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<< Back to podcast list Dr. GPCR Podcast Strategic Partners Dr. Antony A. Boucard Jr About Dr. Antony A. Boucard Jr. Dr. Antony Boucard joined the Université de Sherbrooke (Québec, Canada) as a B.S. student of the Biochemistry program in 1994 from which he graduated in 1997. It is then that his interest bloomed for the study of GPCRs while joining the group of Dr. Richard Leduc and Dr. Gaetan Guillemette in the Pharmacology department at the Université de Sherbrooke. He completed a master’s degree in 2000 and a Ph.D. degree in 2003 with a particular interest in the cardiovascular system by investigating the structure of the Angiotensin and Urotensin receptors through various biochemical approaches centered in the elucidation of ligand binding pocket determinants. Motivated by a new ambition to study the nervous system, Dr. Boucard pursued postdoctoral training at the University of Texas Southwestern Medical Center in Dallas where he joined the group of Dr. Thomas Südhof . In this institution dear to the heart of GPCR enthusiasts given that its faculty personnel included Dr. Alfred Gilman , Nobel Laureate for his discovery of G proteins, Dr. Boucard ventured into the field of synaptic adhesion molecules which would eventually prompt him to investigate the role of a peculiar family of GPCRs belonging to the Adhesion subgroup. After a relocation to Stanford University where he pioneered work on ligand discovery for then orphan adhesion GPCRs, Dr. Boucard moved to Mexico City to establish himself as an independent investigator integrating the department of Cell Biology at the Centro de Investigación y de Estudios Avanzados del Instituto Politécnico Nacional (Cinvestav-IPN). Dr. Boucard´s lab focuses on molecular and cellular mechanisms underlying the function of adhesion GPCRs in the formation of synapses. Having a particular interest for a three-member family named latrophilins, his lab seeks to decipher the molecular code instructing adhesion events mediated by these GPCRs. The pharmacology of latrophilins brings about a great deal of challenges given that they are highly polymorphic proteins expressed as various alternatively spliced isoforms thus potentially resulting in differential modulation of cell signaling pathways. His lab highlighted the importance of splicing events in biasing latrophilins’ regulation of cyclic AMP pathways and for determining the magnitude of ligand selectivity. Additionally, his team is also interested in understanding the pathophysiological relevance of latrophilins’ function in neuropsychiatric disorders given their association with genetic susceptibility to the neurodevelopmental disorder known as attention deficit hyperactivity disorder (ADHD) but also to a comorbid clinical manifestation linked to addiction. He also actively volunteers as an Associate Professor of the non-governmental organization Institut des Sciences, des Technologies et des Etudes Avancées d’Haïti (ISTEAH) to help consolidate higher education in Haiti. Dr. Antony A. Boucard Jr. on the web Website LinkedIn Researchgate Loop Academia Pubmed Adhesion GPCR Consortium University of Haiti Dr. GPCR Ecosystem 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 How GPCR Collaboration Built an Innovation Engine From Pipettes to Platforms: The Evolution of GPCR Research How GPCR Spatial Signaling Sparked a Scientific Journey Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Dr. GPCR Podcast Strategic Partners Dr. Alix A. J. Rouault About Dr. Alix A. J. Rouault "My contribution to science began during the equivalent of U.S. masters training at the Université de Bretagne Occidentale (UBO; France). Under the leadership of Dr. Karine Pichavant , I contributed to the development of a drug to treat hypovolemic shock after severe hemorrhage. During this time, Dr. Olivier Mignen , the director of another research unit at the UBO recommended me to Dr. Julien Sebag , a researcher at the University of Iowa. I spent two years working with Dr. Sebag as an exchanged scholar while my student visa was in the work, during which time I thoroughly reviewed the literature on the melanocortin receptor accessory protein 2 (MRAP2), resulting in my first peer-reviewed publication in Biochimica et Biophysica Acta (BBA). I then undertook my first project where I demonstrated that MRAP2 regulates the signaling of multiple G protein-coupled receptors (GPCRs) through different structural regions. This project yielded my first, first author publication in BBA – Molecular Cell Research, and a book chapter for Neuromethods on a technique I adapted to measure the mitochondrial pyruvate oxidation in primary neurons. In 2017 I officially joined the PhD program in the Department of Molecular Physiology and Biophysics at the University of Iowa Carver College of Medicine, under the mentorship of Dr. Sebag. During my PhD, I continued my studies on MRAP2. I contributed to an In-vivo project that showed that MRAP2 regulates the growth hormone secretagogue receptor-1a (GHSR1a), the results of which are published in Nature Communications. Concurrently, I described the mechanisms by which MRAP2 regulates GHSR1a signaling; this project brought forth our NanoBiT-based arrestin recruitment assay. At the time, NanoBiT was a prototype technology we gained access to by collaborating with Promega. This powerful tool allowed us to create an assay that kinetically measured the arrestin recruitment to an activated GPCR for the first time. Using this novel technique, I showed that MRAP2 biased GHSR1a signaling and shut down its constitutive activity; this work resulted in a first author publication in Science Signaling. While writing my thesis, I published another paper in the Journal of Biological Chemistry which described the molecular mechanisms of MRAP2 regulation of the GHSR1a, and where I notably developed the C-terminal gate theory. This theory states that the post-translational modification of GHSR1a’ C-terminal tail is not a docking space for the arrestins, but rather a necessary modification leading to a structural change granting the arrestins access to the core of the receptor. Some of my data were also used in an In-vivo study published in iScience, showing the relevance of the MRAP2 regulatory effect on GHSR1a in pancreatic islets. Dr. Cone’s lab was a clear choice for a postdoc. Dr. Cone was the first to clone the melanocortin receptors (the GPCRs that led to the discovery of MRAP2), and his lab works is highly In-vivo oriented. Since I joined the lab, I became proficient in many In-vivo techniques, I adapted my arrestin recruitment assay to a high throughput screening format for drug discovery, I have started molecular work on the melanocortin receptors. I also invested a tremendous amount of time in developing my leadership skills. I spent time running for the chair of International Affairs for the U-M Postdoctoral Association (UMPDA). Further, I applied to create a scientific session at the American Physiology Summit (APS) 2024 dedicated to GPCR biased signaling. Dr. Lauren Slosky and Dr. Joshua Gross were enthusiastic about the idea and jumped on board. Our session was picked up by the APS. We were pleasantly surprised by the interest generated by our scientific session, Dr. Michel Bouvier accepted to open our session and will be followed by Dr. John McCorvy , Dr. Dylan Eiger , and Joshua Gross. We are very excited about this event. At this point in my career, I am creating connections with biomedical industry, assessing professional opportunities, and seriously weighing strengths of career options across sectors; however, academia does not make information about industry widely accessible to trainees. This is, in part, why I ran for, and was elected Chair of International Affairs of the University of Michigan Postdoc Association. I want to connect more trainees with diverse career resources to support professional decision-making. I am hopeful that my efforts to support the professional opportunities of my peers, in combination with my own scientific endeavors, will inform my future career decisions." Dr. Alix A. J. Rouault on the web University of Michigan Carver College of Medicine ResearchGate Google Scholar 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 How GPCR Collaboration Built an Innovation Engine From Pipettes to Platforms: The Evolution of GPCR Research How GPCR Spatial Signaling Sparked a Scientific Journey Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

