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<< Back to podcast list Strategic Partner(s) Dr. Kevin Pfleger About this episode Dr. Pfleger trained as a pharmacologist and obtained his Ph.D. at the University of Edinburgh. I sat down with Kevin to chat about GPCRs, pharmacology, and his contributions to the field in both the academic and biotech worlds. Professor Pfleger has developed extensive expertise in profiling receptor binding and function at the molecular and cellular levels over the last 20 years, particularly involving GPCRs. He also has globally-recognized expertise in bioluminescence resonance energy transfer (BRET) technology, including his patented Receptor-Heteromer Investigation Technology (Receptor-HIT) for studying heteromers. Kevin is also Director, Biomedical Innovation at The University of Western Australia (UWA) and the MTPConnect Western Australian Life Sciences Innovation Hub. He is Head of Molecular Endocrinology and Pharmacology at the UWA Centre for Medical Research and Harry Perkins Institute of Medical Research, Deputy Director of the Australian Research Council Centre for Personalised Therapeutics Technologies, Chief Scientific Advisor to Dimerix, and co-founder of RAGE Biotech . He currently serves on the Board of the Australasian Society of Clinical and Experimental Pharmacologists and Toxicologists and is a member of the British Pharmacological Society International Advisory Group. Join me and learn more about Kevin’s work and how he manages all his responsibilities. Dr. Kevin Pfleger on the web LinkedIn ResearchGate Pubmed Google Scholar University of Western Australia Harry Perkins Institute of Medical Research 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 Asking Better Questions in Science: A Practical Guide for Emerging Researchers When the Islet Lit Up: Advancing GPCR Imaging in Native Tissue How Collaboration Sparked a GPCR Imaging Breakthrough in Chemical Biology Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

