Dr. GPCR Podcast << Back to podcast list Dr. Caron Tribute Part 2 ! Widget Didn’t Load Check your internet and refresh this page. If that doesn’t work, contact us. 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 >>

Dr. GPCR Podcast << Back to podcast list 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 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 >>

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

Dr. GPCR Podcast << Back to podcast list Dr. Jennifer Pluznick About this episode Dr. Pluznick discovered that olfactory receptors in mice are also expressed in their kidneys and blood vessels. Her research is focused on the role of chemosensory GPCRs in regulating renal and cardiovascular function, and identifying renal/cardiovascular olfactory receptor ligands, and relating them to whole-animal physiology. This work contributes to a better understanding of how the kidney helps maintain homeostasis in humans. Jennifer is currently an assistant professor of physiology at the Johns Hopkins School of Medicine. She received her undergraduate degree in biology from Truman State University and earned her Ph.D. in renal physiology from the University of Nebraska Medical Center. She then spent five years training as a postdoctoral fellow in the laboratory of Michael Caplan at Yale University, where she studied both renal physiology and sensory biology systems and focused on olfaction. Dr. Jennifer Pluznick on the web John Hopkins Pluznick Lab Pubmed Ted Talk 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 >>

Dr. GPCR Podcast << Back to podcast list Dr. Brian Bender About Dr. Brian Bender Dr. Bender completed his undergraduate studies at Colgate University in upstate New York with a degree in Biochemistry. Between undergraduate and graduate school Brian worked as a technician in an academic lab before moving to Nashville, TN for graduate work at Vanderbilt University where he joined the Department of Pharmacology. Brain’s work there primarily focused on structure prediction of GPCRs from sparse experimental data. He then moved to the University of California in San Francisco to continue his training as a postdoctoral researcher where he used structural models of GPCRs to virtually screen large compound libraries with the goal of finding new chemical matter to probe understudied and orphan receptors. Brian is involved in organizing the GRC/GRS Molecular Pharmacology meeting, which has been postponed to 2023. Brian is one of the organizers of the upcoming Transatlantic ECI GPCR Symposium . Dr. Brian Bender on the web LinkedIn Twitter ResearchGate Dr.GPCR Member Google Scholar 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 >>

Dr. GPCR Podcast << Back to podcast list Dr. Aurélien Rizk ! Widget Didn’t Load Check your internet and refresh this page. If that doesn’t work, contact us. 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 >>