Retreat 2023 About Program Registration Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule Interaction with the cell adhesion molecule NEGR1 affects mGluR5 cell signalling Date & Time Friday, November 3rd / 1:30 PM Abstract Coming Soon About Fabiola Ribeiro "Fabiola M. Ribeiro is an Associate Professor at the Universidade Federal de Minas Gerais (UFMG). She obtained her Ph.D. from UFMG in 2006 and, after that, she performed her postdoctorate studies at the University of Western Ontario, London, Canada, under Dr. Stephen Ferguson’s supervision. She returned to Brazil in 2010, when she founded her independent research group. Since then, Dr. Ribeiro has supervised eleven M.Sc. and six Ph.D. students, as well as five post-doctorate fellows. Nowadays, her research group comprises four undergraduates, two M.Sc., and six Ph.D. students, as well as five post-doctorate fellows and a lab technician. Dr. Ribeiro has 86 per reviewed scientific papers published in highly respected scientific journals, including 17 papers published in journals with impact higher than 7. Moreover, Dr. Ribeiro is the first or last author of 33 of these published articles. Dr. Ribeiro H factor is 28, according to Web of Science, and she is an affiliated member of the Brazilian Academy of Science. She was able to have several grants approved in Brazil and abroad, which have granted her research group a laboratory containing all the necessary equipment to perform state-of-the-art technologies. Dr. Ribeiro main scientific contributions include the study of the mechanisms involved in neurodegeneration and the characterization of neuroprotective drugs acting on the glutamatergic system. These drugs were shown to be very effective to rescue the cell death observed in a mouse model of Huntington’s disease (HD), decreasing synaptic loss and enhancing HD related memory impairment." Fabiola Ribeiro on the web Federal University of Minas Gerais, Brazil Pubmed ResearchGate Instagram Dr. GPCR Previous Event Next Event Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec 22nd GPCR Retreat Sponsored by

