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  • Ep 68 with Dr. Matthew Eddy

    Dr. GPCR Podcast << Back to podcast list Dr. Matthew Eddy About Dr. Matthew Eddy Matthew Eddy earned his BA in Chemistry from Oberlin College, where he trained with solid-state NMR expert Professor Manish Mehta . He then earned his Ph.D. in physical chemistry from the Massachusetts Institute of Technology, training under the mentorship of Prof. Robert Griffin . Following this, Dr. Eddy began learning and investigating human GPCRs while training in the laboratories of Professors Raymond Stevens and Kurt Wüthrich at The Scripps Research Institute. Dr. Matthew Eddy on the web Website Dr. GPCR Ecosystem Thanks for listening to this podcast episode This short survey will help us understand your needs to bring you exciting and informative content; this short survey should take 5 minutes to fill. Listen and subscribe to where you get your podcasts. << Previous Podcast Episode Next Podcast Episode >>

  • GPR176 promotes fibroblast-to-myofibroblast transition in organ fibrosis progression

    < GPCR News < GPCRs in Oncology and Immunology GPR176 promotes fibroblast-to-myofibroblast transition in organ fibrosis progression Published date July 22, 2024 Abstract "Fibrosis is characterized by excessive deposition of extracellular matrix proteins, particularly collagen, caused by myofibroblasts in response to chronic inflammation. Although G protein-coupled receptors (GPCRs) are among the targets of current antifibrotic drugs, no drug has yet been approved to stop fibrosis progression. Herein, we aimed to identify GPCRs with profibrotic effects. In gene expression analysis of mouse lungs with induced fibrosis, eight GPCRs were identified, showing a >2-fold increase in mRNA expression after fibrosis induction. Among them, we focused on Gpr176 owing to its significant correlation with a myofibroblast marker α-smooth muscle actin (αSMA), the profibrotic factor transforming growth factor β1 (TGFβ1), and collagen in a human lung gene expression database. Similar to the lung fibrosis model, increased Gpr176 expression was also observed in other organs affected by fibrosis, including the kidney, liver, and heart, suggesting its role in fibrosis across various organs. Furthermore, fibroblasts abundantly expressed Gpr176 compared to alveolar epithelial cells, endothelial cells, and macrophages in the fibrotic lung. GPR176 expression was unaffected by TGFβ1 stimulation in rat renal fibroblast NRK-49 cells, whereas knockdown of Gpr176 by siRNA reduced TGFβ1-induced expression of αSMA, fibronectin, and collagen as well as Smad2 phosphorylation. This suggested that Gpr176 regulates fibroblast activation. Consequently, Gpr176 acts in a profibrotic manner, and inhibiting its activity could potentially prevent myofibroblast differentiation and improve fibrosis. Developing a GPR176 inverse agonist or allosteric modulator is a promising therapeutic approach for fibrosis." Authors Yasuo Okamoto, Keisuke Kitakaze, Yasuhiro Takenouchi, Rena Matsui, Daisuke Koga, Ryo Miyashima, Hironobu Ishimaru, Kazuhito Tsuboi Tags Fibroblast , Fibrosis , Gpr176 , Myofibroblast , Orphan GPCR , TGFβ1 Source Contribute to the GPCR News Coming soon Become a Contributor Classified GPCR News Call for GPCR papers GPCR Industry News Adhesion GPCRs GPCR Events, Meetings, and Webinars Reviews, GPCRs, and more GPCR Binders, Drugs, and more Methods & Updates in GPCR Research GPCRs in Neuroscience GPCRs in Cardiology, Endocrinology, and Taste GPCRs in Oncology and Immunology Structural and molecular insights into GPCR function GPCR Activation and Signaling More from Dr. GPCR Create an account and get our contributors articles in your inbox Subscribe to the Dr. GPCR Monthly Newsletter today! Follow the Dr. GPCR News and get weekly notifications about the GPCR field Share < Previous Next >