Retreat 2023 About Program Registration Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule Illuminating Functional Selectivity and Allosterism at GPCRs. Date & Time Saturday, November 4th / 11:30 AM Abstract Coming Soon About Stéphane Laporte "Dr. Stéphane Laporte is a Professor of Medicine, and the Director of Research of the Division of Endocrinology and Metabolism at McGill University. He is also an Associate Leader of the Experimental Therapeutics and Metabolism Program and the Director of the Molecular Imaging Platform at the Research Institute of the McGill University Health Centre (RI-MUHC). He is a member of the Executive Committee of the Réseau québécois de recherche sur les médicaments. He has received many awards, including a Canada Research Chair, FRSQ scholarships and the CDA/CSEM/Merck Frosst Young Investigator award. His expertise is in molecular pharmacology and his research program focuses on the molecular and cellular mechanisms regulating G protein-coupled receptor (GPCR) responses, a class of receptors involved in many, if not all, physiological responses, with the ultimate goal of improving drug action. He has developed innovative methods for in-cellulo measurement of protein-protein interactions, receptor trafficking and signalling, useful for drug discovery programs. His research program also studies the allosteric, biased signalling regulation of GPCR and has contributed to the validation of small molecules that block myometrial contraction in pre-term birth. He has contributed to the generation of many intellectual property agreements and patents, and published his findings in high-impact journals. The Canadian Institutes for Health Research and March of Dimes currently support his research." Stéphane Laporte on the web Laporte Lab McGill University LinkedIn 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 Strategic Partner(s) Dr. GPCR Team About Dr. Yamina Berchiche Dr. Yamina A. Berchiche is the founder of Dr. GPCR, an ecosystem designed to bring together stakeholders interested in using G-Protein Coupled Receptors (GPCRs) that control virtually everything in the body as drug targets. The mission of Dr. GPCR is to accelerate GPCR drug discovery by sharing the latest research and technology advances in the field and providing exposure to scientists through the Dr. GPCR podcast. Dr. Berchiche obtained her Master’s and Ph.D. in Biochemistry at the University of Montreal in Canada before training at Rockefeller University in New York and the National Institutes of Health in Bethesda, Maryland. She developed expertise over the past two decades studying structure/function relationships of GPCRs using live-cell bioluminescence resonance energy transfer (BRET). Her work focused on chemokine receptors, members of the GPCR family that control cell movement in the body. Dr. Yamina Berchiche on the web Website LinkedIn Facebook Twitter ResearchGate PubMed Google Scholar Dr. GPCR About Dr. Shivani Sachdev Dr. Sachdev is an early career researcher in the National Institute of Diabetes and Digestive and Kidney Diseases at the National Institutes of Health. Her research centers on developing nanobody-ligand conjugates to target GPCRs, with a focus on receptors relevant for treating osteoporosis, diabetes, and pain. She received her undergraduate degree in Biotechnology from KIIT University in India. She subsequently joined Professor Mark Connor's laboratory at Macquarie University in Australia. Dr. Sachdev pursued Ph.D. in the same lab where she investigated the molecular pharmacology of cannabinoid receptors. She is also very active within the pharmacology community and currently serves on the editorial board of the British Journal of Pharmacology. Given her expertise in GPCR pharmacology and scientific communication, she is poised to make valuable contributions to the field and expand our understanding of GPCR signaling. Dr. Shivani Sachdev on the web NIDDK ReseachGate Google Scholar LinkedIn Twitter Dr. GPCR About Dr. Inês Pinheiro PharmD by training and Ph.D. candidate in Hartley's lab at the University of Geneva. As a young researcher fascinated by chemokine receptors, molecular pharmacology, drug discovery, and immuno-oncology. Dr. Inês Pinheiro on the web LinkedIn University of Geneva Twitter Dr. GPCR About Dr. Monserrat Avila Zozaya I did a PhD in cell biology at CINVESTAV, Mexico. During that time, I investigated the effect of lung cancer-related mutations in the GAIN domain of the Latrophilin 3 receptor. My long-term interest is focused on understanding the mechanisms mediated by GPCRs at the cellular communication level. Dr. Monserrat Avila Zozaya on the web LinkedIn Antony Boucard Lab Dr. GPCR About John Azietaku John Teye Azietaku,PhD is a trained pharmacist, holding a Ph.D. in Drug Discovery Biology and Pharmacology from Monash University. Currently serving as a Post Doctoral research fellow at Monash University, John plays a pivotal role in the pharmacological screening of compounds for a commercial drug discovery program. With prior industry experience as a Clinical Research Associate at IQVIA and regulatory officer at the Food and Drug Authority (FDA) in Ghana, John has a proven track record of ensuring compliance with protocols and regulatory standards. Driven by a passion for advancing drug development, John is committed to leveraging his expertise to enhance healthcare outcomes and contribute to the growth of the pharmaceutical and biotech industry. John Azietaku on the web LinkedIn Dr. GPCR About Ya-Tzu Li Ya-Tzu is a Master's student at the University of South Florida, utilizing large-scale virtual drug screening to identify agonists and antagonists targeting Class A GPCRs. Since beginning her undergraduate studies, she has used computational methods like molecular dynamics simulations and free energy landscape analysis to understand the signaling pathways and activation mechanisms of the Dopamine D3 receptor and the CXCR4-CXCL12 complex. In August, Ya-Tzu will continue her academic and research pursuits by beginning her PhD training in Medical Science at USF, aiming to further contribute to the field of medical pharmacology. Ya-Tzu Li on the web LinkedIn Dr. GPCR About Cam Sinh Lu Cam Sinh Lu is a PhD student at Monash Institute of Pharmaceutical Sciences, Monash University, with a deep interest in understanding drug-receptor interactions. With an immense passion for molecular pharmacology, his research focuses on elucidating the molecular basis of membrane protein signalling using quantitative assays and molecular modelling. Further down the track, he aims to apply this knowledge to develop novel chemical treatments for neuronal and cardiovascular diseases. Cam Sinh Lu on the web LinkedIn Dr. GPCR Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Recent Podcast Articles Asking Better Questions in Science: A Practical Guide for Emerging Researchers When the Islet Lit Up: Advancing GPCR Imaging in Native Tissue How Collaboration Sparked a GPCR Imaging Breakthrough in Chemical Biology Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

Retreat 2023 About Program Registration Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule Dinner 2 Date & Time Friday, November 3rd / 7:00 PM 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

Retreat 2023 About Program Registration Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule Coffee Break 3 Date & Time Friday, November 3rd / 10:25 AM 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

