About Dr. GPCR Podcast In each episode, we chat with an expert about their career trajectory, discoveries, and how their research contributed to the shared pool of knowledge about GPCR biology. At the high of the pandemic, the Dr. GPCR Podcast was created with three major goals in mind: Share the latest scientific discoveries in the GPCR field through discussions with experts Provide researchers with a different outlet to make their work known and Inspire young scientists to work on GPCRs. Dr. GPCR’s mission is to bring together the GPCR community from all corners of the world to connect, exchange, and collaborate to improve human health through a better understanding of GPCR biology. So far we have recorded and released over 156 episodes and hosted GPCR specialists from all over the world, including Dr. Bryan Roth, Dr. Robert Lefkowitz, Dr. Fiona Marshall, Dr. Sam Hoare, Dr. Graciela Pineyro, Dr. Debbie Hay, Dr. Randy Hall, tributes to Dr. Marc Caron with over 30 guests including Dr. Kathleen Caron, Dr. Brian Kobilka, and many other amazing scientists. Latest Podcast Episodes More podcast episodes Most Listened Podcast Episodes More podcast episodes Listen and subscribe where you get your podcasts

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< GPCR News < GPCRs in Oncology and Immunology Elucidation of active components and target mechanism in Jinqiancao granules for the treatment of prostatitis and benign prostatic hyperplasia Published date June 28, 2024 Abstract " Ethnopharmacological relevance: Prostatitis and benign prostatic hyperplasia (BPH) are inflammations of the prostate gland, which surrounds the urethra in males. Jinqiancao granules are a traditional Chinese medicine used to treat kidney stones and this medicine consists of four herbs: Desmodium styracifolium (Osbeck) Merr., Pyrrosia calvata (Baker) Ching, Plantago asiatica L. and stigma of Zea mays L. Aim of the study: We hypothesized that Jinqiancao granules could be a potential therapy for prostatitis and BPH, and this work aimed to elucidate active compounds in Jinqiancao granules and their target mechanisms for the potential treatment of the two diseases. Materials and methods: Jinqiancao granules were commercially available and purchased. Database-driven data mining and networking were utilized to establish a general correlation between Jinqiancao granules and the two diseases above. Ultra-performance liquid chromatography-mass spectrometry was used for compound separation and characterization. The characterized compounds were evaluated on four G-protein coupled receptors (GPCRs: GPR35, muscarinic acetylcholine receptor M3, alpha-1A adrenergic receptor α1A and cannabinoid receptor CB2). A dynamic mass redistribution technique was applied to evaluate compounds on four GPCRs. Nitric acid (NO) inhibition was tested on the macrophage cell line RAW264.7. Molecular docking was conducted on GPR35-active compounds and GPR35 crystal structure. Statistical analysis using GEO datasets was conducted. Results: Seventy compounds were isolated and twelve showed GPCR activity. Three compounds showed potent GPR35 agonistic activity (EC50 < 10 μM) and the GPR35 agonism action of PAL-21 (Scutellarein) was reported for the first time. Docking results revealed that the GPR35-targeting compounds interacted at the key residues for the agonist-initiated activation of GPR35. Five compounds showed weak antagonistic activity on M3, which was confirmed to be a disease target by statistical analysis. Seventeen compounds showed NO inhibitory activity. Several compounds showed multi-target properties. An experiment-based network reflected a pharmacological relationship between Jinqiancao granules and the two diseases. Conclusions: This study identified active compounds in Jinqiancao granules that have synergistic mechanisms, contributing to anti-inflammatory effects. The findings provide scientific evidence for the potential use of Jinqiancao granules as a treatment for prostatitis and BPH." Authors Han Zhou, Tao Hou, Aijin Shen, Wenyi Yu, Liangliang Zhou, Wenjie Yuan, Wanxian Wang, Yumin Yao, Jixia Wang, Yanfang Liu, Xinmiao Liang Tags Benign prostatic hyperplasia , G-protein coupled receptor , Jinqiancao granules , Network pharmacology , Prostatitis 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 Chris Langmead Chris Langmead is Professor, Deputy Director, and Better Medicines Theme Leader of the Neuromedicines Discovery Centre at the Monash Institute of Pharmaceutical Sciences (MIPS), a collaborative venture targeting new medicines development for poorly-treated mental health disorders. He also directs a collaborative neuroscience R&D program with Servier (France) and is the co-founder and CEO of Phrenix Therapeutics, a biotech spin-out