< GPCR News < GPCRs in Oncology and Immunology Neuroimmune interplay during type 2 inflammation: symptoms, mechanisms and therapeutic targets in atopic diseases Published date August 25, 2023 Abstract "Type 2 inflammation is characterized by overexpression and heightened activity of type 2 cytokines, mediators and cells that drive neuroimmune activation and sensitization to previously sub-threshold stimuli. The consequences of altered neuroimmune activity differ with tissue type and disease and include: skin inflammation, sensitization to pruritogens, and itch amplification in atopic dermatitis and prurigo nodularis; airway inflammation/hyperresponsiveness, loss of expiratory volume, airflow obstruction and increased mucus production in asthma; loss of sense of smell in chronic rhinosinusitis with nasal polyps; and dysphagia in eosinophilic esophagitis. We describe the neuroimmune interactions that underlie the various sensory and autonomic pathologies in type 2 inflammatory diseases and present recent advances in targeted treatment approaches to reduce type 2 inflammation and its associated symptoms in these diseases. Further research is needed to better understand the neuroimmune mechanisms that underlie chronic, sustained inflammation and its related sensory pathologies in diseases associated with type 2 inflammation." Authors Brian Kim , Marc E Rothenberg , Xin Sun , Claus Bachert , David Artis , Raza Zaheer , Yamo Deniz , Paul Rowe , Sonya Cyr . Tags ABPA , ACh , AD , ADCC , AFR , AHR , AR , ASM , Acetylcholine , Airway hyperresponsiveness , Airway smooth muscle , Allergic bronchopulmonary aspergillosis , Allergic fungal rhinosinusitis , Allergic rhinitis , Antibody-dependent cellular cytotoxicity , Atopic dermatitis , BAM8-22 , BP , Beta chain , Bovine adrenal medulla peptide 8-22 , Bullous pemphigoid , C-C motif chemokine ligand 17 , CCL17 , CGRP , CIU , COPD , CRSsNP , CRSwNP , CSF2 , CSU , Calcitonin gene-related peptide , Chronic idiopathic urticaria , Chronic obstructive pulmonary disease , Chronic rhinosinusitis with nasal polyps , Chronic rhinosinusitis without nasal polyps , Chronic spontaneous urticaria , Colony stimulating factor 2 , DRG , Dorsal root ganglion , EGPA , EMA , EoE , Eosinophilic esophagitis , Eosinophilic granulomatosis with polyangiitis , European Medicines Agency , FDA , FcεRIα , FeNO , Fractional exhaled nitric oxide , G-protein-coupled receptor , GPCR , Group 2 innate lymphoid cell , HES , High-affinity Fc receptor for IgE , Hypereosinophilic syndrome , IFNG-AS1 , IFNγ , IL , IL-13R , IL-13Rα1/2 , IL-1RαP , IL-31R , IL-31RA , IL-33R , IL-4Rα , IL-5Rα , ILC , ILC2 , IRF1 , IgE , Immunoglobulin E , Innate lymphoid cell , Interferon gamma-AS1 , Interferon regulatory factor 1 , Interferon-gamma , Interleukin , Interleukin-1 receptor alpha P , Interleukin-13 receptor , Interleukin-13 receptor alpha 1/2 , Interleukin-31 receptor , Interleukin-31 receptor A , Interleukin-33 receptor , Interleukin-4 receptor alpha , Interleukin-5 receptor alpha , JAK , JAK inhibitors , JAKi , Janus kinase , MAPK , MCP-4 , MRGPRX1 , Mas-related family of G protein-coupled receptor 11 , Mas-related family of G protein-coupled receptor X1 , Mas-related family of G-protein-coupled receptor 3 , Mas-related family of G-protein-coupled receptors , Mitogen-activated protein kinase , Monoclonal antibody , Monocyte chemoattractant protein-4 , MrgprA , MrgprA3 , MrgprCr11 , NGF , NMU , NP , Na(v) , Nasal polyps , Nerve growth factor , Neuromedin U , OSM , OSMRβ , Oncostatin M , Oncostatin-M specific receptor subunit beta , PAR2 , PC(20) , PN , Protease activated receptor 2 , Provocative concentration causing a 20% drop in forced expiratory volume in 1 second from baseline , Prurigo nodularis , SP , STAT , Sialic-acid-binding immunoglobulin-like lectin 8 , Signal transducer and activator of transcription , Substance P , T helper type 2 cell , TRP , TRPA1 , TRPM4 , TRPM8 , TRPV1 TRPV4 , TSLP , TSLPR , Th2 , Thymic stromal lymphopoietin , Thymic stromal lymphopoietin receptor , Transient receptor potential , Transient receptor potential ankyrin 1 , Transient receptor potential cation channel subfamily M member 4 , Transient receptor potential cation channel subfamily M member 8 , Transient receptor potential vanilloid 1 , US Food and Drug Administration , VIP , Vasoactive intestinal peptide , Voltage-gated sodium channel , gamma chain , mAb , mIgE , membrane IgE , siglec-8 , Βc , β2-adrenergic receptor , β2AR , γc. Source Classified GPCR News More from Dr. GPCR Share < Previous Next >

Dr. GPCR Podcast << Back to podcast list Scott Struthers R. Scott Struthers, Ph.D., is our co-founder and has served as our President and Chief Executive Officer since December 2008. Prior to Crinetics, he was senior director and head of endocrinology and metabolism at Neurocrine Biosciences, Inc., from 1998 to 2008. At Neurocrine, he initiated and led the effort to discover and develop orally active, nonpeptide GnRH antagonists, including elagolix. Prior to Neurocrine, from 1995 to 1998, he co-founded ScienceMedia Inc. to develop eLearning solutions for the life sciences and higher education markets. Between 1992 to 1995 he led contract research efforts at Biosym Technologies to develop and apply computational tools for drug discovery. In 2021, Dr. Struthers co-founded and serves as board chair at Radionetics Oncology, a pharmaceutical company focused on the discovery and development of novel radiotherapeutics for oncology indications. In addition, he is a member of the board of directors of the San Diego Entrepreneurs Exchange, a nonprofit organization that provides resources for early-stage start-ups, which he co-founded in [2009.] R. Scott Struthers on the web LinkedIn Google Scholar Crinetics Radionetics 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 >>

