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- How Lipid Rafts Organize GPCR Signaling | Dr. GPCR Ecosystem
GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses
- Anything BUT GPCRs with Dr. Mikel Garcia-Marcos | Dr. GPCR Ecosystem
GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses
- Model. Predict. Discover. with Dr. Jens Carlsson | Dr. GPCR Ecosystem
GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses
- Dr. Simone Prömel & Dr. Ines Liebscher | Dr. GPCR Ecosystem
GPCR Ecosystem About Dr. Ines Liebscher Dr. GPCR Ecosystem Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses
- The Practical Assessment of Signaling Bias | Dr. GPCR Ecosystem
The Practical Assessment of Signaling Bias Dr. Terry Kenakin < Back Workshop Summary Join Dr. Terry Kenakin , a leading expert in pharmacology, as he unpacks the fascinating world of signaling bias in drug development! 🚀 This workshop will explore how different ligands (compounds) can stabilize unique receptor conformations, leading to distinct signaling outcomes—even when binding to the same receptor. Dr. Kenakin will explain that bias is not an exception but a fundamental principle of pharmacology, occurring whether or not researchers actively seek it. Through an engaging discussion, you'll explore: 🔹 What signaling bias is and why it matters 🔹 How receptor dynamics shape drug responses 🔹 Cutting-edge methods for quantifying bias 📊 🔹 Strategies to harness bias for better drug design —maximizing efficacy while minimizing side effects The session wraps up with a lively Q&A , allowing attendees to explore this game-changing topic in greater depth. Don't miss this opportunity to refine your understanding of bias as a tool, not an obstacle, in pharmacology! Key Highlights 🔍 Bias is Everywhere : Signaling bias naturally occurs in pharmacology—whether we look for it or not! 🧬 Receptor Flexibility : Ligands stabilize different receptor states, creating unique signaling pathways. 📏 Measuring Bias : New techniques allow us to quantify bias and compare drug efficacy more precisely. 💊 Therapeutic Potential : Understanding bias enables researchers to design drugs that target specific effects while avoiding unwanted side effects. 🗣️ Interactive Q&A : The discussion wraps up with an insightful Q&A, tackling real-world drug development challenges. Deep Dives & Insights 📌 Bias is Not an Anomaly—It’s a Feature! 🔹 Instead of avoiding bias, researchers can embrace it to refine drug responses. Dr. Kenakin challenges the traditional approach and encourages leveraging bias for better therapeutic outcomes. 📌 Receptors are Dynamic Players 🔹 Different ligands trigger unique receptor states, meaning the same receptor can signal in entirely different ways depending on what binds to it. Understanding these shifts can revolutionize drug development! 📌 Measuring Bias: A Quantitative Approach 🔹 The operational model provides a structured way to measure bias, combining affinity and efficacy. This allows for a side-by-side comparison of how different compounds influence receptor signaling. 📌 Bridging the Gap: Lab to Clinic 🔹 While measuring bias in a lab is relatively straightforward, translating these findings to clinical applications remains a challenge . The talk explores how to navigate this crucial gap. 📌 The Future of Drug Development 🚀 🔹 By integrating bias into drug design , researchers can craft more selective, effective, and safer therapies. This approach is shaping the next generation of precision medicine! Dr. Terry Kenakin’s workshop offers a fresh perspective on drug discovery . It shows that bias isn’t something to avoid—it’s something to utilize ! Whether you're a researcher, student, or industry professional, this session is packed with insights that will make you rethink your approach to pharmacology . Ready to explore the future of biased drug design? Let’s dive in! 🔬✨ AI Summary - May contain inaccuracies Materials: BIAS_WORKSHOP_PRINT .pdf Download PDF • 9.11MB BIAS_EXERCISE .pdf Download PDF • 721KB What would you like to learn today?
- About Dr. GPCR Ecosystem | Uniting the GPCR Community to Advance Drug Discovery
GPCR Ecosystem We unite the GPCR community to advance drug discovery. GPCR science and drug discovery by connecting people, data, and opportunities across the global GPCR ecosystem , and decision‑makers Access to all member perks for your entire team Product & service listings in ecosystem
- Newsletter for Adhesion GPCR Workshop 2024 | Dr. GPCR Ecosystem
Subscribe to the Adhesion GPCR Workshop 2024 newsletter. Get the latest updates, speaker announcements, and exclusive insights delivered straight to your inbox. Adhesion GPCR workshop 2024 CINVESTAV, Mexico City, Mexico October 23-25 Register AGPCR Newsletter Adhesion GPCR Consortium Newsletter - May 2024 Welcome to the 4th official Adhesion GPCR Consortium newsletter! We welcome suggestions, feedback, and announcements from the community.... Dr. GPCR News 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.