from the Neuromedicines Discovery Centre that is developing next-generation therapeutics for schizophrenia. Prior to these roles this he was Head of Pharmacology at Heptares Therapeutics Ltd., a UK-based biotechnology company (2009-2012), where he was responsible all of the company’s discovery biology. He is an acknowledged expert in drug discovery, particularly in the field of psychiatry, where he has led multiple projects into late stage preclinical development, many of which have progressed into clinical trials. These successes enabled the US$400M sale of Heptares Therapeutics Ltd. to the Sosei Group Corporation in 2015. Prior to joining Heptares, Chris was a neuroscience researcher at GlaxoSmithKline, UK (1998-2009). He has a degree and PhD in pharmacology from Queens' College, Cambridge and University College London, respectively, was the youngest person to be elected as a Fellow of the British Pharmacological Society in 2012, and was the recipient of the British Pharmacological Society Novartis Prize in 2017. Chris serves on the editorial boards of the British Journal of Pharmacology, ACS Chemical Neuroscience, ACS Pharmacology & Translational Science and Frontiers in Pharmacology. He is also a corresponding member of NC-IUPHAR. He has published over 70 research articles, reviews and book chapters on drug discovery, which have been cited over 5000 times. Christopher Langmead on the web Monash University T witter Google Scholar Linkedin PubMed Monash Neuromedicines 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 Arey About this episode Brian Arey is Senior Director of Mechanistic Pharmacology within Leads Discovery and Optimization at Bristol-Myers Squibb Co . in Lawrenceville, NJ. He obtained both his MS and Ph.D. in Neuroendocrine Physiology at Florida State University before completing his postdoctoral training at Northwestern University. He then moved to work in the pharmaceutical industry where he has held positions of increasing responsibility. He currently leads a team that provides a mechanistic understanding of small molecule drug candidates across the entire portfolio of BMS. Brian has contributed to the discovery or development of 5 marketed drugs through his work spanning molecular, biochemical, cellular, and in vivo assessment of drug candidates in many different physiological systems. Dr. Arey’s laboratory discovered the first described synthetic agonists and antagonists of the FSHR and has been an early champion of signaling bias as a physiological mechanism of gonadotropin action. He continues to pioneer in drug discovery studying GPCRs and other target classes. His recently published book on signaling bias, Biased Signaling in Physiology, Pharmacology, and Therapeutics is available on Amazon . I sat down with Brian to chat about GPCRs, working in the industry, and being a leader. This is part 1 of our conversation. Dr. Brian Arey on the web LinkedIn ResearchGate 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. Aurélien Rizk About Dr. Aurélien Rizk "Dr. Aurélien Rizk is a scientist and entrepreneur in drug discovery. He is Chief Scientific Officer and co-founder of InterAx Biotech, where he specializes in the development of a technology platform deciphering cell signaling pathways combined with AI-based approaches to elucidate structure to signaling relationship. During four years of postdoctoral research at ETH Zurich and the Paul Scherrer Institute in Switzerland, under the guidance of Prof. Gebhard Schertler, he developed methods for kinetic mathematical analysis of GPCR signaling. He also worked on creating novel methods for systems biology using temporal logic specifications while pursuing his Ph.D. at INRIA Paris-Rocquencourt, France. Before focusing on the development of innovative mathematical modeling and simulation methods for drug discovery, Dr. Aurélien Rizk co-founded Algorizk, a company that created real-time physics simulations for education, serving over 1 million users. His academic background includes studies in mathematics, physics, and computer science at the French Grande École, École Normale Supérieure de Cachan." Dr. Aurélien Rizk on the web InterAx Biotech Paul Scherrer Institut The Org LinkedIn Google Scholar Dr. GPCR AI Summary AI-generated content may be inaccurate or misleading. Always check for accuracy. Quick recap Yamina Berchiche and Aurelien Rizk engaged in a conversation about their professional backgrounds and current projects. They explored the potential of merging mathematical models with biology, the complexities of GPCRs within cells, and the applicability of technology to other fields. They also discussed the founding of a company focused on GPCRs, the transition from academia to the biotech sector, the evolution of a