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< GPCR News < GPCRs in Oncology and Immunology Combinatorial depletions of G-protein coupled receptor kinases in immune cells identify pleiotropic and cell type-specific functions Published date November 1, 2022 Abstract G-protein coupled receptor kinases (GRKs) participate in the regulation of chemokine receptors by mediating receptor desensitization. They can be recruited to agonist-activated G-protein coupled receptors (GPCRs) and phosphorylate their intracellular parts, which eventually blocks signal propagation and often induces receptor internalization. However, there is growing evidence that GRKs can also control cellular functions beyond GPCR regulation. Immune cells commonly express two to four members of the GRK family (GRK2, GRK3, GRK5, GRK6) simultaneously, but we have very limited knowledge about their interplay in primary immune cells. In particular, we are missing comprehensive studies comparing the role of this GRK interplay for (a) multiple GPCRs within one leukocyte type, and (b) one specific GPCR between several immune cell subsets. To address this issue, we generated mouse models of single, combinatorial and complete GRK knockouts in four primary immune cell types (neutrophils, T cells, B cells and dendritic cells) and systematically addressed the functional consequences on GPCR-controlled cell migration and tissue localization. Our study shows that combinatorial depletions of GRKs have pleiotropic and cell-type specific effects in leukocytes, many of which could not be predicted. Neutrophils lacking all four GRK family members show increased chemotactic migration responses to a wide range of GPCR ligands, whereas combinatorial GRK depletions in other immune cell types lead to pro- and anti-migratory responses. Combined depletion of GRK2 and GRK6 in T cells and B cells shows distinct functional outcomes for (a) one GPCR type in different cell types, and (b) different GPCRs in one cell type. These GPCR-type and cell-type specific effects reflect in altered lymphocyte chemotaxis in vitro and localization in vivo. Lastly, we provide evidence that complete GRK deficiency impairs dendritic cell homeostasis, which unexpectedly results from defective dendritic cell differentiation and maturation in vitro and in vivo . Together, our findings demonstrate the complexity of GRK functions in immune cells, which go beyond GPCR desensitization in specific leukocyte types. Furthermore, they highlight the need for studying GRK functions in primary immune cells to address their specific roles in each leukocyte subset. Authors Katharina M Glaser, Teresa K Tarrant, Tim Lämmermann Tags B cells; G-protein coupled receptors; GRK; T cells; dendritic cells; immune cell trafficking; leukocytes; neutrophils. Source Classified GPCR News More from Dr. GPCR Share < Previous Next >

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Dr. GPCR Podcast << Back to podcast list The Role of Quantitative Sciences in GPCRs with Dr. Nagarajan Vaidehi About Dr. Nagarajan Vaidehi "Nagarajan Vaidehi, Ph.D., is professor and chair of the Department of Computational and Quantitative Medicine (DCQM) at the Beckman Research Institute of the City of Hope in Los Angeles, CA. She is also the Associate Director of the City of Hope Comprehensive Cancer Center. Dr. Vaidehi received her Ph.D. in quantum chemistry from the Indian Institute of Technology in India, where she was honored with the Distinguished Alumni Award in 2016. Following her postdoctoral studies on protein dynamics simulation methods at University of Southern California, and at Caltech, she became the director of biomolecular simulations at the Materials and Process Simulation Center, Beckman Institute at Caltech. Dr. Vaidehi joined the Beckman Research Institute of the City of Hope in 2006 as a Professor and became chair of DCQM in 2018. She has advanced the use of computational methods to meet the challenges of designing therapeutics with lower off target effects. She is an internationally recognized biophysicist for her contributions in developing constrained molecular dynamics simulation methods with emphasis on application to G-protein coupled receptors and drug design." Dr. Nagarajan Vaidehi on the web City of Hope Google Scholar 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 >>