Retreat 2023 About Program Registration Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule Developing a PROTAC to Degrade the Constitutively Active Onco-GPCR in Uveal Melanoma Date & Time Friday, November 3rd / 4:20 PM About Victoria Rasmussen "Victoria Rasmussen is a graduate fellow in Dr. Thomas Sakmar’s laboratory at Rockefeller University, where she studies the signaling and degradation of G protein-coupled receptors. She completed her undergraduate education at Providence College, receiving a B.S. in Biology and a B.A. in Psychology. During her time at Providence College, she received the Walsh Grant Fellowship to develop novel methods of synthesizing 2-imidazoline scaffolds to be used as proteasome modulators in the laboratory of Travis Bethel. Victoria started her Ph.D. at the Tri-Institutional Ph.D. program in Chemical Biology, where she joined the lab of Thomas Sakmar at Rockefeller University. She is currently working to understand the signaling and degradation of GPCRs in disease states to help test the feasibility of using protein-targeted degradation as a therapeutic strategy. " Victoria Rasmussen on the web Tri-Institutional PhD Program Chemical Biology LinkedIn 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 Strategic Partner(s) Yao Lu (Jackie) About Yao Lu (Jackie) "Jackie is a Ph.D. student, at Monash University, Australia, investigating the role of functional selectivity in a novel class of potential antipsychotics for the treatment of schizophrenia. Her work involves the pharmacological and structural characterisation of novel putative antipsychotic small molecules. Her research aims to provide a molecular explanation of small molecules for their pre-clinical efficacy and to support the design of novel therapeutics. " Yao Lu (Jackie) on the web Monash University Georgina Sweet Fellowship Authorea Dr. GPCR Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Recent Podcast Articles Asking Better Questions in Science: A Practical Guide for Emerging Researchers When the Islet Lit Up: Advancing GPCR Imaging in Native Tissue How Collaboration Sparked a GPCR Imaging Breakthrough in Chemical Biology Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

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 Strategic Partner(s) Dr. Kathleen Caron About Kathleen M. Caron Kathleen M. Caron, Ph.D. is the Frederik L. Eldridge Distinguished Professor and Chair of the Department of Cell Biology & Physiology at The University of North Carolina at Chapel Hill—a large, interdisciplinary basic science department currently ranked 1st in the Nation in NIH funding. Dr. Caron received a BS in Biology and BA in Philosophy at Emory University and a PhD at Duke University while training with Dr. Keith Parker to elucidate the role of steroidogenesis in regulating sexual determination and adrenal and gonadal development using genetic mouse models. She pursued postdoctoral training with Nobel Laureate Dr. Oliver Smithies at UNC-CH, where she was the first to discover the essential role of adrenomedullin peptide for embryonic survival. With a special emphasis on G protein coupled receptors and receptor activity modifying proteins in vascular biology, the Caron laboratory has gained valuable insights into the genetic basis and pathophysiology of lymphatic vascular disease, preeclampsia and sex-dependent cardiovascular disease. Dr. Caron has received numerous awards including a Burroughs Wellcome Fund Career Award in the Biomedical Sciences, an Established Investigator Award and an Innovator Award from the American Heart Association, a Jefferson Pilot Award in Biomedical Sciences and a UNC-CH Mentoring Award. She currently serves as Associate Editor of Physiological Reviews; the #1 ranked journal in Physiology (IF 46.5). Dr. Caron is also past Associate Editor at JCI and served as the inaugural Associate Editor at ACS-Pharmacology and Translational Science. Dr. Caron currently holds multiple scientific advisory roles in academia, industry and the National Institutes of Health. Kathleen M. Caron on the web Lab Website Twitter Pubmed Google Scholar Orcid Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Recent Podcast Articles Asking Better Questions in Science: A Practical Guide for Emerging Researchers When the Islet Lit Up: Advancing GPCR Imaging in Native Tissue How Collaboration Sparked a GPCR Imaging Breakthrough in Chemical Biology Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

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

Retreat 2023 About Program Registration Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule Breakfast 2 Date & Time Saturday, November 4th / 7:30 AM 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 Departure < Previous Session Next Session >

Retreat 2023 About Program Registration Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule Closing Remarks. Lunch and farewell Date & Time Saturday, November 4th / 12:30 PM 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