- Departure | Adhesion GPCR Workshop 2024 | Dr. GPCR Ecosystem
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 >
- Dr. GPCR Podcast Audience-Survey | Dr. GPCR Ecosystem
Join the Dr. GPCR Podcast community and shape our next season! Take our quick 5-minute audience survey to help us tailor our content to your needs. Your input matters in delivering exciting and informative episodes. Thank you for being part of our journey and for tuning in! Dr. GPCR Podcast Audience Survey Thanks for listening to this podcast episode Follow us on your favorite Podcast Player Be our Guest Listen and subscribe where you get your podcasts
- Donation for Adhesion GPCR Workshop 2024 | Dr. GPCR Ecosystem
Support the Adhesion GPCR Workshop 2024 with a donation. Help advance GPCR research, enable education, and connect the scientific community. DONATIONS Adhesion GPCR workshop 2024 CINVESTAV, Mexico City, Mexico October 23-25 Our Sponsors
- Posters | Adhesion GPCR Workshop 2024 | Dr. GPCR Ecosystem
Full Agenda Adhesion GPCR workshop 2024 CINVESTAV, Mexico City, Mexico October 23-25 Download PDF Program HERE < Back to Full Agenda Posters Interrogating The Role Of CELSR1 (ADGRC1) In Breast Cancer Caroline Formstone Generation and characterization of collecting duct specific GPR56 knockout mice Jianxiang Xue Anti-Tumorigenic Role of Brain Angiogenesis Inhibitor 3 (BAI3) in WNT-Activated Medulloblastomas Virginea de Araujo Farias Conformational And Functional Coupling Between Extracellular and Transmembrane Regions of a Holo-Adhesion GPCR Szymon P. Kordon Deorphanization Of The Adhesion GPCRs GPR110 and GPR116 Tingzhen Shen Self-Cleavage of GPR110 SEA Domain and Its Impact on GAIN Domain Autoproteolysis Bill Huang Tethered Agonist Dependent ADGRL3 Signaling Activity In The G12/13 Pathway Júlia Rosell Endocytic Cues Determine the Signaling Profile of Adhesion GPCR ADGRL1 / Latrophilin-1 Sheila Ribalta-Mena GPR110 modulates anxiety-like behaviors and memory function in mice potentially through neuronal and neuroimmune alterations during neurodevelopment Mariam Melkumyan Interrogating The Role Of CELSR1 (ADGRC1) In Breast Cancer Caroline Formstone Abstract "Breast cancer is the most common form of cancer amongst women. Ductal carcinomas are increasingly diagnosed but identifying which will progress to invasive disease remains difficult highlighting an urgent need for new biomarkers that distinguish ductal carcinomas on this basis. Planar cell polarity (PCP) proteins contribute to tumour growth and invasion. Recent studies identify CELSR1, a key PCP gene, as a novel biomarker for early-stage breast cancer. CELSR1 is reactivated in luminal-type ductal carcinomas. The impact of CELSR1 on cancer progression, however, is unclear. Our working hypothesis is that distinct CELSR1 protein isoforms differentially regulate tissue adhesiveness by influencing the stability/plasticity of cell-cell and cell-matrix contacts. Notably, our pilot data from luminal-type breast cancer cell lines representative of breast carcinomas with lower versus higher invasive potential reveal differential enrichment of CELSR1 protein isoforms. To test the specific hypothesis that biased expression of CELSR1 isoforms will predict invasive potential of a luminal breast carcinoma we will (a) determine, via loss-of-function assays in vitro and in vivo, whether CELSR1 protein isoforms differentially influence the stability of cell-cell and/or cell-matrix adhesions to dictate breast tumour invasive mechanism (b) quantify CELSR1 isoform expression (mRNA and protein) within patient luminal carcinoma samples exhibiting non-invasive or invasive features, the latter including heterogeneous tumours with mixed pathology. Through study of known protein isoforms of CELSR1, which would be missed in gene expression microarray analyses, we hope to illuminate the prognostic potential of CELSR1 for early-stage breast cancer." Authors & Affiliations "Klena, Ladislav University of Hertfordshire" About Caroline Formstone "Cell and developmental biologist with a focus on how planar cell polarity drives complex tissue morphogenesis. I study the cell and tissue level consequences of its failure in foetal development and of its reemployment in cancer" Caroline Formstone on the web University of Hertfordshire Generation and characterization of collecting duct specific GPR56 knockout mice Jianxiang Xue Abstract "GPR56 is a multifunctional adhesin G protein-coupled receptor involved in diverse biological processes. The role of GPR56 in the kidneys has been understudied. A recent study demonstrated that GPR56 in the glomerular endothelial cells promoted diabetic kidney disease progression via regulation of eNOS. Using RNAscope in situ hybridization (ISH) for GPR56, aquaporin 2 and NKCC2 (thick ascending limb, TAL marker), we detected GPR56 mRNA highly expressed in the collecting duct and TAL of the loop of Henle with limited expression in the proximal tubule. To determine the physiological role of GPR56 in the collecting duct, we generated a collecting duct-specific GPR56 knockout (GPR56CD-KO) mouse model by crossing GPR56flox (Control) with cadherin 16 Cre mice. The deletion of GPR56 in the collecting duct was confirmed by RNAscope ISH. GPR56CD-KO mice were born at predicted Mendelian frequencies, appeared grossly indistinguishable from Con mice, and developed normally. For baseline phenotypic characterization, blood gas analysis showed no differences in blood pH, blood HCO3-, blood Na+, or blood K+ between GPR56CD-KO and control mice. Metabolic cage experiments demonstrated no differences in fluid intake, urine volume, urinary pH or urine osmolality between genotypes in baseline. 