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 >

Dr. GPCR Podcast << Back to podcast list Dr. Rosie Dawaliby About Dr. Rosie Dawaliby "I’m an expert in early-stage drug discovery, targeting membrane proteins, especially GPCR. I have 10 years of experience in the development and management of R&D projects and teams in the field of pharmacology, in prestigious academic laboratories as well as in biopharmaceutical companies in Europe and the United States. I hold a Ph.D. in Life Sciences from the University of Lausanne, Switzerland, Department of Biochemistry (2005-2009), where I started working on membranes and membrane protein biochemistry by studying membrane fusion and autophagy in yeast and mammalian cells. I have developed my expertise in the field of pharmacology and biochemistry of GPCR and the crucial role of the lipidic environment on their structure and function during my post-doctoral work (2010-2015). This joint project between prof. Brian Kobilka's lab at Stanford University and the SFMB laboratory at the Université Libre de Bruxelles (ULB) resulted in the first systematic study of phospholipid's effect on GPCR conformation and function. In 2016, I joined a company that specialized in therapeutic candidate discovery targeting GPCR ( Confo Therapeutics ) as a team and project leader for antibody discovery for metabolic and inflammatory diseases. I developed G.CLIPS biotech's innovative technology as a synthesis of the different knowledge, experiences, and know-how from the different stages of my career. Before founding G.CLIPS biotech in June 2020. And since then, my incredible adventure as CEO of this fast-growing company started and is continuing." Dr. Rosie Dawaliby on the web LinkedIn Dr. GPCR Ecosystem G.CLIPS Biotech on the web Website LinkedIn 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 >>

< GPCR News < GPCRs in Oncology and Immunology Chemokine N-terminal-derived peptides differentially regulate signaling by the receptors CCR1 and CCR5 Published date November 23, 2023 Abstract "Inflammatory chemokines are often elevated in disease settings, where the largest group of CC-chemokines are the macrophage inflammatory proteins (MIP), which are promiscuous for the receptors CCR1 and CCR5. MIP chemokines, such as CCL3 and CCL5 are processed at the N-terminus, which influences signaling in a highly diverse manner. Here, we investigate the signaling capacity of peptides corresponding to truncated N-termini. These 3 to 10-residue peptides displayed weak potency but, surprisingly, retained their signaling on CCR1. In contrast, none of the peptides generated a signal on CCR5, but a CCL3-derived tetrapeptide was a positive modulator boosting the signal of several chemokine variants on CCR5. In conclusion, chemokine N-termini can be mimicked to produce small CCR1-selective agonists, as well as CCR5-selective modulators." Authors Olav Larsen , Sara Schuermans , Anna Walser , Stavroula Louka , Ida Aaberg Lillethorup , Jon Våbenø , Katrine Qvortrup , Paul Proost , Mette M Rosenkilde Tags GPCR , allosteric modulation , chemokine , chemokine truncation , pharmacology 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 >

Dr. GPCR Podcast << Back to podcast list Dr. Maria Waldhoer About this episode Dr. Maria Waldhoer is originally from Austria. She earned her M.Sc. in Zoology and Neurobiology before completing a Ph.D. in Biology and Pharmacology at the University of Vienna. GPCRs led Maria to Thue W. Schwartz’s lab in Copenhagen where she completed her postdoctoral training. After working in the US and at the University in Graz in Austria, Maria worked several years at Novo Nordisk before joining InterAx Biotech in Switzerland as their Chief Scientific Officer. Even though Maria stumbled upon the GPCR field, her 20 years in both academia and in the industry working on GPCRs make her a strong and dedicated scientific leader. Dr. Maria Waldhoer on the web LinkedIn InterAx Biotech Pubmed 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 >>

