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Greetings, Pioneers of GPCR Science! Embark on this week’s thrilling updates in GPCR research, learning opportunities, and industry developments. Don’t just stay informed—immerse yourself, expand your knowledge, and become a trailblazer in the field! This Week’s Highlights: Celebrating Excellence: Wessel A. C. Burger , Arthur Christopoulos , David M. Thal , et al., for their groundbreaking work on Positive allosteric modulation of a GPCR ternary complex Unlock Your Learning: Limited Spots Available! There are only 5 spots left for our upcoming courses, so seize the chance to learn from the best in the field. 🚨 Hurry to reserve your spot for the Principles of Pharmacology I & II BUNDLE before the Early Bird Deadline on September 27 . With just one week left, becoming a premium member is all it takes to benefit from this discount! Not a premium member yet?  No worries – you can sign up for a 5-day FREE trial! Gain access to over 500 minutes of recorded classes in our  GPCR courses   taught by Drs. Terry Kenakin  and Sam Hoare ! Every Thursday at 10 AM EST: Principles of Pharmacology I Dates: October 3, 10, 17, 24 (four sessions) Topics: Pharmacologic activity measurement, mechanisms of action, and GPCR discovery strategies. Registration deadline: September 27, 2024 Principles of Pharmacology II Dates: October 31, November 7, 14, 21, December 5 (five sessions) (we skipped Thanksgiving, of course!) Topics: New cellular assays, real-time kinetics, and unique GPCR behaviors. Registration deadline: October 25, 2024 🔥 Why You Should Enroll Now: Cost-effective & Distinctive Educational Experience Affordable courses that maintain high-quality standards. Adaptable Learning Access recorded sessions at your convenience to enhance your understanding. Our Students Highly Recommend Us! Previous students praise the course content and our exceptional service. Join us for an exciting discussion with Dr. Terry Kenakin to gain insights and prepare for upcoming courses. Don't miss this valuable opportunity! Exclusive Deal for Scientists Residing and Working in Developing Nations If you live and work  in a developing country, please complete this form to enjoy complimentary access to Dr. Kenakin's upcoming courses. Our goal is to ensure that education is within reach for everyone! Secure your spot today and dive into the evolving world of GPCRs! GPCR Event Spotlight Discovery on Target’s 19th Annual GPCR-Based Drug Discovery Targeting G Protein-Coupled Receptors for New Therapeutic Options 📍  Boston, MA 📅 October 2 -3, 2024 Join leading scientists to investigate the most recent advancements in GPCR-targeted drug development, incorporating machine learning, innovative biophysical methods, and medicinal chemistry. Register today for the GPCR Drug Discovery Conference and save $200 with discount code “ DRGPCR24 ”. 11th Adhesion GPCR Workshop    📍  Mexico City 📅 October 23-25, 2024 Engage with your peers and delve into the latest developments in adhesion GPCR biology. The full agenda is now available; check it here ! If you want to enhance your brand, email Hello@DrGPCR.com  for sponsorship opportunities. Classified GPCR News  Let’s dive into the   Classified GPCR News from September 9th to 15th, 2024 Industry News MBX aims for $136M IPO to take potential rival to Ascendis' Yorvipath into phase 3 Certa Therapeutics Announces International Non-Proprietary Name for its First-in-class GPR68 Inhibitor Asengeprast (FT011) AlphaProteo generates novel proteins for biology and health research Innovate UK announced the winners of its Transforming Cancer Therapeutics grant, which focuses on developing life-changing cancer treatments. 𝗦𝘂𝗺𝗺𝗮𝗿𝘆 𝗼𝗳 𝘁𝗵𝗲 𝗿𝗲𝘀𝘂𝗹𝘁𝘀 𝗼𝗳 𝗔𝗘𝗙𝟬𝟭𝟭𝟳 𝗣𝗵𝗮𝘀𝗲 𝟮𝗯 𝗶𝗻 𝗖𝗨𝗗 Nxera Pharma’s Partner Centessa Announces Positive Interim Phase 1 Clinical Data with its Novel Orexin Receptor 2 (OX2R) Agonist, ORX750, in Acutely Sleep-Deprived Healthy Volunteers Cumulus raising $50M, spinning GPR68 small molecules into GIO New treatments being developed for schizophrenia Crinetics Pharmaceuticals Announces September 2024 Inducement Grants Under Nasdaq Listing Rule 5635(c)(4) Call for GPCR Papers Deadline: Nov 1, 2024. Emerging Voices in GPCR Biology in Special Issue of Molecular Pharmacology GPCR Events, Meetings, and Webinars September 5 - 6, 2024 | 4th Transatlantic ECI GPCR Symposium