24hr water deprivation experiment showed that GPR56CD-KO mice can concentrate urine as effectively as control mice. In conclusion, we successfully generated collecting duct-specific GPR56 knockout mouse and found no defective urine concentrating ability in GPR56CD-KO mice. This mouse model will be useful to delineate the collecting duct-specific role of GPR56 for renal function, including acid-base regulation." Authors & Affiliations "Hailey Steichen, Krystin Eaton, Teagan Yan, and Nathan Zaidman; Department of Biochemistry and Molecular Biology, University of New Mexico" About Jianxiang Xue "I am a postdoctoral researcher working in the Department of Biochemistry and Molecular Biology, University of New Mexico. I earned my PhD degree in Biomedical Sciences from the University of South Florida. During my graduate studies, using various transgenic mouse models and expertise in intestinal and renal physiology, I systematically characterized the function of sodium/hydrogen exchanger 3 in the intestine and kidneys for fluid and electrolyte homeostasis and acid-base balance. My predoctoral work was supported by an American Heart Association fellowship. Since staring my postdoctoral training, I have continued to develop my expertise to answer fundamental questions on adhesion GPCR in renal physiology and pathology. In my free time, I enjoy reading, workouts, and hiking." Jianxiang Xue on the web Zaidman Physiology Lab Anti-Tumorigenic Role of Brain Angiogenesis Inhibitor 3 (BAI3) in WNT-Activated Medulloblastomas Virginea de Araujo Farias Abstract Only available for AGPCR 24 Workshop Attendees Authors & Affiliations "Van Meir, Erwin G. University of Alabama at Birmingham" About Virginea de Araujo Farias "Brain Angiogenesis Inhibitor (BAI) proteins are members of group VII of the adhesion G protein-coupled receptor (aGPCR) family. BAI1-3 are highly expressed in the brain, where they participate in synaptogenesis and synapse maintenance. In cancers, BAI1-3 expression can be lost through epigenetic silencing, copy number loss or truncating mutations. In medulloblastomas (MB), BAI3 (ADGRB3) expression is specifically reduced in the WNT-activated group (WNT-MB), but not in the other three molecular groups. WNT pathway activation in WNT-MB is driven by mutations of the CTNNB1 gene, activating ß-catenin-dependent signaling; however, no interactions between BAI3 and the WNT signaling pathway have been described so far. MAGI3, a PDZ-containing scaffolding protein is known to downregulate WNT signaling by interacting with ß-catenin in gliomas, but it is unknown whether this involves BAI3. To explore a possible connection between BAI3 and ß-catenin signaling through MAGI3 in WNT-MB, we probed for potential protein-protein interactions using co-IP experiments. We found an interaction between BAI3 and MAGI3 in mouse brain lysates. Therefore, we hypothesize that re-expression of BAI3 in WNT-MB cells will restrain ß-catenin activity through the formation of a BAI3/MAGI3/ß-catenin complex, reducing their tumorigenic properties. To test this hypothesis, we created WNT-like MB cell lines stably expressing tet-on wild-type BAI3 or a BAI3 lacking the C-terminal PDZ-binding motif (PBM). We will present the effects of BAI3 re-expression on WNT-MB cells oncogenic properties and signaling." Virginea de Araujo Farias on the web Google Scholar Conformational And Functional Coupling Between Extracellular and Transmembrane Regions of a Holo-Adhesion GPCR Szymon P. Kordon Abstract "Adhesion G Protein-Coupled Receptors (aGPCRs) are key cell-adhesion molecules involved in numerous physiological functions. aGPCRs have large multi-domain extracellular regions (ECR) that mediate cell adhesion and play roles in transmitting extracellular signals to the inside of the cell. Ligand binding and mechanical force applied on the ECR regulate receptor function. However, how the ECR communicates with the seven-pass transmembrane domain (7TM) remains elusive, because the relative orientation and dynamics of the ECR and 7TM within a holoreceptor is unclear. Here, we describe the cryo-EM reconstruction of an aGPCR, Latrophilin3/ADGRL3, and reveal that the conserved GAIN domain, that directly precedes 7TM, adopts a parallel orientation to the membrane and has constrained movement. Single-molecule FRET experiments unveil three slow-exchanging FRET states of the ECR relative to the 7TM within the holoreceptor. GAIN-targeted antibodies, and cancer-associated mutations at the GAIN-7TM interface, alter holoreceptor conformations, and modulate downstream receptor signaling. Altogether, this data demonstrates conformational and functional coupling between the ECR and 7TM, suggesting an ECR-mediated mechanism for aGPCR activation." Authors & Affiliations "Cechova Kristina (3), Bandekar Sumit J.