Dr. GPCR Podcast << Back to podcast list Dr. Nicholas Holliday About Dr. Nicholas Holliday After an undergraduate degree at the University of Cambridge, Nick carried out his Ph.D. at King’s College London, supported by an AJ Clark Ph.D. studentship from the British Pharmacological Society. It was these studies and subsequent postdoctoral work that led to Nick's interest in peptide messengers regulating appetite, metabolism, and the immune system, and the molecular mechanisms underlying the signaling and regulation of their GPCRs. Nick joined the University of Nottingham in 2006, where he is now Associate Professor, establishing a lab focused on G protein-coupled receptor kinetics, signaling, and trafficking and on using novel imaging techniques, such as fluorescent ligands and complementation methods, to investigate the underlying mechanisms. Since 2019, Nick has combined his university role with the leadership of Excellerate Bioscience as Chief Scientific Officer, a contract research organization specializing in molecular and cellular pharmacology. Excellerate is involved in several pre-clinical drug discovery projects for both GPCR and non-GPCR targets, using its expertise in pharmacology to deliver high-quality target validation, lead optimization, and mechanism of action studies for our clients. Dr. Nicholas Holliday on the web LinkedIn ORCID University of Nottingham Twitter Excellerate Bio 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 >>

Dr. GPCR Podcast << Back to podcast list Dr. Jean Martin Beaulieu About Dr. Jean Martin Beaulieu Dr. Beaulieu received a Ph.D. in Neurological Sciences from McGill University and completed his post-doctoral training at Duke University. Prior to his recruitment Dr. Beaulieu was an associate professor and Canada Research Chair (Tier2) in the Department of Psychiatry and Neuroscience at Laval University. Dr. Beaulieu’s research is aimed at understanding how cellular and molecular mechanisms regulated by psychoactive drugs intersect with genetic risk factors for mental illnesses such as schizophrenia, depression, and bipolar disorder. Dr. Beaulieu has pioneered work establishing a role for Beta-arrestin signaling in the brain in vivo and has established its importance in D2 dopamine receptors (D2R) functions. These receptors belong to the super-family of G-protein coupled receptors (GPCR), the major molecular target for drug development. In particular, D2R is the main pharmacological target of antipsychotic drugs prescribed for schizophrenia and bipolar disorders. Work by the Beaulieu Lab has demonstrated that mood stabilizer drugs (e.g. lithium) used for bipolar disorder therapy target signaling mechanisms regulated by dopamine receptors, thus providing a framework to understand how different drug classes can engage overlapping cellular mechanisms to exert their action. The Beaulieu group is presently investigating how cell surface express proteins can act as allosteric modulators of D2R signaling and explores the potential usefulness of beta-arrestins for the development of new pharmaceutical agents. Translational validation is important to validate findings obtained from experimental models research and bridge the gap between bench and bedside. Working in collaboration with geneticists, the Beaulieu-Lab has identified interactions between cellular mechanisms engaged by D2R and psychiatric drugs with genetic risk factors implicated in schizophrenia by large whole-genome association studies (GWAS) in humans. These investigations have led to the identification of an RNA binding protein (FXR1P) involved in the regulation of protein synthesis as a potential downstream effector of the action of mood stabilizers and other psychoactive drugs. In addition to basic research, the Beaulieu group is also actively implicated in translational research and industry collaboration to develop new drugs and drug development technology. Dr. Jean Martin Beaulieu on the web University of Toronto Google Scholar LinkedIn ResearchGate 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 >>