<< Back to podcast list Dr. GPCR Podcast Strategic Partners Dr. Adriano Marchese About Dr. Adriano Marchese Adriano Marchese is a Professor of Biochemistry at the Medical College of Wisconsin. Adriano received his Bachelor of Science degree in Pharmacology in 1991 from the University of Toronto. He continued his graduate studies at the University of Toronto where he earned his MSc (1994) and Ph.D. (1998) in Pharmacology. He then moved to Thomas Jefferson University in Philadelphia, PA, for his postdoctoral training in Jeff Benovic’s laboratory studying the regulation of G protein-coupled receptor trafficking and signaling. In 2004 Adriano joined the faculty of the Department of Pharmacology at Loyola University Chicago. In 2016 he decided to move his lab to the Medical College of Wisconsin in Milwaukee, WI. Adriano’s research has contributed to our understanding of the role that ubiquitin plays in GPCR signaling and trafficking. His laboratory is interested in understanding the mechanisms that govern spatial and temporal regulation of GPCR signaling by -arrestins and post-translational modifications (PTMs), such as phosphorylation, ubiquitination, and SUMOylation. His lab has shown a role for -arrestins and PTMs in GPCR trafficking and signaling and has leveraged this knowledge to reveal the spatial and temporal requirements for GPCR activation of signaling pathways related to cell survival, proliferation, and migration. The ultimate goal of Adriano’s research is to target novel aspects of GPCR signaling for therapeutic development. Dr. Adriano Marchese on the web Twitter LinkedIn Google Scholar Website Dr. GPCR Ecosystem 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 How GPCR Collaboration Built an Innovation Engine From Pipettes to Platforms: The Evolution of GPCR Research How GPCR Spatial Signaling Sparked a Scientific Journey 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 Coffee Break with pastries announcement of the aGEM award Complimentary < 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 Departure < Previous Session Next Session >

Home → Flash News → New cryo-EM insights reveal how extracellular domains communicate with transmembrane regions in holo-adhesion GPCRs, uncovering mechanisms behind receptor activation. Subscribe to the Dr. GPCR Newsletter 📰 and get the latest GPCR News delivered to your inbox ➡️https://www.ecosystem.drgpcr.com/adhesion-gpcrs/conformational-coupling-between-extracellular-and-transmembrane-domains-modulates-holo-adhesion-gpcr-function #gpcr #drgpcr Published on January 7, 2025 Category GPCR Weekly News New cryo-EM insights reveal how extracellular domains communicate with transmembrane regions in holo-adhesion GPCRs, uncovering mechanisms behind receptor activation. Subscribe to the Dr. GPCR Newsletter 📰 and get the latest GPCR News delivered to your inbox ➡️ https://www.ecosystem.drgpcr.com/adhesion-gpcrs/conformational-coupling-between-extracellular-and-transmembrane-domains-modulates-holo-adhesion-gpcr-function #gpcr #drgpcr Previous Next Recent Articles

Retreat 2023 About Program Registration Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule Complex Allosteric Cannabinoid Receptor Pharmacology Date & Time Friday, November 3rd / 11:30 AM Abstract Coming Soon About Robert Laprairie "Dr. Robert Laprairie is an Associate Professor and the Saskatchewan Research Chair in Drug Discovery and Development at the College of Pharmacy and Nutrition, University of Saskatchewan. Robert was the President and Director of Education for the Canadian Consortium for the Investigation of Cannabinoids (CCIC) and the 2021 Recipient of the William A. Devane Young Investigator Award from the International Cannabinoid Research Society (ICRS). Robert and his lab have been interested in the molecular pharmacology of cannabinoids for nearly 10 years and he has published more than 50 studies in the field." Robert Laprairie on the web University of Saskatchewan Pubmed Twitter Instagram ResearchGate Google Scholar Dr. GPCR Previous Event Next Event Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec 22nd GPCR Retreat Sponsored by