(1, 2), Leon Katherine (1, 2), Dutka Przemysław (1, 4), Siffer Gracie (3), Kossiakoff Anthony A. (1), Vafabakhsh Reza (3), Araç Demet (1, 2) 1. Department of Biochemistry and Molecular Biology, The University of Chicago, Chicago, IL, USA; 2. Neuroscience Institute, Institute for Biophysical Dynamics, and Center for Mechanical Excitability, The University of Chicago, Chicago, IL, USA; 3. Department of Molecular Biosciences, Northwestern University, Evanston, IL, USA; 4. Current affiliation: Department of Structural Biology, Genentech, South San Francisco, CA, USA" About Szymon P. Kordon "I am a postdoctoral scholar in the Araç Lab at The University of Chicago, studying the structure and function of aGPCRs. Utilizing synthetic antibody fragments, I aim to understand better the structural basis of the aGPCRs activation and signaling and to characterize ECR-mediated signal transduction at the molecular level." Szymon P. Kordon on the web Araç Laboratory at UChicago Deorphanization Of The Adhesion GPCRs GPR110 and GPR116 Tingzhen Shen Abstract Only available for AGPCR 24 Workshop Attendees Authors & Affiliations "Frank E. Kwarcinski, Gregory G. Tall (University of Michigan, Ann Arbor)" About Tingzhen Shen "A graduate student from Tall Lab, department of Pharmacology, University of Michigan, Ann Arbor." Tingzhen Shen on the web University of Michigan Self-Cleavage of GPR110 SEA Domain and Its Impact on GAIN Domain Autoproteolysis Bill Huang Abstract Only available for AGPCR 24 Workshop Attendees Authors & Affiliations "Hee-Yong Kim, Laboratory of Molecular Signaling, National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, Rockville, MD, USA" About Bill Huang "Researcher" Bill Huang on the web LinkedIn Tethered Agonist Dependent ADGRL3 Signaling Activity In The G12/13 Pathway Júlia Rosell Abstract Only available for AGPCR 24 Workshop Attendees Authors & Affiliations "Regmi, Rajesh (1), Perry-Hauser, Nicole A. (2), Javitch, Jonathan A. (2), Mathiasen, Signe (1) (1) Department of Biomedical Sciences, Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen, Denmark. (2) Department of Psychiatry and Molecular Pharmacology and Therapeutics, Columbia University Vagelos College of Physicians and Surgeons, New York, USA; Division of Molecular Therapeutics, New York State Psychiatric Institute, New York, USA" About Júlia Rosell "I am a first-year PhD student with two years of experience in the adhesion GPCR field. I completed my Master’s thesis on ADGRL3, where I conducted research involving mammalian cell cultures and techniques such as BRET assays and gene expression assays. Currently, my research focuses on the intracellular signaling of ADGRL3 from a single-molecule perspective and investigating how the binding of extracellular transsynaptic ligands modulates ADGRL3 activity, aiming to elucidate their interplay." Júlia Rosell on the web LinkedIn Endocytic Cues Determine the Signaling Profile of Adhesion GPCR ADGRL1 / Latrophilin-1 Sheila Ribalta-Mena Abstract Only available for AGPCR 24 Workshop Attendees Authors & Affiliations " Hernández-Aranda Judith 2, Correoso-Braña Kerlys 1, Vialou Vincent 3, Leduc Richard 4, Olivares-Reyes Jesús Alberto 2, Boucard Antony A1. 1 Department of Cell Biology, Centro de Investigación y de Estudios Avanzados del Instituto Politécnico Nacional (Cinvestav-IPN), México City, México. 2 Department of Biochemistry, Centro de Investigación y de Estudios Avanzados del Instituto Politécnico Nacional (Cinvestav-IPN), México City, México. 3 Sorbonne Université, Inserm, CNRS, Neurosciences Paris Seine, Paris, France. 4 Department of Physiology and Pharmacology, Université de Sherbrooke, Sherbrooke, Canada " About Sheila Ribalta-Mena " Cell Biology PhD student " Sheila Ribalta-Mena on the web CINVESTAV ResearchGate LinkedIn GPR110 modulates anxiety-like behaviors and memory function in mice potentially through neuronal and neuroimmune alterations during neurodevelopment Mariam Melkumyan Abstract "GPR110, an adhesion G protein coupled receptor (GPCR), is widely expressed in developing brains but diminishes in adult stage except in the hippocampus, a region involved in learning and memory. Ligand-induced GPR110 signaling stimulates neurogenesis and synaptogenesis during development, and the absence of the ligand-induced signaling causes object recognition and spatial memory deficits in adulthood and increased neuroinflammatory responses. Nevertheless, the role