< GPCR News < GPCRs in Oncology and Immunology LPA1-mediated inhibition of CXCR4 attenuates CXCL12-induced signaling and cell migration Published date September 25, 2023 Abstract "Background: G protein-coupled receptor heteromerization is believed to exert dynamic regulatory impact on signal transduction. CXC chemokine receptor 4 (CXCR4) and its ligand CXCL12, both of which are overexpressed in many cancers, play a pivotal role in metastasis. Likewise, lysophosphatidic acid receptor 1 (LPA1) is implicated in cancer cell proliferation and migration. In our preliminary study, we identified LPA1 as a prospective CXCR4 interactor. In the present study, we investigated in detail the formation of the CXCR4-LPA1 heteromer and characterized the unique molecular features and function of this heteromer. Methods: We employed bimolecular fluorescence complementation, bioluminescence resonance energy transfer, and proximity ligation assays to demonstrate heteromerization between CXCR4 and LPA1. To elucidate the distinctive molecular characteristics and functional implications of the CXCR4-LPA1 heteromer, we performed various assays, including cAMP, BRET for G protein activation, β-arrestin recruitment, ligand binding, and transwell migration assays. Results: We observed that CXCR4 forms heteromers with LPA1 in recombinant HEK293A cells and the human breast cancer cell line MDA-MB-231. Coexpression of LPA1 with CXCR4 reduced CXCL12-mediated cAMP inhibition, ERK activation, Gαi/o activation, and β-arrestin recruitment, while CXCL12 binding to CXCR4 remained unaffected. In contrast, CXCR4 had no impact on LPA1-mediated signaling. The addition of lysophosphatidic acid (LPA) further hindered CXCL12-induced Gαi/o recruitment to CXCR4. LPA or alkyl-OMPT inhibited CXCL12-induced migration in various cancer cells that endogenously express both CXCR4 and LPA1. Conversely, CXCL12-induced calcium signaling and migration were increased in LPAR1 knockout cells, and LPA1-selective antagonists enhanced CXCL12-induced Gαi/o signaling and cell migration in the parental MDA-MB-231 cells but not in LPA1-deficient cells. Ultimately, complete inhibition of cell migration toward CXCL12 and alkyl-OMPT was only achieved in the presence of both CXCR4 and LPA1 antagonists. Conclusions: The presence and impact of CXCR4-LPA1 heteromers on CXCL12-induced signaling and cell migration have been evidenced across various cell lines. This discovery provides crucial insights into a valuable regulatory mechanism of CXCR4 through heteromerization. Moreover, our findings propose a therapeutic potential in combined CXCR4 and LPA1 inhibitors for cancer and inflammatory diseases associated with these receptors, simultaneously raising concerns about the use of LPA1 antagonists alone for such conditions. Video Abstract." Authors Jong Min Hong , Jin-Woo Lee , Dong-Seung Seen , Jae-Yeon Jeong , Won-Ki Huh Tags Cancer , Chemokine receptor 4 , Chemotaxis , G protein-coupled receptor , GPCR heteromer , GPCR signaling , Inflammatory disease , Lysophosphatidic acid receptor 1 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 >

Retreat 2023 About Program Registration Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule Unveiling Non-Canonical Functions for Gαq Signaling Pathways Date & Time Friday, November 3rd / 11:55 AM About Catalina Ribas " Dr. Catalina Ribas, is currently an Associate Professor at the University Autonomous of Madrid (UAM) and she has been Academic Secretary of Molecular Biology Department for several years. The research group led by Dr. Catalina Ribas, located in the Centro de Biología Molecular “Severo Ochoa” (UAM/CSIC) and belongs also to the Health Research Institute La Princesa, has extensive experience in the field of GPCR. Dr. Catalina Ribas made a postdoctoral stay in the laboratory of Dr. SM. Lanier in the MUSC (USA). During this period and her doctoral thesis, she has deepened the regulatory mechanisms of GPCR signaling. In her postdoctoral period, she has participated in the identification and characterization of proteins that act at the level of G proteins and which are part of a multimolecular signaling complex (AGS, de “Activators of G-protein signaling). In Spain, Dr. Ribas continued working on the regulation of GPCR. The group of Dr. Ribas has characterized the existence of a new signaling pathway with a relevant role in cardiac hypertrophy led by a new Gαq interactome. Recently, Dr. Ribas' group has described a new interaction region in a cellular protein that has turned out to be very relevant in the control of the cellular process known as autophagy. These results have been published in the journal Nature Communications (12 (1):4540, 2021) with the title "Gαq controls autophagy via modulation of the mTORC1 signaling hub". Furthermore, Dr. Ribas has also described a new protective role of G protein-coupled receptor kinase 2 (GRK2), a known regulator of Gq-GPCR signaling in HNSCC tumor progression (International Journal of Cancer, 2020). " Catalina Ribas on the web Severo Ochoa Molecular Biology Center X (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