September 18, 2024 | FREE Webinar - The value of GPCR cell-based assays in drug discovery September 22, 2024 | Biomolecular Horizons 2024 September 30 - October 3, 2024 | 22nd Discovery on Target October 2024 | Biologics US 2024   October 2 - 4, 2024 | 9th GPCRs in Medicinal Chemistry October 17, 2024 | Unprecedented fragment-based screening using Spectral Shift for GPCRs October 23 - 25, 2024 | 11th Adhesion GPCR Workshop November 5 - 7, 2024 | 16th Annual PEGS Europe   NEW November 25 - 27, 2024 | 1st Virtual GPCR Forum Conference November 26 - 28, 2024 | GPCRs-Targeted Drug Discovery Summit Europe July 12 - 17, 2026 | 20th World Congress of Basic and Clinical Pharmacology GPCR Jobs HIGHLIGHT Research Associate - Professor Graeme Milligan HIGHLIGHT Postdoc in Molecular Pharmacology - The Hauser Group NEW Postdoctoral Scholar – iPSC in cardiac and endothelial cell function NEW Protein Biochemist/Structural Biologist Senior Scientist/Staff Scientist, Computational Chemistry Postdoc in GPCR mechanosensing   Postdoctoral Position Postdoctoral research position Adhesion GPCRs Loss of cardiomyocyte-specific Adhesion G Protein Coupled Receptor G1 (ADGRG1/GPR56) promotes pressure overload-induced heart failure GPCR Activation and Signaling Positive allosteric modulation of a GPCR ternary complex GPCR Binders, Drugs, and more Progress on the development of Class A GPCR-biased ligands GPCRs in Cardiology, Endocrinology, and Taste CRTC1 in Mc4r-expressing cells is required for peripheral metabolism and systemic energy homeostasis Eiken syndrome with parathyroid hormone resistance due to a novel parathyroid hormone receptor type 1 mutation: clinical features and functional analysis GPCRs in Neuroscience Gain control of sensory input across polysynaptic circuitries in mouse visual cortex by a single G protein-coupled receptor type (5-HT2A) GPCRs in Oncology and Immunology The power of many: Multilevel targeting of representative chemokine and metabolite GPCRs in personalized cancer therapy GPR97 depletion aggravates imiquimod-induced psoriasis pathogenesis via amplifying IL-23/IL-17 axis signal pathway Structural and Molecular Insights into GPCR Function Exploring the constitutive activation mechanism of the class A orphan GPR20 Become a Premium Member! 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Hello GPCR Enthusiasts, Dive into this week's exciting updates on cutting-edge GPCR research, new learning opportunities, and industry news! Don't miss out—explore, learn, and elevate your expertise today! Weekly Highlights: Congrats to: Daniel Matúš , Simone Prömel , et al., for their work on The N terminus-only (trans) function of the Adhesion GPCR Latrophilin-1 controls multiple processes in reproduction of C. elegans Alexei Sirbu , Paolo Annibale , et al., for their study on Cell swelling enhances ligand-driven β-adrenergic signaling ✨ Reserve Your seat before these fill up! Our updated course schedule is designed to fit seamlessly into your routine, offering an enriched learning experience. Every Thursday at 10 AM EST: Principles of Pharmacology I October 3, 10, 17, 24 (four sessions) Topics: Pharmacologic activity measurement, mechanisms of action, and GPCR discovery strategies. Principles of Pharmacology II October 31, November 7, 14, 21, December 5 (five sessions) (we skipped Thanksgiving, of course!) Topics: New cellular assays, real-time kinetics, and unique GPCR behaviors. 🔥 Why You Should Enroll Now: Act Fast & Save Big! The Principles of Pharmacology I & II BUNDLE is your key to mastering the field. You can embrace a  25% OFF early bird discount as a premium member . But act fast – this offer is only available for a limited time. Not a premium member yet? No problem – we offer a 5-day FREE trial! And access over 500 minutes of recorded classes in our  GPCR courses with Drs. Terry Kenakin and Sam Hoare ! Affordable & Unique Learning Experience Our budget-friendly courses offer a unique approach to mastering pharmacology. Flexible Learning Rewatch sessions anytime to reinforce your learning. Our Students Love Us! Past students rave about the content and service of our courses. Join us for an exciting discussion with Dr. Terry Kenakin as he shares insights into what you can anticipate for the upcoming courses. Don't miss this fantastic opportunity to gain valuable knowledge and prepare for the forthcoming