of GPR110 signaling in behavioral consequences has not been fully explored. This study aimed to understand the effects of GPR110 on mouse behaviors in relation to neurodevelopmental and neuroimmune gene and protein expression. Anxiety and memory function were tested using both male and female mice at 5-6 month of age. GPR110 knockout (KO) mice displayed trends for increased anxiety-like behaviors in the elevated plus maze test and in the open field test. Memory tests, including the novel object test and the radial 8-arm maze showed worsened spatial and reference memory in the GPR110 KO mice compared to wildtype mice. The y-maze showed a significant sex by genotype interactions with GPR110 KO male mice having increased number of correct alterations and errors, while the GPR110 KO females had fewer correct alterations and errors. RNAseq data indicated significantly impaired developmental gene expression for neuronal differentiation, axonogenesis, and synaptogenesis, as well as altered neuroinflammatory marker expression in GPR110 KO mouse brains. Further studies exploring the protein expression and neural activity of these mouse brain will give insight on the mechanism underlying the behavioral consequences associated with the GPR110 receptor. " Authors & Affiliations "Joel Toro, Bill Huang, Hee-Yong Kim Laboratory of Molecular Signaling, National Institute of Alcohol Abuse and Alcoholism, NIH" About Mariam Melkumyan "Mariam Melkumyan is a postdoctoral fellow at the Laboratory of Molecular Signaling studying the role of GPR110 in neurotransmission and neuroimmune activity involved in learning and memory, anxiety, and alcohol use. Mariam, originally from Armenia, completed her bachelor's degree in Neuroscience at American University in Washington, DC and her dual-title PhD in Neuroscience and Clinical and Translational Sciences at Penn State College of Medicine in Hershey, PA. Mariam started her postdoctoral training in February 2024 and is hoping to become an academic professor and mentor the next generation of scientists." Mariam Melkumyan on the web LinkedIn Google Scholar < Previous Session Next Session >
- From Curiosity to Breakthrough: Ajay Yekkirala on GPCR Innovation | Dr. GPCR Ecosystem
GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses
- Re-cap of Endocrine Metabolic GPCR 2024 with the Organizers | Dr. GPCR Ecosystem
GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses
- The Role of Quantitative Sciences in GPCRs with Dr. Nagarajan Vaidehi | Dr. GPCR Ecosystem
GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses
- GPCR Pharmacology, Career Twists & Serendipity with Sokhom Pin | Dr. GPCR Ecosystem
GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses
- A Brief History of allosteric modulation with Dr. Arthur Christopoulos | Dr. GPCR Ecosystem
GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses
- Visualizing GLP-1 & GIP Receptors in Islets and Brain | Dr. GPCR Ecosystem
GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses
- Dr. Khaled Abdelrahman, Victoria Rasmussen and Madelyn Moore | Dr. GPCR Ecosystem
GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses
- GPCR Assay Strategy, Bias, and Translational Drug Discovery | Dr. GPCR Ecosystem
GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses
- Leadership, Impact, and GPCR Signaling with Dr. Michelle Halls | Dr. GPCR Ecosystem
GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses
- Structure Based Design of Modulators of Purinergic GPCRs | Dr. GPCR Ecosystem
Explore structure-based design of purinergic GPCR modulators with NIH scientist Kenneth A. Jacobson, covering A3 receptor agonists and P2Y14 antagonists in chronic pain. < Back Structure-Based Design of Modulators of Purinergic GPCRs Mar 12, 2026 10 AM - 12:30 PM EST 🔒 Watch Recordings Access the full library of recorded Masterclass sessions. Get Live Updates Be notified when new live Masterclasses are scheduled. Introduction Purinergic GPCRs, including receptors for adenosine and extracellular nucleotides, play critical roles in inflammatory signaling, neurological processes, and chronic pain biology. This session examines how structure-based approaches have guided the discovery of selective ligands targeting these receptors. Drawing on decades of medicinal chemistry research, the course explores the development of A3 adenosine receptor agonists and P2Y14 receptor antagonists, integrating chemical synthesis, pharmacological characterization, and computational modeling. Participants will also examine emerging insights into extrahelical allosteric binding sites and their implications for GPCR modulation. The session is designed for PhD scientists, postdoctoral researchers, and industry professionals interested in translational pharmacology and GPCR-targeted drug discovery. Instructors Kenneth A. Jacobson Dr. Kenneth A. Jacobson is Chief of the Molecular Recognition Section in the Laboratory of Bioorganic Chemistry at the National Institute of Diabetes