Retreat 2023 About Program Registration Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule Biased agonism at the GLP-1 receptor: from structure to animal models of disease Date & Time Friday, November 3rd / 11:05 AM Abstract Coming Soon About Patrick Sexton " Patrick Sexton is a NHMRC Senior Principal Research Fellow and Director, ARC Centre for Cryo-electron Microscopy of Membrane Proteins ( www.ccemmp.org ). He is a leader in the study of GPCRs. Recently, his team has applied cryo-EM to elucidation of the structure and dynamics of GPCRs. Prof. Sexton has published over 335 peer reviewed journal articles and has been cited >29,000 times (Google Scholar). He is a 2022 Clarivate Analytics Highly Cited Researcher in two disciplines: Pharmacology & Toxicology; Biology & Biochemistry, a corresponding member of NC-IUPHAR, a member of the Faculty of 1000 and an elected Fellow of the British Pharmacological Society (BPS). Prof. Sexton’s awards include the ASCEPT Lecturer award, Endocrine Society (Australia) Senior Plenary award, Rand Medal (ASCEPT), Paxinos-Watson Award (Australian Neuroscience Society), Vane Medal (BPS), Gordon Hammes Lectureship Award (American Chemical Society) and the GSK Research Excellence award. Prof. Sexton is also a co-founder of Septerna Inc. " Patrick Sexton on the web CCeMMP Monash University 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 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 >

Retreat 2023 About Program Registration Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule G Proteins and GPCRs in Cancer: Novel Precision Targeted and Immunotherapies Date & Time Friday, November 3rd / 3:30 PM Abstract Coming Soon About J. Silvio Gutkind "Dr. Gutkind is a Distinguished Professor and Chair of the Department of Pharmacology, School of Medicine, and Associate Director for Basic Science at the Moores Cancer Center, University of California San Diego (UCSD). He served as Branch Chief at NIDCR, NIH, since 1998 until his recruitment to UCSD in 2015. His research team has pioneered the study of G proteins and G protein coupled receptors (GPCRs) in human malignancies. He is exploiting the emerging information on dysregulated signaling circuitries and individual genomic and molecular alterations to develop new precision cancer treatments, and to identify novel multimodal strategies to enhance the response to cancer immunotherapies." J. Silvio Gutkind on the web Gutkind Lab – UC San Diego Moores Cancer Center Gutkind Lab publications Pubmed LinkedIn Twitter UCSD Moores Cancer Center 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 Strategic Partner(s) Dr. Paul J. Gasser About Dr. Paul J. Gasser " I received my BS and MS in Zoology & Physiology at the University of Wyoming, where I studied signaling processes involved in light-induced regulation of melatonin synthesis in the rainbow trout pineal organ, a directly photosensitive endocrine organ. I received my PhD in Biology at Arizona State University, where I worked in the lab of Miles Orchinik, studying cellular mechanisms underlying non-genomic actions of corticosteroid hormones. My postdoctoral work, conducted at the University of Bristol, UK, in Christopher Lowry's lab, examined the role of organic cation transporter 3 (OCT3) in the regulation of monoamine signaling in the brain. I joined the faculty of Biomedical Sciences at Marquette in 2007. I teach undergraduate Biochemistry and a variety of graduate neuroscience courses. Research in my lab is currently focused on understanding the signal transduction pathways activated by beta-adrenergic receptors localized to the inner nuclear membrane and their role in the regulation of gene expression." Dr. Paul J. Gasser on the web Gasser Lab Marquette University Google Scholar ResearchGate LinkedIn Twitter Dr. GPCR Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Recent Podcast Articles Asking Better Questions in Science: A Practical Guide for Emerging Researchers When the Islet Lit Up: Advancing GPCR Imaging in Native Tissue How Collaboration Sparked a GPCR Imaging Breakthrough in Chemical Biology Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