sessions! Exclusive Deal for Scientists Residing and Working in Developing Nations If you live and work  in a developing country, please complete this form to enjoy complimentary access to Dr. Kenakin's upcoming courses. Our goal is to ensure that education is within reach for everyone! Secure your spot today and dive into the evolving world of GPCRs! GPCR Event Spotlight Discovery on Target’s 19th Annual GPCR-Based Drug Discovery Targeting G Protein-Coupled Receptors for New Therapeutic Options 📍  Boston, MA 📅 October 2 -3, 2024 Join top researchers to explore the latest in GPCR-targeted drug design, including machine learning, new biophysical techniques, and medicinal chemistry. Register today for the GPCR Drug Discovery Conference and save $200 with discount code “ DRGPCR24 ”. 11th Adhesion GPCR Workshop    📍  Mexico City 📅 October 23-25, 2024 Connect with your colleagues and immerse yourself in the most recent advancements in adhesion GPCR biology. Stay tuned for the release of the full agenda! Are you interested in boosting your brand? Contact us at Hello@DrGPCR.com  for sponsorship opportunities. Classified GPCR News  Let’s dive into the   Classified GPCR News from September 2nd to 8th, 2024 Industry News Superluminal Medicines Closes $120 Million Series A Round Domain Therapeutics has been nominated for Prix Galien USA Carterra unveils its most sensitive biosensor platform; Carterra Ultra™ ushers in a new frontier in fragment and small molecule drug discovery Is the pharma community looking hard enough before trying to engage highly challenging neurology targets? Engaging multiple sclerosis by drugging a “simple” GPCR. This technique for studying cell receptors could have sweeping implications for drug development DeepCure team is excited to welcome Justin Potnick, to our Medicinal Chemistry group Call for GPCR Papers Emerging Voices in GPCR Biology in Special Issue of Molecular Pharmacology GPCR Events, Meetings, and Webinars September 5 - 6, 2024 | 4th Transatlantic ECI GPCR Symposium September 18, 2024 | FREE Webinar - The value of GPCR cell-based assays in drug discovery NEW September 22, 2024 | Biomolecular Horizons 2024 September 30 - October 3, 2024 | 22nd Discovery on Target October 2024 | Biologics US 2024   October 2 - 4, 2024 | 9th GPCRs in Medicinal Chemistry October 17, 2024 | Unprecedented fragment-based screening using Spectral Shift for GPCRs October 23 - 25, 2024 | 11th Adhesion GPCR Workshop November 5 - 7, 2024 | 16th Annual PEGS Europe   NEW November 26 - 28, 2024 | GPCRs-Targeted Drug Discovery Summit Europe July 12 - 17, 2026 | 20th World Congress of Basic and Clinical Pharmacology GPCR Jobs HIGHLIGHT Research Associate - Professor Graeme Milligan HIGHLIGHT Postdoc in Molecular Pharmacology - The Hauser Group Senior Scientist/Staff Scientist, Computational Chemistry Postdoc in GPCR mechanosensing   Postdoctoral Position Postdoctoral research position Adhesion GPCRs The N terminus-only (trans) function of the Adhesion GPCR Latrophilin-1 controls multiple processes in reproduction of C. elegans The G protein-coupled receptor ADGRG6 maintains mouse growth plate homeostasis through IHH Signaling GPCR Activation and Signaling Illuminating GPCR trafficking Cell swelling enhances ligand-driven β-adrenergic signaling Roles of the gate loop in β-arrestin-1 conformational dynamics and phosphorylated receptor interaction Early Events in β2AR Dimer Dynamics Mediated by Activation-Related Microswitches Nuclear translocation of the membrane oxoeicosanoid/androgen receptor, OXER1: Possible mechanisms involved An engineered trafficking biosensor reveals a role for DNAJC13 in DOR downregulation GPCRs in Cardiology, Endocrinology, and Taste Role of G protein coupled receptors in acute kidney injury Ligand-Dependent and G Protein-Dependent Properties for the Sweet Taste Heterodimer, TAS1R2/1R3 GPCRs in Neuroscience GPCR-Mediated Natural Products and Compounds: Potential Therapeutic Targets for the Treatment of Neurological Disease s Activation of GPR55 alleviates neuropathic pain and chronic inflammation Developmental exposures to common environmental pollutants result in long-term Reprogramming of hypothalamic-pituitary axis in mice GPCRs in Oncology and Immunology A disturbed metabolite-GPCR axis is associated with microbial dysbiosis in IBD patients: Potential role of GPR109A in macrophages Structural and Molecular Insights into GPCR Function Insights into the structure and activation mechanism of some class B1 GPCR family members Structural basis of Frizzled 4 in recognition of Dishevelled 2 unveils mechanism of WNT signaling activation Become a Premium Member! 