and Digestive and Kidney Diseases at the National Institutes of Health. A medicinal chemist specializing in the structure and pharmacology of G protein-coupled receptors and ion channels, his research focuses particularly on purinergic receptors for adenosine, ATP, and related nucleotides. He earned a B.A. from Reed College and a Ph.D. in Chemistry from the University of California, San Diego, followed by postdoctoral training at the Weizmann Institute of Science. Dr. Jacobson’s contributions to receptor pharmacology and medicinal chemistry have been recognized with numerous honors including the Medicinal Chemistry Hall of Fame, the Smissman Award, and the Goodman and Gilman Award. His expertise underpins the strategies discussed in this Masterclass. Matteo Pavan Matteo Pavan, PhD, is a molecular modeler and visiting postdoctoral researcher in the Laboratory of Bioorganic Chemistry at the National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, working under the direction of Dr. Kenneth Jacobson. His research focuses on developing computational pipelines for rational ligand design targeting therapeutically relevant receptors, with emphasis on GPCRs within the purinergic signaling family. His work integrates molecular dynamics, virtual screening, and early-stage lead optimization to support medicinal chemistry programs. He received his PhD in Molecular Sciences from the University of Padua in 2023 under the supervision of Prof. Stefano Moro. In this Masterclass, he presents computational and SAR studies identifying an extrahelical allosteric site on the A3 adenosine receptor. Upcoming Live Sessions
- Full Agenda for Adhesion GPCR Workshop 2024 | Dr. GPCR Ecosystem
Home Registration Full Agenda Venue Travel Tips Sponsors Special Issue on Adhesion GPCRs CINVESTAV, Mexico City, Mexico October 23-25 Full Agenda Adhesion GPCR workshop 2024 CINVESTAV, Mexico City, Mexico October 23-25 Download PDF Program HERE Oct 23 - 9:00 AM Registration & Coffee with light breakfast Read More 9:50 AM Welcoming Remarks Read More 10:00 AM Student Flash Presentations Health and Disease, Metabolism, Nervous System, Proteomics and Transcriptomics, Receptor Structure, Signaling and Activation Mechanism Abhishek Kumar Singh · Alex Torrelli-Diljohn · Emmanouil Kyrloglou · Vasiliki Karagiannakou · Lara-Sophie Brodmerkel · Rashed Rezwan Parag · Hailey Steichen · Tyler Bernadyn · Jesse Stillwell Read More 12:00 PM Coffee Break with lights snacks Read More 12:30 PM State of the Art Talk Adhesion GPCR in Mechanobiology Tobias Langenhan Read More 1:00 PM Plenary Lecture Identification and Functional Characterization of Adhesion GPCRs As Steroid Hormone Receptors and Hearing and Balance Receptors Jinpeng Sun Read More 2:00 PM Complimentary Lunch Read More 3:00 PM Session I Tethered agonist - dependent/independent activation mechanism in AGPCRs Signe Mathiasen · Demet Araç · Andrew Dates · Frank Kwarcinski · Peng Xiao Read More 4:30 PM Leaving for City Center Read More 5:00 PM Mexico City Nocturnal Tour, Food and drinks Read More Oct 24 - 9:00 AM Session II AGPCR signaling pathways and trafficking Yuling Feng · Monserrat Avila Zozaya · Erwin G. Van Meir · Pal Kasturi Read More 10:30 AM Coffee Break with lights snacks Read More 11:00 AM Session III Molecular tools and biosensors directed at AGPCR signaling and function Stephanie Häfner · Laurent Sabbagh · Ana Lilia Moreno Salinas Read More 12:00 PM Session IV AGPCRs signaling in the nervous system Joseph Duman · Simeon R. Mihaylov · Anne Bormann Read More 1:00 PM Complimentary Lunch Read More 2:00 PM Posters Caroline Formstone · Jianxiang Xue · Virginea de Araujo Farias · Szymon P. Kordon · Tingzhen Shen · Bill Huang · Júlia Rosell · Sheila Ribalta-Mena · Mariam Melkumyan Read More 3:00 PM Session V Structural mechanisms of AGPCR signaling and function Fabian Pohl · Sumit Bandekar · Florian Seufert Read More 4:00 PM Board meeting/General assembly Welcome to Join Read More 5:00 PM Leave for dinner reception Read More 5:30 PM Complimentary Reception dinner Read More Oct 25 - 9:00 AM Session VI AGPCRs shaping the nervous system Yimin Zou · Dimitris Placantonakis · Nicole Perry-Hauser Read More 10:00 AM Coffee Break with lights snacks Read More 10:30 AM Session VII Physiological and pathological roles of AGPCRs in the nervous system Beatriz Blanco Redondo · Willem Berend Post Read More 11:10 AM Dr. GPCR Community Presentation Monserrat Avila Zozaya Read More 11:30 AM Session VIII Physiological and pathological roles of AGPCRs in the periphery Cheng-Chih Hsiao · Anastasia Georgiadi · Douglas Tilley Read More 12:30 PM Complimentary Lunch Read More 1:30 PM Session VIII * Physiological and pathological roles of AGPCRs in the periphery Tobias Langenhan · Anastasia Georgiadi · Douglas Tilley · Hee-Yong Kim · Alain Garcia De Las Bayonas · Gabriela Aust Read More 2:50 PM Session IX / Technology capsule: Light on aGPCR signaling and function NovoiSMART - A new platform for GPCR antibody drug