Full Agenda Adhesion GPCR workshop 2024 CINVESTAV, Mexico City, Mexico October 23-25 Download PDF Program HERE < Back to Full Agenda Dr. GPCR Community Presentation Breaking Barriers: My Journey from Mexico to the Heart of the Dr. GPCR Ecosystem and beyond 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 < 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 Coffee Break with lights snacks Complimentary < 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 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 >

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 >

Home → Flash News → A new study from the Hudson Lab at the University of Glasgow shows that the FFA receptor antagonist AH7614 is actually an inverse agonist - suppressing fat cell formation, boosting lipolysis and reducing glucose uptake. Explore how targeting FFA4 could help fight metabolic disorders. Catch up with the latest research conducted in the Hudson lab in Ep. 161 of the Dr. GPCR Podcast. Subscribe to the Dr. GPCR Newsletter 📰 and get the latest GPCR News delivered to your inbox ➡️https://www.ecosystem.drgpcr.com/gpcrs-in-cardiology-endocrinology-and-taste/inverse-agonism-of-the-ffa4-free-fatty-acid-receptor-controls-both-adipogenesis-and-mature-adipocyte-function #GPCR #drGPCR #FFA4 #metabolism #adipocytes” Published on April 7, 2025 Category GPCR Weekly News A new study from the Hudson Lab at the University of Glasgow shows that the FFA receptor antagonist AH7614 is actually an inverse agonist - suppressing fat cell formation, boosting lipolysis and reducing glucose uptake. Explore how targeting FFA4 could help fight metabolic disorders. Catch up with the latest research conducted in the Hudson lab in Ep. 161 of the Dr. GPCR Podcast. Subscribe to the Dr. GPCR Newsletter 📰 and get the latest GPCR News delivered to your inbox ➡️ https:// www.ecosystem.drgpcr.com/gpcrs-in-cardiology-endocrinology-and-taste/inverse-agonism-of-the-ffa4-free-fatty-acid-receptor-controls-both-adipogenesis-and-mature-adipocyte-function #GPCR #drGPCR #FFA4 #metabolism #adipocytes Previous Next Recent Articles

At Uppsala University, Jens Carlsson’s lab uses modeling to shape experiments—not just explain them. Discover how strategic collaboration drives real GPCR drug discovery impact. Home → Flash News → ep 175 with jens carlsson clip 2 If your model can’t change an experiment, what’s the point? Published on October 31, 2025 Category Dr. GPCR Podcast If your model can’t change an experiment, what’s the point? That’s the standard Dr. Jens Carlsson sets in his lab at Uppsala University. For him, modeling isn’t just about elegant simulations; it’s about impact . The kind of impact that shows up in how experiments are designed, which compounds get prioritized, and what gets synthesized next. Carlsson’s lab doesn’t work in isolation. They collaborate deeply with medicinal chemists, pharmacologists, and biotech partners to create workflows that connect virtual screening to synthesis and bioassay. Every step has a purpose. Every prediction feeds into a testable hypothesis. But the real differentiator? The way they collaborate: strategically, transparently, and without ego. His team is clear about the capabilities and limitations of their models, an honesty that builds long-term trust across disciplines. In GPCR drug discovery, where complexity is the rule and timelines are tight, this kind of cross-functional fluency is no longer optional. It’s the catalyst for turning insight into innovation. 🎧 Learn how Carlsson turns models into translational outcomes in this episode of the Dr. GPCR Podcast: model predict discover #DrGPCR #GPCR #CollaborationInScience #ComputationalChemistry #Pharmacology #DrugDesign Previous Next Recent Articles

Home → Flash News → pharmacology at your fingertips terrys corner launches Published on July 4, 2025 Category GPCR Weekly News Stronger pharmacology drives smarter decisions in GPCR discovery. Terry’s Corner is now live —an on-demand learning hub led by Dr. Terry Kenakin . New and unique lessons are released weekly on Tuesday. Elevate your drug discovery program with 45+ lessons yearly. Whether you’re refining assay strategy or evaluating data, these lessons give you the tools to think clearer and act faster. Explore on-demand lessons by Dr. Terry Kenakin with short videos, clear summaries, and curated references. Also in this week’s Dr. GPCR Weekly: ♦️ Yamina’s Corner—GPCR consulting to de-risk and accelerate your pipeline ♦️ Celtarys’ validated TR-FRET assay for CB1/CB2 ♦️ Chemokine-GPCR selectivity decoded ♦️ PTH1R structures reveal Gq bias mechanisms ♦️ NMBR simulations uncover new activation pathways ♦️ Axcelead & Superluminal expand collaboration ♦️ Industry momentum: collaborations, new data, and next-gen GLP-1 strategies Unlock deeper insight—starting now. ➡️ Read the newsletter: https://www.ecosystem.drgpcr.com/post/pharmacology-at-your-fingertips-terry-s-corner-launches #DrGPCR #GPCR #DrugDiscovery #pharmacology #biotechnews #terrykenakin #GPCRconsulting Previous Next Recent Articles