Dr. GPCR Podcast << Back to podcast list Dr. Terry Hébert About this episode Dr. Terry Hébert wanted to be a microbiologist. Instead, he ended up getting interested in membrane protein as he followed the biology of a bacterial toxin that affects a mammalian ion channel. Today he and his team are working on understanding receptor signaling in specialized cellular environments to gain a better grasp of receptor function in pathophysiological settings with a special interest in the cardiovascular system. His favorite GPCR is the angiotensin 1 receptor, especially for its ability to activate a large variety of signaling pathways. Terry is also very active on social media. With over 2000 followers on Facebook and Twitter, he shares the latest available information on GPCR research daily. Dr. Terry Hébert on the web Institute of Health Sciences Education Hébert Lab LinkedIn Facebook GPCR Consortium PubMed 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 >>

Full Agenda Adhesion GPCR workshop 2024 CINVESTAV, Mexico City, Mexico October 23-25 Download PDF Program HERE < Back to Full Agenda Session VII Physiological and pathological roles of AGPCRs in the nervous system Uncovering the signaling pathway of the ADGRA homolog Remoulade in Drosophila Beatriz Blanco Redondo The Adhesion GPCR Latrophilin Interacts With The Notch Pathway To Control Germ Cell Proliferation Willem Berend Post Uncovering the signaling pathway of the ADGRA homolog Remoulade in Drosophila Beatriz Blanco Redondo Abstract "The Drosophila genome contains five loci encoding adhesion G-protein coupled receptors (aGPCRs). Phylogenetic analysis revealed that the remoulade (remo) gene is a homologue of the vertebrate aGPCR ADGRA family, sharing the same overall receptor domain structure. In vivo expression profiling has shown Remo expression in the central (CNS) and peripheral nervous systems (PNS) of third-instar larvae (L3) and adults. In L3 PNS specimen Remo is expressed in a subset of neurons expressing the DEG/ENaC channel pickpocket (PPK), which is involved in transduction of sensory information like nociception. remoKO larvae and animals, in which remo was knocked down in ppk-neurons through RNA interference, show a higher nocifensive response compared to wildtype remorescue controls indicating that remo is required in PPK-neurons for this behaviour. Furthermore, with the aim to analyse the biochemical properties of Remo, we performed immunoprecipitation analysis. We found that the receptor is cleaved despite the lack of a consensus GPS sequence. Hence, Remo is proteolytically processed, either by the GAIN domain or an alternative protease that cleaved Remo near the GPS. We also aimed at identifying the signaling pathway that Remo is involved in. The mammalian Remo homolog ADGRA2/Gpr124 cooperates with other GPCRs of the Frizzled family, and the transmembrane proteins RECK and Lrp5/6. Collectively these proteins form a cell surface complex that acts as a recognition platform for Wnt ligands. Knowledge of the structural dynamics of this complex is limited and pharmacological and in vivo systems that would allow its characterization are scarce. Remo may serve a role in this peculiar signaling pathway and require further analysis." Authors & Affiliations "Auger, Genevieve Marie1, Bigl, Marina1, America, Michelle2, Vanhollebeke Benoit2, Langenhan Tobias1 1Rudolf Schönheimer Institute of Biochemistry, Division of General Biochemistry, Medical Faculty, Leipzig University, Johannisallee 30, 04103 Leipzig, Germany 2Laboratory of Neurovascular Signaling, Department of Molecular Biology, ULB Neuroscience Institute, Université libre de Bruxelles (ULB), Gosselies B-6041, Belgium" About Beatriz Blanco Redondo "I studied Biomedicine at the University of Barcelona. After my bachelors, I moved to Germany where I obtained my Master’s of Science and PhD degree in Dr. Buchner’s group at the University of Wuerzburg. Shortly after receiving my PhD, I joined Dr. Neil Shneider’s group as a postdoctoral research scientist at Columbia University, New York, where I studied the mechanisms of motor neuron degeneration in Amyotrophic Lateral Sclerosis (ALS). In 2017, I joined the group of Prof. Langenhan where I am studying and characterizing newly generated adhesion GPCR receptors in Drosophila as a model organism for future pharmacological applications." Beatriz Blanco Redondo on the web Blanco-Redondo Lab LinkedIn Google Scholar X (Twitter) The Adhesion GPCR Latrophilin Interacts With The Notch Pathway To Control Germ Cell Proliferation Willem Berend Post Abstract Only available for AGPCR 24 Attendees Authors & Affiliations "Groß Victoria Elisabeth 1, Matúš Daniel 2,3, Kaiser Anette 4, Ließmann Fabian 5, Meiler Jens 5, Schöneberg Torsten 2,6, Prömel Simone 1 1 Institute of Cell Biology, Department of Biology, Heinrich Heine University Düsseldorf, Düsseldorf, Germany 2 Rudolf Schönheimer Institute of Biochemistry, Medical Faculty, Leipzig University, Leipzig, Germany 3 Department of Molecular and Cellular Physiology, Stanford University, Stanford CA, USA 4 Department of Anaesthesiology and Intensive Care, Medical Faculty, Leipzig University, Leipzig, Germany 5 Institute for Drug Discovery, Faculty of Medicine, Leipzig University 6 School of Medicine, University of Global Health Equity, Kigali, Rwanda" About Willem Berend Post "Willem Berend Post is a PhD student in Cell Biology at Heinrich Heine University in Düsseldorf, Germany. His research focuses on the relevance of aGPCRs in physiology and signaling using both in vitro and in vivo approaches." Willem Berend Post on the web Cell Biology LinkedIn < Previous Session Next Session >