discovery Gavin Zhang Read More 3:20 PM Coffee Break with pastries announcement of the aGEM award Read More 4:00 PM Closing remarks Read More Jinpeng Sun Identification and Functional Characterization of Adhesion GPCRs As Steroid Hormone Receptors and Hearing and Balance Receptors Bill Huang Self-Cleavage of GPR110 SEA Domain and Its Impact on GAIN Domain Autoproteolysis Andrew Dates Heterogeneity of Tethered Agonist Signaling in Adhesion G Protein-Coupled Receptors Pal Kasturi Site Specific N-Glycosylation Of The N-Terminal Fragment Of ADGRG6 Drives Proteolytic Processing, Trafficking And Signalling Ana Lilia Moreno Salinas Characterizing hADGRE5/CD97 Activation and Signaling: A Mechanical Stimulation BRET-Based Approach (MS-BRET) Florian Seufert Unveiling the GPS Cleavage Mechanism in ADGRL1 with QM/MM Willem Berend Post The Adhesion GPCR Latrophilin Interacts With The Notch Pathway To Control Germ Cell Proliferation Tobias Langenhan The CELSR/ADGRC Homolog Flamingo Is Not Autoproteolytically Processed By The GAIN Domain Rashed Rezwan Parag Novel isoforms of adhesion G protein coupled receptor B1 (ADGRB1/BAI1) generated from an alternative promoter in intron 17 Emmanouil Kyrloglou GPR124 Mediates Adhesion Of Leukemic Stem Cells To Their Niche And Leads To Myeloid Skewing Virginea de Araujo Farias Anti-Tumorigenic Role of Brain Angiogenesis Inhibitor 3 (BAI3) in WNT-Activated Medulloblastomas Szymon P. Kordon Conformational And Functional Coupling Between Extracellular and Transmembrane Regions of a Holo-Adhesion GPCR Frank Kwarcinski 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 Erwin G. Van Meir Adhesion GPCR BAI1/ADGRB1 can block IGF1R-mediated growth signalling, increase radiosensitivity and augment survival in medulloblastoma. Laurent Sabbagh bioSens-All: A Multiparametric BRET-Based Platform for Comprehensive Profiling of adhesion GPCR Signaling and Pharmacology-Enabling Drug Discovery Fabian Pohl Structural Determinants Of GAIN Domain Autoproteolysis And Cleavage Resistance Of Adhesion G Protein-Coupled Receptors Beatriz Blanco Redondo Uncovering the signaling pathway of the ADGRA homolog Remoulade in Drosophila Douglas Tilley ADGRF5-mediated regulation of cardiac health and disease Abhishek Kumar Singh Adgrg6/Gpr126 is Required for Myocardial Notch Activity and N-cadherin Localization to Attain Trabecular Identity Lara-Sophie Brodmerkel GAIN Domain Dynamics And Its Relevance For Adhesion GPCR Signaling In Vivo Caroline Formstone Interrogating The Role Of CELSR1 (ADGRC1) In Breast Cancer Mariam Melkumyan GPR110 modulates anxiety-like behaviors and memory function in mice potentially through neuronal and neuroimmune alterations during neurodevelopment Signe Mathiasen Signaling Properties of ADGRL3 Monserrat Avila Zozaya The ADGRF5/GPR116 receptor is a key regulator of lymphatic endothelial cell identity and function Simeon R. Mihaylov Bai1 Is A Novel Neuronal Substrate Of The Psychiatric Risk Kinase TNIK Sumit Bandekar Structural studies of the CELSR1 extracellular region reveal a compact multidomain module of fourteen domains which regulates signaling Nicole Perry-Hauser Adhesion G protein-coupled receptor latrophilin-3 (ADGRL3) modulation of dopaminergic neurotransmission Anastasia Georgiadi Adhesion GPCR GPR116/Adgrf5 controls a lineage of anti-thermogenic adipocytes with implications for adaptive thermogenesis during prolonged cold exposure Jesse Stillwell Next Generation MBD2 inhibitors for Brain Cancer Therapy Hailey Steichen Identification of Differentially Expressed Gpr116 (Adgrf5) Transcript Variants in Mouse Kidney Sheila Ribalta-Mena Endocytic Cues Determine the Signaling Profile of Adhesion GPCR ADGRL1 / Latrophilin-1 Jianxiang Xue Generation and characterization of collecting duct specific GPR56 knockout mice Demet Araç An ECR-Mediated and TA-independent Mechanism of aGPCR Activation: Direct Communication of Extracellular Region with Transmembrane Domain in a Holo-Adhesion GPCR Yuling Feng Localization of putative ligands for adhesion G protein-coupled receptors in mouse tissues. Joseph Duman BAI1/ADGRB1-mediated Regulation of Mitochondrial Morphology in Axons Yimin Zou ADGRCs in glutamatergic synapse formation, maintenance and degeneration Cheng-Chih Hsiao ADGRG1/GPR56 regulates survival of terminally differentiated CD8+ T cells Alain Garcia De Las Bayonas The Adhesion GPCR Cupidon Regulates Mating In The Closest Relatives Of Animals Alex Torrelli-Diljohn Investigating The Role of ADGRB3 Loss of Expression in Brain Tumor Formation in Li-Fraumeni Syndrome Tyler Bernadyn Elucidating The Role Of GPR97/ADGRG3 In Neutrophil Biology Tingzhen Shen Deorphanization Of The Adhesion GPCRs GPR110 and GPR116 Júlia Rosell Tethered Agonist Dependent ADGRL3 Signaling Activity In The G12/13 Pathway Peng Xiao Tethered Peptide Activation Mechanism of Adhesion GPCRs Stephanie Häfner The NTF Release Sensor Approach for Drug Discovery for Human Adhesion GPCRs Anne Bormann Intricacies Of Complex Assembly And Ligand Interaction In The Adhesion GPCR Latrophilin/Cirl Dimitris Placantonakis Antibody-drug conjugates targeting CD97 in glioblastoma Gabriela Aust Critical role for CD97/ADGRE5 in the induction of allergic airway inflammation Hee-Yong Kim Characterization of Phenotypes Associated with GPR110 Deletion Vasiliki Karagiannakou A single cell GPCR map of thermogenic fat Gavin Zhang NovoiSMART - A new platform for GPCR antibody drug discovery