  • Ep 70 with Dr. Stephen Ferguson

    Dr. GPCR Podcast << Back to podcast list Dr. Stephen Ferguson About Dr. Stephen Ferguson Dr. Stephen Ferguson is a Professor in the Department of Cellular and Molecular Medicine at the University of Ottawa. He did B.Sc. in biology at McGill University and received his Ph.D. under the mentorship of Dr. Brian Collier in the Department of Pharmacology and Therapeutics at McGill University (1994). He did his postdoctoral training with Dr. Marc G. Caron at Duke University (1994-1997), where he and his colleagues investigated the role of G protein-coupled receptor kinases and beta-arrestin in regulating G protein-coupled receptor endocytosis, trafficking, and signaling. He has held four Canada Research Chairs since 2001 and was previously a Heart and Stroke Foundation of Canada MacDonald Scholar (1998-2003) and Heart and Stroke Foundation of Ontario Career Investigator (2003-2016). He was a recipient of Canada's Top 40 under 40 award in 2004 and received Queen Elizabeth II, Diamond Jubilee Medal, in 2012. He has also received both Junior (2001) and Senior (2005) investigator awards from the Pharmacological Society of Canada. Most recently, in 2021, he was elected as a Fellow of the Canadian Academy of Health Science (FCAHS). His research career has focused on the investigation of the regulation of G protein-coupled receptors signaling mechanisms in health and disease. He currently holds multiple research grants from the Canadian Institutes of Health Research (CIHR) for his research investigating the role of metabotropic glutamate receptor signaling in Huntington’s and Alzheimer’s disease. Dr. Stephen Ferguson on the web Carlton University Canada Research Chairs Twitter ResearchGate LinkedIn Dr. GPCR Ecosystem Thanks for listening to this podcast episode This short survey will help us understand your needs to bring you exciting and informative content; this short survey should take 5 minutes to fill. Listen and subscribe to where you get your podcasts. << Previous Podcast Episode Next Podcast Episode >>

  • Ep 12 with Dr. Antonella Di Pizio

    Dr. GPCR Podcast << Back to podcast list Dr. Antonella Di Pizio About this episode In this episode of the Dr. GPCR podcast , we meet with Dr. Antonella Di Pizio, an independent research group leader at the Leibniz Institute for Food Systems Biology at the Technical University of Munich. Antonella trained as a medicinal chemist in Italy, followed by a Ph.D. in computational medicinal chemistry, during which she developed a taste for structural biology. Antonella then moved to Israel, where she first started working on bitter taste GPCRs in Dr. Masha Niv's lab . Today, Antonella has expanded her research to olfactory GPCRs and trace amine receptors. Join us to learn more about chemosensory GPCRs and how computational pharmacology can help better understand their function. Dr. Antonella Di Pizio on the web Leibniz-Institute for Food Systems Biology at the Technical University of Munich Google Scholar PubMed LinkedIn Dr. GPCR Ecosystem Thanks for listening to this podcast episode This short survey will help us understand your needs to bring you exciting and informative content; this short survey should take 5 minutes to fill. Listen and subscribe to where you get your podcasts. << Previous Podcast Episode Next Podcast Episode >>