Join the forefront of GPCR research at the Dr. GPCR Summit! Embracing innovation and technology, we connect global scientific communities. Experience talks spanning time zones, with options for live or pre-recorded presentations. Uncover groundbreaking insights in GPCR science together. GPCR EVENT Dr. GPCR Summit 2022 Dr. GPCR Ecosystem Partners Welcome to the official page of the 3rd edition of the Dr. GPCR Summit This year the Summit will be held between October 10th and 16th. You can join us for free when you become a Dr. GPCR Ecosystem site member, which is also free! The content of the Summit will only be available to site-members who must be approved to join us. You can participate: As an attendee by becoming a site member. It only takes a minute, and it's free With your pre-recorded talk By presenting a poster on Wonder By giving a live talk. Space is limited, and we will do our best to accommodate your request For Speakers and presenters: Make sure you are registered as a site member to get access to the entire Summit for Free! Verify that you talk data and time are in your calendar. You can verify it too by checking out the schedule on our website. Live talks should be 30 mins with 15 mins Q/A. Live trainee talks should be 15 mins with 5 mins Q/A. All live talks will be on Zoom, the link will be added to your calendar invite and will be available here on our website but only visible to registered site-members. Similar to previous years: The meeting will be virtual (on Zoom) to host as many participants as possible Live talks will be hosted on Zoom from October 10th to the 14th Trainees are invited to participate by presenting a trainee talk, a poster, or a pre-recorded talk Presentation prizes will be available for the best trainee talks and posters We are also trying out a few new things: Networking and poster sessions on Wonder A full day dedicated to trainee talks Workshops and panel discussions In case you'd like to present your work, you'll need: Become an Ecosystem site member Pick the correct form and submit it before September 30th, 2022 You'll need a 1-minute video abstract in addition to the written version You can always email us with any questions and comments at Hello@DrGPCR.com << Submit your live talk details >> << Submit a pre-recorded talk >> << Submit your poster >> << Live talk schedule >> << Pre-recorded talk list >> << Poster presentation list >> Tags Dr. GPCR Summit Dr. GPCR Summit 2022 Dr. GPCR Summit 2022 Schedule Dr. GPCR Summit 2022 Details Dr. GPCR Summit 2022 Pre-Recorded Talks Dr. GPCR Summit 2022 Live Talks Dr. GPCR Summit 2022 Poster Presentations Submit Pre-Recorded Talk Presentation for Dr. GPCR Summit 2022 Submit Live Talk Presentation for Dr. GPCR Summit 2022 Submit Poster Presentation for Dr. GPCR Summit 2022

Home → Flash News → encoding and decoding selectivity and promiscuity in the human chemokine GPCR interaction network Published on July 7, 2025 Category GPCR Weekly News How do chemokines and GPCRs decode selectivity? A landmark Cell paper delivers the answer—mapping how conserved and variable sequence–structure elements govern interaction logic across 46 chemokines and 23 GPCRs. The result: a framework for designing ligands with altered receptor preferences. ♦️ Defines “public” vs. “private” binding determinants ♦️ Highlights role of structured + unstructured regions ♦️ Includes a web tool + viral chemokine engineering demo This is a must-read for GPCR modelers, immunopharmacologists, and ligand engineers. ➡️ Read the paper: https://www.cell.com/cell/fulltext/S0092-8674(25)00398-8 #DrGPCR #GPCR #Chemokines #StructuralBiology #Pharmacology #ProteinEngineering #Immunology #DrugDiscovery Previous Next Recent Articles