company that started with the development of technologies combining mathematical methods and a wet lab, and the importance of interdisciplinary teamwork in drug and technology development. They emphasized the significance of mathematical models in systems biology and pharmacology and the challenges of transferring information between different families of GPCRs. They wrapped up the conversation by discussing job opportunities at Interax Biotech and their anticipation for future interactions. Summary Professional Backgrounds and Projects Discussed Yamina Berchiche and Aurelien Rizk had a conversation about their professional backgrounds and current projects. Aurelien Rizk, a co-founder and CEO of Interax Biotech, shared about the company's development of a discovery platform for GPCRs and their focus on signaling pathways. He also talked about his past experiences in mathematics, physics, and computer sciences, and his involvement in developing mathematical models for various systems. The discussion concluded without any clear decisions, action items, or open questions. Integrating Mathematical Models and Biology: A Fascinating Discussion Yamina and Aurelien Rizk had a conversation about the importance of merging mathematical models and biology. They highlighted that while there was a time when biology lagged due to the lack of appropriate tools, it is now progressing faster. They found it fascinating to integrate both fields and the potential it holds. Aurelien Rizk mentioned the importance of being able to test and adjust predictions in real-life scenarios. They also touched upon the transferability of this approach across different systems, which Yamina found attractive. GPCRs, Software, and Fluid Dynamics Yamina Berchiche and Aurelien Rizk discussed the complexities of GPCRs within cells and the potential for applying models from one system to another. Yamina also questioned Aurelien Rizk about his interest in software, computer science, and mathematics. Aurelien Rizk shared his journey of using these disciplines in biology and how his company, Interax, came to be. The discussion ended with Aurelien Rizk sharing his current work on numerical simulations of fluid dynamics. GPCRs: A Focus for New Company Aurelien Rizk and Yamina Berchiche discussed the founding of a company focused on GPCRs and the potential applicability of the technology to other fields. Aurelien Rizk shared that he had always focused on GPCRs but had also worked on other types of receptors, indicating that the technology could be applied broadly. Yamina asked if there was ever a consideration to work on targets other than GPCRs, to which Aurelien Rizk explained that they chose GPCRs due to their wide application and potential impact. The conversation concluded with Yamina asking if Aurelien Rizk had a favorite GPCR to work on, though his response was not included in the transcript. Cell Signaling and Cancer Metastasis Discussion Aurelien Rizk and Yamina Berchiche had a detailed conversation about the intricacies of cell signaling and chemokine receptors. Yamina shared her research experience, emphasizing the fascination of understanding how cells respond to gradients and signals, particularly in relation to cancer metastasis. Aurelien Rizk also contributed to the conversation, highlighting the complexity of the process. However, the transcript is somewhat unclear and disjointed, making it difficult to summarize the specific points discussed. Academia to Biotech: Strategic Planning and Interdisciplinary Approach Yamina Berchiche and Aurelien Rizk discussed the differences between academia and the biotech industry, with Aurelien Rizk sharing his experiences transitioning from academia into the biotech sector. They highlighted the strategic importance of planning in the biotech sector due to limited funds and the need to show positive results when securing new investments. Aurelien Rizk also mentioned the interdisciplinary nature of his company, which includes mathematics, signaling pathways, a wet lab for data generation, and AI and computational chemistry. The discussion also touched on recent changes in leadership at Aurelien Rizk's company, with the introduction of a new CEO a year ago and the valuable contributions of Mark Levick, a former reviewer for the European Medicines Agency and CEO of a biotech company. Technology Evolution and Ligand Residence Time Prediction Yamina Berchiche and Aurelien Rizk discussed the evolution of the company, which started with the development of technologies combining mathematical methods and a wet lab to ensure the technology functioned. They validated their technology and made collaborations for expertise on chemokine receptors. The conversation also revolved around the company's