  • Session II | Adhesion GPCR Workshop 2024 | Dr. GPCR Ecosystem

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

  • Ep 113 with Dr. Prasenjit Saha

    Dr. GPCR Podcast << Back to podcast list Dr. Prasenjit Saha About Dr. Prasenjit Saha I conducted my doctoral research at the Indian Institute of Science, Bangalore, India, to investigate the mechanisms behind rare mitochondrial diseases, which can lead to heart failure, muscle fatigue, and neurodegenerative disorders. I am now working at the Cleveland Clinic in Ohio, USA, studying the gut microbiome and its impact on cardiovascular disease (CVD). Specifically, I am interested in understanding dysregulated G-protein coupled receptor (GPCR) signaling linked to atherosclerosis and diabetes. My research goal is to identify novel cellular target receptors of human gut microbe-derived metabolites that are pathologically linked to CVD. Discovering these receptors would be a significant breakthrough in cardiovascular biology as they could be targeted for therapeutic purposes. During my post-doctoral research, I was part of a study that identified the receptors of a novel human gut microbe-derived metabolite called phenylacetylglutamine (PAG), which is linked to cardiovascular disease. This study demonstrated that PAG is a potential diagnostic marker for CVD as it causes serious fatal conditions such as thrombus formation, which can block blood vessels. In this study, I discovered adrenergic receptors (α2A, α2B, and β2-adrenergic receptors) that serve as the gut microbial metabolite (PAG) receptor and characterized the receptor-metabolite interaction. More recently, I have shifted my focus to identifying allosteric modulators of host G-protein-coupled receptors (GPCRs) that contribute to cardio-metabolic disorders. Traditional drug discovery efforts have focused on agonists and antagonists that bind to the orthosteric site of the receptor. However, the pursuit of allosteric modulators has gained attention as they have the potential to fine-tune cellular responses with greater selectivity among the subtypes of GPCRs. My long-term plan is to conduct research in the field of receptor biology, with a focus on GPCRs. They are the largest, most versatile, and most ubiquitous class of plasma membrane receptors and serve as targets for more than one-third of all prescribed drugs currently used in the treatment of human diseases all over the world. Dr. Prasenjit Saha on the web Google Scholar Pubmed LinkedIn Dr. GPCR Thanks for listening to this podcast episode This short survey will help us understand your needs to bring you exciting and informative content; this short survey should take 5 minutes to fill. Listen and subscribe to where you get your podcasts. << Previous Podcast Episode Next Podcast Episode >>

  • Ep 141 with Dr Tobi Langenhan

    Dr. GPCR Podcast << Back to podcast list Dr. Tobi Langenhan About Dr. Tobi Langenhan "I studied medicine at the University of Würzburg, where I obtained my license to practice and my Dr. med. degree in neuroanatomy. Then I moved to the University of Oxford on a 4-year Wellcome Trust Scholarship in Neuroscience, through which I gained an M.Sc. from Somerville College and a D.Phil. from Magdalen College Oxford, both in Neuroscience. For my doctoral studies, I joined the lab of Dr Andreas Russ at the Department of Biochemistry and first came across GPCRs, particularly the receptor family I have been investigating ever since: adhesion GPCRs. After returning to Germany I set up my own lab at the Institute of Physiology at Würzburg, where I later became Heisenberg Professor for 'Physiology and pathophysiology of mechanoceptive signalling pathways'. Shortly after was recruited to the Medical Faculty of Leipzig University, where I now head the Department of General Biochemistry at the Rudolf Schönheimer Institute. I work with invertebrate animal models (mainly D. melanogaster) and in vitro techniques to pick apart the physiological and pharmacological principles that underlie the workings of adhesion GPCRs in health and disease. This entails the deciphering of cellular and organ functions, which require individual adhesion GPCRs, and extends to the development of novel screening approaches to identify pharmacological modulators of human adhesion GPCRs." Dr. Tobi Langenhan on the web Langenhan Lab ORCID LinkedIn University of Leipzig Dr. GPCR Thanks for listening to this podcast episode This short survey will help us understand your needs to bring you exciting and informative content; this short survey should take 5 minutes to fill. Listen and subscribe to where you get your podcasts. << Previous Podcast Episode Next Podcast Episode >>

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  • Adhesion GPCR Workshop 2024 | Dr. GPCR Ecosystem

    Register for the AGPCR24 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 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 Register for the AGPCR24 [ Registration extended until September 15th ] 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.

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  • Travel Tips for Adhesion GPCR Workshop 2024 | Dr. GPCR Ecosystem

    TRAVELING TIPS Adhesion GPCR workshop 2024 CINVESTAV, Mexico City, Mexico October 23-25 Register DO's and DONT's for travelers in Mexico Mexico travel advice *Travelers are encouraged to consult their country's embassy advisories as they may differ from the one posted above. The Canadian embassy provides a comprehensive list. Register for the Adhesion GPCR 2024 Learn more about the Adhesion GPCR workshop 2024 Up About the event Learn more about the Adhesion GPCR workshop 2024 and its preliminary program. Up About the venue Discover Cinvestav, the host venue for the upcoming workshop. Up Abstract Submission Submit your research abstracts following our guidelines to present at the conference. Up Logo Contest Enter our logo contest for a chance to have your design represent the upcoming event.

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    Premium Monthly $24.99 $ 24.99 Every month ​ Immerse yourself into the GPCR World Valid for 12 months + 5 day free trial Select Go to GPCR Retreat Page

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