRB1 and ADGRB3 in medulloblastoma (pediatric brain tumor)." Rashed Rezwan Parag on the web Google Scholar Identification of Differentially Expressed Gpr116 (Adgrf5) Transcript Variants in Mouse Kidney Hailey Steichen Abstract "Adhesion G protein-coupled receptors (aGPCRs) are important and understudied modulators of physiological processes. Previous work suggests that aGPCRs, and Adgrf5 in particular, undergo significant tissue-specific mRNA processing that results in holoreceptors with unique and variable N-terminal structures (Knierim et al. 2019). Recently, it was shown that transcripts of the postsynaptic aGPCR Latrophilin-3 (Lphn3/Adgrl3) undergo physiologically relevant alternative splicing, which determined heterotrimeric signaling through Gαs- or Gα12/13- mediated pathways (Südhof et al. 2024). These results demonstrate that identifying precise, tissue-specific transcript variants is critical to understanding the physiological relevance of aGPCRs. Moreover, these studies highlight the possibility that tissue expression of single aGPCRs is likely comprised of multiple transcript variants. We previously demonstrated that kidney-specific Adgrf5/Gpr116 knockout causes luminal membrane accumulation of V-ATPase in acid-secreting A-type intercalated cells (AICs) in the collecting ducts and a significant reduction in urine pH (Zaidman et al. 2020). Renal Adgrf5 is restricted to two distinct populations of cells: AICs and endothelial cells (ECs). We hypothesized that cell-specific Adgrf5 transcript variants are expressed in renal AICs and ECs, and therefore are activated by distinct mechanisms unique to the cellular microenvironment. We detected and aligned three Adgrf5 exons that undergo differential expression in the kidney: exons 2, 12, and 22. Adgrf5 transcripts in FACS-sorted GFP+ ICs do not contain the exon 2 variable region, or the alternative exons 12 and 22, while ECs contain all three. However, EC markers were detected in GFP+ ICs, demonstrating some EC contamination in the sorted ICs. Detection of transcripts that do, and do not, contain multiple variable regions suggests expression of multiple mRNAs in specific cells. These data demonstrate that Adgrf5 transcript variants are cell-specific in the kidney. Moreover, the complete repertoire of aGPCRs expressed in the kidney is undefined. We performed single-nucleus RNA sequencing on male and female kidneys. snRNAseq revealed abundant, cell-specific expression of six aGPCRs (Adgrl4, Adgre5, Adgrf1, Adgrf5, Adgrg1, and Adgrg3). Detection of these, as well as 18 other aGPCRs, was confirmed by PCR screening for GAIN/GPS domains on cDNA from whole-kidney lysates. These results reveal the complete set of aGPCRs expressed in the murine kidney. Future studies will focus on determining the physiological roles and tissue-specific variants of these receptors." Authors & Affiliations "Department of Biochemistry & Molecular Biology, University of New Mexico Health Sciences Center Xue, Jianxiang; Yan, Teagan; Eaton, Krystin, and Zaidman, Nathan" About Hailey Steichen "I currently work in Dr. Nathan Zaidman’s lab at the University of New Mexico Health Sciences Center. I am researching the physiological relevance of Adgrf5 (Gpr116) transcript variants in specific cell types in the kidney. I have also worked in the laboratory of Dr. James Bridges at National Jewish Health in Denver, CO researching molecular mechanisms of lung injury and repair mediated by Adgrf5. I received my MS in Applied Toxicology from the University of Washington, and my BA in Biology from Vassar College." Hailey Steichen on the web Zaidman Physiology Lab Elucidating The Role Of GPR97/ADGRG3 In Neutrophil Biology Tyler Bernadyn Abstract Only available for AGPCR 24 Workshop Attendees Authors & Affiliations "Gandhi, Riya; Chandan, Nancy; Kwarcinski, Frank; Smrcka, Alan; and Tall, Gregory G." About Tyler Bernadyn "4th year Pharmacology Ph.D. Student in Greg Tall's Lab." Tyler Bernadyn on the web LinkedIn Next Generation MBD2 inhibitors for Brain Cancer Therapy Jesse Stillwell Abstract "Medulloblastoma (MB) is one of the most lethal pediatric brain tumors. Standard of care for MB includes tumor resection, chemotherapy, and cranio-spinal radiation. This regimen has long lasting side-effects, including neuroendocrine and cognitive problems, and ~ 30% of patients still do not survive 5 years past diagnosis. Clearly, a new, less toxic therapeutic is needed. Our lab has previously shown that expression of adhesion GPCR BAI1 (ADGRB1) is lost by epigenetic silencing in MB. Restoration of ADGRB1 expression slowed tumor growth and improved survival in mice bearing MB xenografts. The ADGRB1 promoter is methylated in MB, and this allows for Methyl CpG Binding Domain protein 2 (MBD2) to silence the gene through recruitment of the NuRD silencing complex. KCC-07 is an inhibitor that prevents MBD2 from binding to DNA, allowing re-expression of BAI1. To further optimize the chemical scaffold, we synthesized KCC07 analogs that we’re testing for their ability to reactivate BAI1 expression. The current methods for testing KCC-07’s ability to reactivate ADGRB1 expression involve western blotting and RT-qPCR, both of which are semi-quantitative methods that require large numbers of cells and high volumes of analogs, creating a bottleneck in screening. These methods are time consuming, and their inherent variability makes precise quantification difficult. This research focuses on the design of a new endogenous ADGRB1 activation reporter assay to test analogs faster and with more reproducibility." Authors & Affiliations "Erwin Van Meir, University of Alabama at Birmingham/Sadanandan Velu, University of Alabama at Birmingham/Takahiro Yamamoto, Kumamoto University" About Jesse Stillwell "Jesse Stillwell is a 3rd year graduate student with a research focus in drug development. His project is drug discovery focused, with particular interest in use of a novel epigenetic therapy to reactivate ADGRB1 expression." Jesse Stillwell on the web Van Meir Lab – Heersink School of Medicine < Previous Session Next Session >