ability to predict the residence time of a ligand and its potential correlation with a therapeutic effect or activation of a specific signaling pathway. The discussion concluded with the idea that ligand residence time could be an important factor in effective therapy. Therapeutic Effect and Receptor Interactions Aurelien Rizk and Yamina had a detailed discussion about the importance of gaining more information about the therapeutic effect in patients or animals and the dynamics of receptor interactions. They emphasized the need to quantify the dynamics of the pathways and the residence time of the receptor. Yamina raised a question about the transferability of information between different families of GPCRs and the possibility of generating a mathematical model for potential patterns. They also discussed the challenges of system dependency in data and the need to express data in a uniform way to apply models. Mathematical Models in Systems Biology and Pharmacology Aurelien Rizk and Yamina discussed the importance and relevance of mathematical models in systems biology and pharmacology. They reminisced about previous meetings and events, including a GPCR retreat where Terry presented his work. Yamina mentioned her struggle with the mathematical aspects of Terry's papers but acknowledged their importance in quantifying and removing system biases. They also discussed plans to offer a course with Terry, due to high interest. Towards the end, Aurelien Rizk shared his top three 'aha' moments as a scientist, emphasizing the importance of learning and controlling systems. Interdisciplinary Teamwork and Drug Development Yamina Berchiche and Aurelien Rizk emphasized the significance of interdisciplinary teamwork in drug and technology development, noting the challenges of communication and collaboration across different fields. They also shared their preference for small molecule therapies over protein therapeutics. Aurelien Rizk confirmed his attendance at the upcoming GPCR-Targeted Drug Discovery Summit in Boston. The discussion concluded with a brief overview of job opportunities at Interax Biotech, with Aurelien Rizk and Yamina clarifying that job openings are communicated via email and through their job board. They expressed their anticipation for future interactions. 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 Structure-based discovery of functionally selective 5-HT1A receptor agonists Date & Time Saturday, November 4th / 9:05 AM Abstract Coming Soon About Peter Gmeiner "Prof. Dr. Peter Gmeiner received his Ph.D. from the University of Munich. He was a postdoc at the University of California in Berkeley, USA. He subsequently returned to Munich as a research associate at the Institute of Pharmaceutical Chemistry. Upon receiving his Dr. Habilitus, he was appointed at the University of Bonn as a Professor of Pharmaceutical Chemistry declining an offer for a professorship at the University of Heidelberg, at the same time. Peter has been chaired Full Professor of Pharmaceutical / Medicinal Chemistry at the Friedrich-Alexander University Erlangen-Nürnberg and declined an offer for the Chair for Pharmaceutical Chemistry at the University of Münster. Peter Gmeiner has been spokesman of the Research Training Group "Medicinal Chemistry of Selective GPCR Ligands" (GRK 1910). " Peter Gmeiner on the web Friedrich Alexander University Erlangen-Nürnberg Pubmed Google Scholar LinkedIn Dr. GPCR Previous Event Next Event Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec 22nd GPCR Retreat Sponsored by

Retreat 2023 About Program Registration Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule Coffee Break 4 Date & Time Friday, November 3rd / 3:00 PM Previous Event Next Event Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec 22nd GPCR Retreat Sponsored by

< GPCR News < GPCRs in Oncology and Immunology Simultaneous activation of CXC chemokine receptor 4 and histamine receptor H1 enhances calcium signaling and cancer cell migration Published date February 1, 2023 Abstract "C-X-C chemokine receptor 4 (CXCR4) is widely overexpressed in various types of cancer and is involved in several cancer phenotypes including tumor growth, survival, and metastasis. The roles of histamine and histamine receptor H1 (HRH1) in cancer pathogenesis remain controversial. Here, we show that HRH1 is widely expressed in various cancer cell lines and cancer tissues and that coexpression of CXCR4 and HRH1 is associated with poor prognosis in breast cancer. Using bimolecular fluorescence complementation and bioluminescence resonance energy transfer donor saturation assays, we demonstrate that CXCR4 and HRH1 can assemble into a heteromeric complex. Simultaneous activation of CXCR4 and HRH1 synergistically increases calcium