Dr. GPCR Podcast << Back to podcast list Dr. Graeme Milligan About Dr. Graeme Milligan Professor Graeme Milligan is Gardiner Professor of Biochemistry, Dean of Research, and Deputy Head of the College of Medical, Veterinary, and Life Sciences at the University of Glasgow. His main research group centers on the function, structure, and regulation of G protein-coupled receptors (GPCRs) and their interacting proteins. His experience also includes translating knowledge generated into the selection of targets, screening, and identification of small molecule regulators of these proteins, and progressing such ligands in drug development programs. Prof. Milligan has published more than 550 peer-reviewed articles and his research has been cited more than 35,000 times. He was elected to the Fellowship of the Royal Society of Edinburgh in 1998 and to the Fellowship of the Academy of Medical Sciences in 2016. Prof. Milligan is the co-founder of both Caldan Therapeutics (2015) which discovers novel therapeutics for metabolic diseases including Type 2 Diabetes and other indications including non-alcoholic steatohepatitis (NASH) and inflammatory diseases and Keltic Pharma Therapeutics (2020) which is developing new treatments for malaria. Dr. Graeme Milligan on the web University of Glasgow ResearchGate PubMed Orcid Google Scholar 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 >>

Dr. GPCR Podcast << Back to podcast list Dr. Patrick Sexton About Dr. Patrick Sexton Patrick Sexton is a Professor of Pharmacology, National Health and Medical Research Council of Australia Senior Principal Research Fellow, and Director of the Australian Research Council Centre for Cryo-electron Microscopy of Membrane Proteins ( www.ccemmp.org ). He is a leader in the study of GPCRs, biased agonism, and also on allosteric interactions between GPCRs and other proteins and small molecule ligands. More recently, his team has been at the forefront of the application of cryo-EM to elucidate of the structure and dynamics of GPCRs. Prof. Sexton has published over 320 peer-reviewed journal articles and has been cited >26,000 times (Google Scholar). He is a 2021 Clarivate Analytics Highly Cited Researcher in two disciplines: Pharmacology & Toxicology and Biology & Biochemistry, a corresponding member of the International Union of Basic and Clinical Pharmacology Committee on Receptor Nomenclature and Drug Classification, and a member of the Faculty of 1000 (Molecular Pharmacology division) and an elected Fellow of the British Pharmacological Society (BPS). Prof. Sexton’s awards include the Australasian Society for Clinical and Experimental Pharmacologists and Toxicologists (ASCEPT) Lecturer award, Endocrine Society of 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 the San Francisco-based biotechnology company Septerna Inc . Dr. Patrick Sexton on the web CCeMMP Monash University 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 >>

Dr. GPCR Podcast << Back to podcast list Dr. Mark Connor ! Widget Didn’t Load Check your internet and refresh this page. If that doesn’t work, contact us. 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 >>

Full Agenda Adhesion GPCR workshop 2024 CINVESTAV, Mexico City, Mexico October 23-25 Download PDF Program HERE < Back to Full Agenda Leaving for City Center Coming Soon < Previous Session Next Session >