Retreat 2023 About Program Registration Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule Coffee Break 1 Date & Time Thursday, November 2nd / 2:45 PM 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 Strategic Partner(s) Dr. Hannes Schihada About Dr. Hannes Schihada Following studies in Pharmacy in Regensburg, Germany, I joined the receptor pharmacology group of Martin Lohse at the Institute of Pharmacology & Toxicology in Würzburg, Germany, in 2015. My project involved the development of FRET/BRET -based GPCR conformational biosensors, which can be employed in high throughput ligand screening. After my Ph.D. defense in 2019, I moved with a DFG (German research council) PostDoc fellowship to Stockholm, Sweden, in order to focus my research on class Frizzled GPCR s in the lab of Gunnar Schulte at the Karolinska Institute. I spent 2 1/2 years in his lab and developed novel conformational sensors for these intriguing receptors, allowing us to better understand their mode of action. By the end of 2021, I moved back to Germany and joined the pharmaceutical chemistry group of Peter Kolb in Marburg. I was recently awarded a Marie Sklodowska Curie PostDoc Fellowship in order to investigate and find better ligands for the orphan class A GPCRs , GPR3 , GPR6 , and GPR12 . Dr. Hannes Schihada on the web Karolinska Institutet Twitter Adher´n Rise LinkedIn 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 Asking Better Questions in Science: A Practical Guide for Emerging Researchers When the Islet Lit Up: Advancing GPCR Imaging in Native Tissue How Collaboration Sparked a GPCR Imaging Breakthrough in Chemical Biology Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

Retreat 2023 About Program Registration Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule A positive Allosteric Modulator of M1 Acetylcholine Receptors Improves Cognitive Deficits in Male and Female Alzheimer’s Mice Date & Time Friday, November 3rd / 1:55 PM About Khaled Abdelrahman Dr. Khaled Abdelrahman graduated in 2006 with a BSc in Pharmaceutical Sciences from Alexandria University (Egypt) followed by MSc in Pharmacology in the same university that was conferred in 2009. He joined the laboratory of Dr. William Cole at the University of Calgary in 2010 for his Ph.D. where he studied the molecular basis underlying altered cerebrovascular function and blood flow in type 2 diabetes. In 2015, He joined Dr. Stephen Ferguson’s laboratory in the Departments of Cellular & Molecular Medicine and Neuroscience at the University of Ottawa as a Postdoctoral Fellow to explore novel G protein-coupled receptor (GPCR) candidates that can be targeted pharmacologically to slow neurodegeneration. He has been also studying what aspects of GPCR signaling are regulated in a sex-selective manner and how this can influence drug discovery in the area of neurodegenerative diseases. He is also a Registered Pharmacist in Canada and held two of the most prestigious Clinician Postdoctoral Fellowships offered by Alberta Innovates and Canadian Institutes of Health Research. He received the Canadian Society of Pharmacology and Therapeutics Postdoctoral and Publication awards along with many Young Scientist Awards from the American Society for Pharmacology and Experimental Therapeutics. Khaled Abdelrahman on the web University of British Columbia Twitter PubMed 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