Explore Terry’s Pharmacology Vault. Master irreversible kinetics, target depletion, and structured tissue penetration in real drug discovery contexts. Home → Flash News → irreversible drugs post 3 Irreversible kinetics = strategic lever in drug design. Published on October 27, 2025 Category Terry's Corner Receptor pharmacology has evolved. Irreversible interactions are no longer niche curiosities — they’re strategic levers that shape how molecules behave in vivo and whether candidates advance or stall in discovery. Inside Terry’s Corner, you’ll gain access to focused, high-impact modules built for teams who need to engineer binding kinetics, not just potency . These lessons bridge molecular pharmacology with real-world design strategy, giving discovery teams the tools to make smarter decisions earlier in the pipeline. Here’s what’s covered in this week’s lesson: Target depletion vs. replenishment dynamics — how offset rates control exposure windows, shape therapeutic durability, and influence dosing intervals. Structured tissue penetration challenges — why high-affinity molecules stall at the periphery and how to optimize kinetic profiles for deeper reach. Quantifying irreversible activity (K_inact / K_I) — turning persistent binding into measurable design parameters that guide candidate optimization. Join to learn the same principles guiding successful drug programs today. 🟢 Browse the full video vault and stay ahead of the curve: ✳️ Courses by Terry | Dr. GPCR Ecosystem #GPCR #DrGPCR #Pharmacology #DrugDiscovery #Kinetics #ReceptorPharmacology #MedicinalChemistry #PKPD #DrugDevelopment Previous Next Recent Articles

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 >

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 >

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 Mexico City Nocturnal Tour, Food and drinks Coming Soon < Previous Session Next Session >

Home → Flash News → Science isn't always about eureka moments—sometimes it's about steady progress. In our latest Dr. GPCR Podcast episode, Ian Chronis shares his top aha moments, from learning the hard way about gel electrophoresis to discovering the hidden complexities of GPCR signaling. ✅ https://buff.ly/FTB69y9 #GPCR #DrGPCR #SciencePodcast #Pharmacology Published on April 22, 2025 Category Dr. GPCR Podcast Science isn't always about eureka moments—sometimes it's about steady progress. In our latest Dr. GPCR Podcast episode, Ian Chronis shares his top aha moments, from learning the hard way about gel electrophoresis to discovering the hidden complexities of GPCR signaling. ✅ https://buff.ly/FTB69y9 #GPCR #DrGPCR #SciencePodcast #Pharmacology Previous Next Recent Articles

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 >

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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 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 IX / Technology capsule: Light on aGPCR signaling and function NovoiSMART - A new platform for GPCR antibody drug discovery Abstract Developing monoclonal antibody drugs against GPCRs and other multi-pass transmembrane targets, such as ion channels, remains a significant challenge. Novoprotein developed a NovoiSMART technology, utilizing mRNA-based immunization, which can overcome these obstacles by producing high-quality antibodies that more accurately mimic natural protein structures. This approach contrasts with other antigen forms like peptides or DNA, which face limitations in structural integrity and immunogenicity. mRNA technology, demonstrated in the success of COVID-19 vaccines, is emerging as a promising method for antibody discovery. Several case studies of GPCR and other multi-pass transmembrane targets are presented, including GPRC5D, Claudin 6 and Napi2b. These studies show that mRNA immunization yields higher antibody titers and greater epitope diversity compared to other methods. These examples underscore the potential of NovoiSMART technology in developing highly specific antibodies for complex targets, with implications for overcoming challenges like drug resistance and tumor escape. About Gavin Zhang Gavin is a currently a director of business and operations at Novoprotein Scientific. His research experience includes phylogenetics and cancer epigenetics. Gavin Zhang on the web LinkedIn < Previous Session Next Session >

Home → Flash News → “Research is all about knowing when to walk and when to run.” –Ben Clements In Ep. 166 of the Dr.GPCR Podcast, hear how a postdoc is reshaping the conversation on opioid use, imposter syndrome, and the power of collaborative science. Why early-career voices are critical in GPCR drug discovery —and how lab culture makes all the difference. 🎧 Watch here: https://buff.ly/Kr3qKud #GPCRresearch #DrGPCR #GPCRpodcast #OpioidPharmacology #DrugDiscovery Published on May 20, 2025 Category Dr. GPCR Podcast “Research is all about knowing when to walk and when to run.” –Ben Clements In Ep. 166 of the Dr.GPCR Podcast, hear how a postdoc is reshaping the conversation on opioid use, imposter syndrome, and the power of collaborative science. Why early-career voices are critical in GPCR drug discovery —and how lab culture makes all the difference. 🎧 Watch here: https://buff.ly/Kr3qKud #GPCRresearch #DrGPCR #GPCRpodcast #OpioidPharmacology #DrugDiscovery Previous Next Recent Articles

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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 >