- Session VIII * | Adhesion GPCR Workshop 2024 | Dr. GPCR Ecosystem
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 >
- Session VI | Adhesion GPCR Workshop 2024 | Dr. GPCR Ecosystem
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 >
- Session III | Adhesion GPCR Workshop 2024 | Dr. GPCR Ecosystem
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 >
- Sponsorship Prospectus for Adhesion GPCR Workshop 2024 | Dr. GPCR Ecosystem
Explore sponsorship opportunities for the Adhesion GPCR Workshop 2024. Connect your organization with leading GPCR researchers and showcase your brand to the scientific community. SPONSORSHIP PROSPECTUS Adhesion GPCR workshop 2024 CINVESTAV, Mexico City, Mexico October 23-25 Sponsor We are delighted to present the sponsorship opportunities available for Adhesion GPCR Workshop 2024, a premier scientific meeting bringing together leaders and innovators in G Protein-Coupled Receptor (GPCR) biology. Adhesion GPCR Workshop 2024 will take place on October 23-25, 2024 at Centro de Investigación y de Estudios Avanzados del Instituto Politécnico Nacional (known as Cinvestav) in Mexico City, offering a dynamic platform for knowledge exchange, collaboration, and networking. About the Adhesion GPCR Workshop 2024: Adhesion GPCR Workshop 2024 is a high-profile expert conference, attracting attendees from across the globe. Our agenda includes keynote presentations, panel discussions, workshops, and networking sessions covering the latest advancements and challenges in Membrane Receptor biology. This event provides an unparalleled opportunity for sponsors to showcase their commitment to scientific excellence and innovation. Audience Profile: Basic Scientists Academics Clinical Scientists Industry Professionals Health Professionals Policy Makers Students Why Sponsor Adhesion GPCR Workshop 2024? Align your brand with scientific excellence and innovation. Showcase your products, services, and research initiatives to a targeted audience. Enhance brand visibility and recognition among key stakeholders in the field. Network with leading professionals and decision-makers in the industry. Support the advancement of knowledge and collaboration within the scientific community. Sponsorship Opportunities Platinum Sponsor Exclusive recognition as the Platinum sponsor in all promotional materials. Prime placement of company logo on event website, signage, and marketing collateral. Opportunity to deliver opening remarks or introduce keynote speakers. Complimentary exhibition booth in a prominent location at the event venue. Recognition in press releases and media coverage. Complimentary registration for 3 representatives. Opportunity to be designated in print on the 1 st ever “aGPCR Excellence and Mentoring Award” Customized sponsorship package available upon request. Gold Sponsor Prominent recognition as a Gold sponsor in all promotional materials. Company logo displayed on event website, signage, and marketing collateral. Opportunity to sponsor a keynote session or panel discussion. Recognition during opening and closing remarks. Complimentary exhibition booth at the event. Complimentary registration for 2 representatives. Customized sponsorship package available upon request. Silver Sponsor Recognition as a Silver sponsor in all promotional materials. Company logo displayed on event website and signage. Opportunity to sponsor a workshop or networking session. Recognition during opening and closing remarks. Complimentary registration for 1 representative. Customized sponsorship package available upon request. Bronze Sponsor Recognition as a Bronze sponsor in all promotional materials. Company logo displayed on event website.Recognition during opening and closing remarks. Additional Sponsorship Opportunities: Networking Reception Sponsorship Conference Cup and T-Shirt Sponsorship Conference Bag Sponsorship Lanyard Sponsorship Coffee Break Sponsorship Customized Opportunities Available 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.
- Complimentary Lunch | Adhesion GPCR Workshop 2024 | Dr. GPCR Ecosystem
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 >
- Session VIII | Adhesion GPCR Workshop 2024 | Dr. GPCR Ecosystem
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 >
- Closing remarks | Adhesion GPCR Workshop 2024 | Dr. GPCR Ecosystem
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 >
- Abstract Submission Adhesion GPCR Workshop 2024 | Dr. GPCR Ecosystem
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.