<< Back to podcast list Strategic Partner(s) Dr. Samuel Hoare About Dr. Samuel Hoare Sam completed his Ph.D. in biochemistry, studying allosteric modulation of dopamine receptors, from the University of Kent, United Kingdom. He then moved to the National Institute of Mental Health, researching pharmacological mechanisms of Class B GPCRs as part of his postdoctoral training. Today, Sam is a pharmacology data analyst and the founder of Pharmechanics LLC , a consultancy and data analysis company supporting pharmaceutical, life science, and academic scientists in the development of new therapeutics and the understanding of receptor systems. As an industry pharmacologist, he consults with numerous pharma and biotechs in understanding and applying in vitro pharmacology data to advance drug discovery. He specializes in kinetic analysis of drug action and is known for applying binding kinetics to the development of effective therapeutics, particularly GPCR antagonists. Before founding Pharmechanics in 2016, Dr. Hoare was a pharmacology leader in the pharmaceutical industry for 15 years at Neurocrine Biosciences . He guided the in vitro biology efforts of the company for numerous drug discovery campaigns. Sam is known for demystifying complicated and newly-emerging pharmacology concepts, enabling them to be applied by project teams in optimizing new molecules. I very much enjoyed chatting with Sam about his love for GPCRs, kinetics, and decorticate the complexities of GPCR function to better target receptors. Dr. Samuel Hoare on the web Pharmechanics LLC LinkedIn Pubmed Google Scholar YouTube Dr. GPCR Member ResearchGate 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 Asking Better Questions in Science: A Practical Guide for Emerging Researchers When the Islet Lit Up: Advancing GPCR Imaging in Native Tissue How Collaboration Sparked a GPCR Imaging Breakthrough in Chemical Biology Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Strategic Partner(s) Dr. Bruno Giros About Dr. Bruno Giros Dr. Giros' lab investigates how molecular changes at the nerve synapse might impact integrated behavior and what we might learn from these mechanisms to cure mental illness. After doctoral training at the Pierre and Marie Curie University in Paris and a short internship at Genentech Inc. in South San Francisco, he joined the CNRS as a Research Fellow in 1987 in the INSERM Laboratory directed by Jean-Charles Schwartz in Paris, where he cloned and characterized dopamine D2 and D3 receptor subtypes. From 91 to 94, he was an assistant professor at Duke University in North Carolina, working with Marc Caron and Robert Lefkowitz (2012 Nobel Prize in Chemistry) to characterize several neurotransmitter transporters and kinases and establish the first knock-out for these genes. In 1999, in France, Dr. Giros created the INSERM/CNRS laboratory on the "Neurobiology of Psychiatric Disorders," first in Créteil with Marion Leboyer, then at the University of Paris-Sorbonne with Hervé Chneiweiss. Since 2008, he has arrived at McGill University as a Canada Research Chair. At McGill, his laboratory has two main axes of research: 1) Studying interindividual vulnerability to chronic stress and depression and; 2) Understanding the role of phenotypically defined subpopulations of striatal neurons in motor and cognitive functions. Bruno Giros has trained 59 master's, doctoral and postdoc students, most of his trainees obtain positions in the academic or private sectors or are currently pursuing postdoctoral research training or have entered medical studies. Dr. Giros has published more than 200 publications with an H factor of 79 and 32,000 citations (Google Scholar) and has received several distinctions, including the CNRS silver medal, the FRM "Young Researcher" prize, the ISI “Highly Cited” and F-1000 in Pharmacology, and recently received the Heinz Lehmann Award from the Canadian College of NeuroPsychopharmacology and the distinguished James B. McGill Professor Award. Dr. Bruno Giros on the web Dougles Research Center LinkedIn Google Scholar Researchgate Dr. GPCR Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Recent Podcast Articles Asking Better Questions in Science: A Practical Guide for Emerging Researchers When the Islet Lit Up: Advancing GPCR Imaging in Native Tissue How Collaboration Sparked a GPCR Imaging Breakthrough in Chemical Biology Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

Retreat 2023 About Program Registration Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule Cannabinoid compounds to augment L-DOPA treatment in Parkinson's Disease Date & Time Friday, November 3rd / 9:20 AM Abstract Coming Soon About Ali Salahpour "Dr. Salahpour did his undergrad (1993-1996) and PhD (1996-2002) at University of Montreal in the Department of Biochemistry. His PhD work was under the supervision of Dr. Michel Bouvier working on the topic of GPCR dimerization/oligomerization. In November of 2002, he joined the lab of Dr. Marc Caron at Duke University for his post-doctoral training. In the Caron lab, Dr. Salahpour worked on Dopamine Transporter and its role on regulating dopamine transmission and homeostasis. In April 2009, he joined the Department of Pharmacology and Toxicology at University of Toronto and has continued working on dopamine transmission and homeostasis and the role of several of key modulators of the dopamine system, including the dopamine transporter (DAT), the Vesicular Monoamine Transporter 2 (VMAT2), Tyrosine Hydroxylase (TH) and Trace Amine Associate Receptor 1 (TAAR1)." Ali Salahpour on the web University of Toronto Pubmed Google Scholar Twitter 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

Retreat 2023 About Program Registration Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule Lunch 1 Date & Time Friday, November 3rd / 12:10 PM 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

Retreat 2023 About Program Registration Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule Registration Date & Time Thursday, November 2nd / 11:00 AM - 1:30 PM 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