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Significant advancements in the cellular biology of G protein-coupled receptors (GPCRs) about a novel biosensor shed light on the endosomal proteome associated with the δ-opioid receptor (DOR). This study, published in Nature Chemical Biology, highlights the role of the chaperone protein DNAJC13 in the endosomal-lysosomal pathway for DOR. The research team, led by Brandon Novy and colleagues, utilized an innovative APEX2/AUR biosensor that allows scientists to monitor the agonist-induced trafficking of DOR to the lysosome with high precision. By employing this biosensor, the research team identified 492 genes that significantly influence DOR function, with DNAJC13 emerging as a standout candidate along with WDR91 and SNX24. The findings suggest that DNAJC13 is crucial to the trafficking of DOR, facilitating its downregulation and influencing cellular signaling pathways essential for pain and anxiety regulation. How does this new biosensor work? The critical player is Apurinic/Apyrimidinic Endodeoxyribonuclease 2 (APEX2). APEX2 is a peroxidase enzyme that catalyzes the oxidation of specific substrates in the presence of hydrogen peroxide (H 2 O 2 ). Therefore, it’s a great molecular tool for proximity labeling approaches in living cells.  In this study, the DOR receptor was genetically fused to APEX2, creating a DOR-APEX2 construct. Upon agonist activation, the DOR-APEX2 complex is internalized and trafficked to the lysosome. During this process, APEX2 can label proteins in the vicinity, allowing the capture of a snapshot of the endosomal proteome associated with the DOR receptor. APEX2 biosensor utilizes a fluorogenic substrate called Amplex UltraRed (AUR). When AUR is oxidized by APEX2 in the presence of H 2 O 2 , it produces a fluorescent product that can be detected and quantified. This fluorescence serves as a readout for the activity of APEX2 and, by extension, the trafficking of the GPCR of interest. After the labeling reaction, the researchers purified and biotinylated proteins (those that have been labeled by APEX2) and analyzed them using quantitative proteomics such as tandem mass tags. Finally, this analysis provided insights into the molecular composition of the endosomal environment and the proteins involved in the trafficking of the DORs. The development of molecular tools to study GPCR trafficking in real-time opens new avenues for understanding drug tolerance and resistance, particularly in the context of opioid therapies. As the opioid crisis continues to challenge public health, insights gained from this research could inform the development of safer analgesics that minimize the risk of addiction while maintaining their efficacy. The implications of this research extend beyond basic science ; understanding the role of DNAJC13 in GPCR trafficking could profoundly affect the development of therapeutic strategies for conditions related to other GPCR-mediated pathways. As the field continues to evolve, this study represents a crucial step toward unraveling the understanding of GPCR regulation and its potential to revolutionize human health. For further details, refer to the full article: DOI: 10.1038/s41589-024-01705-2

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

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

Full Agenda Adhesion GPCR workshop 2024 CINVESTAV, Mexico City, Mexico October 23-25 Download PDF Program HERE < Back to Full Agenda Session VIII Physiological and pathological roles of AGPCRs in the periphery The CELSR/ADGRC Homolog Flamingo Is Not Autoproteolytically Processed By The GAIN Domain Tobias Langenhan 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 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 "Yin Kwan Chung, Leipzig University Falko Nagel, 7TM Antibodies GmbH Stefan Schulz, Friedrich-Schiller-University Jena and 7TM Antibodies GmbH" 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 X (Twitter) LinkedIn 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 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 >