Full Agenda Adhesion GPCR workshop 2024 CINVESTAV, Mexico City, Mexico October 23-25 Download PDF Program HERE < Back to Full Agenda Leave for dinner reception Coming Soon < Previous Session Next Session >

A collaboration between chemistry and biology sparked a GPCR imaging breakthrough, leading to new chemical probes for GLP-1R visualization in real tissue. Home → Flash News → A GPCR imaging breakthrough that didn’t start in a grant proposal A GPCR imaging breakthrough that didn’t start in a grant proposal Published on December 3, 2025 Category It started with a cold email. A young chemist, Dr. Johannes Broichhagen, was asked if he could synthesize a molecule “when you’re back in Munich.” That small moment pulled him into islet biology, confocal imaging, and a collaboration that would reshape how GLP-1R is visualized in real tissue. The new blog takes you behind the scenes — the London trip, the early confocal experiments, the pivot to chemical probes, and the trust-driven partnership that sparked a new era in GPCR imaging. If you care about chemical biology, receptor visualization, or building tools that actually work in complex systems, this one is worth reading. 🔗 Read the full story : https://www.ecosystem.drgpcr.com/post/how-collaboration-sparked-a-gpcr-imaging-breakthrough-in-chemical-biology Previous Next Recent Articles Why Biotech Fundraising Fails Due to Intellectual Property Gaps 👉 Why has intellectual property become a first-order fundraising signal? Biotech fundraising has undergone a subtle yet significant shift. Capital still exists, but investors are making decisions earlier and filtering more carefully . As a result, intellectual property is no longer something that comes up late in the process. 👉 It has become an early signal of whether a biotech company is fundable at all. This shift does not mean founders need more patents or heavier legal Attila Foris 5 days ago The Hidden Operating Cadence That’s Actually Driving Your Biotech Founders love the idea that a new year, or a new quarter, will reset the company. But here’s the uncomfortable truth: 👉 Your biotech is already running on an operating cadence you didn’t consciously design. And that cadence is shaping everything: timelines, decisions, investor calls, BD traction, internal focus. Most CEOs think they’re steering the strategy. 👉 In reality, their operating cadence is steering them. And until you see it, you can’t change it. Operating cadence Attila Foris Dec 24, 2025 GPCR Binding Affinity Experiments: Interpreting Data With Confidence as We Head Into 2026 As scientists, we know curves don’t equal clarity. As 2025 comes to a close, this final edition of Weekly News focuses on how GPCR binding affinity experiments are interpreted—and how those interpretations quietly shape SAR, lead selection, and development timelines long before anyone notices. The goal isn’t more data. It’s cleaner interpretation. And that’s exactly what carries strong discovery programs into 2026. Dr. GPCR News Dec 18, 2025 Scientific Isolation: The Real Reason Early Biotechs Lose Traction The Quiet Drift You Don’t Feel Until It’s Too Late 👉 Every early-stage biotech reaches a moment where the science finally starts clicking… and the company quietly stops doing anything else. BD conversations stay warm but motionless. Investor updates become thinner. Internal meetings slowly morph into scientific colloquia instead of decision-making forums. 👉 The uncomfortable truth: your company is doing a lot of science and very little building. No drama. No blow-ups.Just Attila Foris Dec 17, 2025 Orthosteric Binding Experiments: How to Avoid the Most Common Data Pitfalls Binding affinity appears straightforward: add ligand, measure signal, fit a curve. Yet discovery teams routinely lose time and misallocate resources because the underlying biology behaves nothing like the idealized systems we learned in textbooks. GPCRs couple, decouple, isomerize, deplete tracers, and shift apparent affinity depending on stoichiometry and time. The result is a recurring pattern across programs—clean data that is not actually telling the truth. Orthosteric bi Terry's Desk Dec 16, 2025

Full Agenda Adhesion GPCR workshop 2024 CINVESTAV, Mexico City, Mexico October 23-25 Download PDF Program HERE < Back to Full Agenda Complimentary Reception dinner MENU Four Mushroom Soup Tomato, Panela Cheese, and Spinach tower with Oregano Vinaigrette Cane Sugar and Arbol Chile Lacquered Duck Monte Cristo Chocolate Cake Coffee or Tea Vegetarian option* -Mushroom-stuffed chiles on refried bean sauce- instead of the duck < Previous Session Next Session >