Retreat 2023 About Program Registration Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule Biochemical Mechanisms Underlying Location Bias in GPCR Signaling Date & Time Saturday, November 4th / 8:40 AM Abstract Coming Soon About Sudarshan Rajagopal "Dr. Sudarshan Rajagopal is a physician-scientist and is currently an Associate Professor of Medicine and Biochemistry at Duke University School of Medicine. He obtained his B.S. in Chemistry from The University of Chicago in 1998 and subsequently enrolled in the Medical Scientist Training Program at The University of Chicago. During his doctoral work in the lab of Prof. Keith Moffat, he studied the structural mechanisms of bacterial photoreceptors using time-resolved Laue crystallography. He was awarded his PhD in 2004 and his MD in 2006. He then joined the Internal Medicine Residency training program at Duke University Medical Center. During his Cardiology fellowship, he trained in the lab of Dr. Robert J. Lefkowitz, where his research focused on biased agonism, with the development of approaches to quantify ligand bias and the identification of ACKR3 as an endogenously beta-arrestin-biased receptor. After completing his training, he joined the faculty at Duke, with a focus on the mechanisms underlying biased agonism at GPCRs and its contribution inflammation and cardiovascular disease. His group and others have shown that many of these ligands act as biased agonists for the same receptor. His lab is also interested in identifying novel signal transduction mechanisms of GPCRs, such as the formation of complexes between G proteins and beta-arrestins. His clinical focus is on pulmonary arterial hypertension, a disease of the pulmonary arterioles that causes right heart failure, and he serves as co-director of the Duke Pulmonary Vascular Disease Center." Sudarshan Rajagopal on the web The Rajagopal Lab Google Scholar Pubmed LinkedIn 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

Join the Adhesion GPCR Workshop 2024 in Mexico City at CINVESTAV, bringing together researchers to explore the latest in GPCR science. Home Registration Full Agenda Venue Travel Tips Sponsors Special Issue on Adhesion GPCRs Publish Your Work Welcome to the Adhesion GPCR Workshop 2024 , hosted in the vibrant heart of Mexico City at the prestigious venue, CINVESTAV - Centro de Investigación y de Estudios Avanzados del IPN (in English: Center for Research and Advanced Studies of the National Polytechnic Institute). About the venue Cinvestav: Centro de investigación y de Estudios Avanzados del IPN Av. Instituto Politécnico Nacional no 2508 Mexico City, C.P. 07360 Room: Auditorium Arturo Rosenblueth *Have an ID card ready (Passport, Driver's license, etc), as this will be required at the venue entrance Register now to join the exclusive Adhesion GPCR Workshop group and stay updated with all the latest event news. Join the AGPCR24 group Preliminary Program Layout Date Time Title 10/23/2024 09:00 AM Registration & Welcoming Remarks 10/23/2024 10:00 AM Flash Presentations 10/23/2024 11:30 AM Coffee Break 10/23/2024 12:00 PM Session I 10/23/2024 01:00 PM Plenary Lecture 10/23/2024 2:00 PM Lunch 10/23/2024 3:00 PM Session II 10/23/2024 7:00 PM Mexico City Nocturnal Tour 10/24/2024 09:00 AM Session III 10/24/2024 10:30 AM Coffee Break 10/24/2024 11:00 AM Session IV 10/24/2024 12:00 PM Plenary Lecture II 10/24/2024 1:00 PM Posters 10/24/2024 2:00 PM Lunch 10/24/2024 3:00 PM Session V 10/24/2024 4:30 PM Board Meeting 10/24/2024 5:00 PM Career Development 10/24/2024 6:00 PM Networking / Dinner / Reception 10/25/2024 09:00 AM Session VI 10/25/2024 10:30 AM Coffee Break 10/25/2024 11:00 AM Session VII 10/25/2024 12:00 PM Plenary Lecture III 10/25/2024 1:00 PM Session VIII 10/25/2024 2:00 PM Lunch 10/25/2024 3:00 PM Session IX 10/25/2024 4:30 PM Closing Remarks October 23, 2024 October 24, 2024 October 25, 2024 *Flash Presentations: 10 min *Talks 20 min (15 min+ 5 min questions Check AGPCR Program Page Everything you need to know about the event Listen to Dr. Antony Boucard and Dr. Yamina Berchiche at the Dr.GPCR Newsletter Learn more about the Adhesion GPCR workshop 2024 Up Abstract Submission Submit your research abstracts following our guidelines to present at the conference. Up About the venue Discover Cinvestav, the host venue for the upcoming workshop. Up Traveling Tips Find essential tips about Mexico City, including transportation options and local insights. Up Logo Contest Enter our logo contest for a chance to have your design represent the upcoming event.

Full Agenda Adhesion GPCR workshop 2024 CINVESTAV, Mexico City, Mexico October 23-25 Download PDF Program HERE < Back to Full Agenda Board meeting/General assembly Welcome to Join Coming Soon < 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 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 >