flux in MDA-MB-231 cells that endogenously express CXCR4 and HRH1 but not in cells deficient in CXCR4 or HRH1. Costimulation of CXCR4 and HRH1 also significantly enhances CXCL12-induced MDA-MB-231 cell migration, while histamine alone does not induce cell migration. Synergistic effects on calcium flux and cell migration are inhibited by the Gαi inhibitor pertussis toxin and the Gαq inhibitor YM254890, suggesting that the Gαi and Gαq pathways are involved in the synergy. Enhanced calcium signaling and cell migration are also observed in NCI-H23 and HeLa cells, which coexpress CXCR4 and HRH1. Taken together, our findings demonstrate an interplay between CXCR4 and HRH1, and suggest the possibility of the CXCR4-HRH1 heteromer as a potential therapeutic target for anticancer therapy." Authors Chulo Park , Jin-Woo Lee , Kiheon Kim , Dong-Seung Seen , Jae-Yeon Jeong , Won-Ki Huh 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 >

< GPCR News < GPCRs in Oncology and Immunology PAXIP1-AS1 is associated with immune infiltration and predicts poor prognosis in ovarian cancer Published date August 15, 2023 Abstract "The long non-coding RNA (LncRNA) PAXIP1 antisense RNA 1 (PAXIP1-AS1) was found to promote proliferation, migration, EMT, and apoptosis of ovarian cancer (OC) cells in OC cell lines, but the relationship between PAXIP1-AS1 expression and clinical characteristics, prognosis, and immune infiltration of OC patients and its regulatory network are unclear. 379 OC tissues were collected from The Cancer Genome Atlas (TCGA) database. 427 OC tissues and 88 normal ovarian tissues were collected from GTEx combined TCGA database. 130 OC samples were collected from GSE138866. Kruskal-Wallis test, Wilcoxon sign-rank test, logistic regression, Kaplan-Meier method, Cox regression analysis, Gene set enrichment analysis (GSEA), and immuno-infiltration analysis were used to evaluate the relationship between clinical characteristics and PAXIP1-AS1 expression, prognostic factors, and determine the significant involvement of PAXIP1-AS1 in function. QRT-PCR was used to validate the expression of PAXIP1-AS1 in OC cell lines. Low PAXIP1-AS1 expression in OC was associated with age (P = 0.045), histological grade (P = 0.011), and lymphatic invasion (P = 0.004). Low PAXIP1-AS1 expression predicted a poorer overall survival (OS) (HR: 0.71; 95% CI: 0.55-0.92; P = 0.009), progression free interval (PFS) (HR: 1.776; 95% CI: 1.067-2.955; P = 0.001) and disease specific survival (DSS) (HR: 0.67; 95% CI: 0.51-0.89; P = 0.006). PAXIP1-AS1 expression (HR: 0.711; 95% CI: 0.542-0.934; P = 0.014) was independently correlated with PFS in OC patients. GSEA demonstrated that neutrophil degranulation, signaling by Interleukins, GPCR-ligand binding, G alpha I signaling events, VEGFAVEGFR-2 signaling pathway, naba secreted factors, Class A 1 Rhodopsin-Like Receptors, PI3K-Akt signaling pathway, and Focal Adhesion-PI3K-Akt-mTOR-signaling pathway were differentially enriched in PAXIP1-AS1 high expression phenotype. PAXIP1-AS1 was significantly downregulated in OC cell lines compared with IOSE29 cell line. The expression of PAXIP1-AS1 was associated with immune infiltration. low expression of PAXIP1-AS1 was correlated with poor OS (HR: 0.52; 95% CI: 0.34-0.80; P = 0.003) from GSE138866. There were some genomic variations between the PAXIP1-AS1 high and low expression groups. Low expression of PAXIP1-AS1 was significantly associated with poor survival and immune infiltration in OC. PAXIP1-AS1 could be a promising prognosis biomarker and response to immunotherapy for OC." Authors Buze Chen , Xiaoyuan Lu , Qingmei Zhou , Qing Chen , Siyan Zhu , Guilin Li , Hui Liu 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. Sudha Shenoy About Dr. Sudha Shenoy Dr. Sudha Shenoy is currently an Associate Professor in Medicine & Cell Biology in the Division of Cardiovascular Medicine, Duke University Medical Center. She received her Ph.D. from Oklahoma State University and completed her postdoctoral training with Dr. Robert J. Lefkowitz (Nobel Laureate, 2012) at Duke University. Dr. Shenoy’s postdoctoral research discovered that ubiquitination of mammalian G protein-coupled receptors is a tag for lysosomal degradation, whereas ubiquitination of the adaptor protein, β-arrestin, is a tag for receptor internalization and formation of signaling endosomes. Her laboratory has continued to work on identifying the molecular mechanisms that ascribe ubiquitin code on GPCRs and β-arrestins. Current efforts aim to understand the regulation of GPCR and beta-arrestin signaling in the heart and vascular endothelium by the deubiquitinating enzymes USP20 and USP33. Dr. Sudha Shenoy on the web Duke University Personal Reflections and Words of Wisdom: Story From Dr. Sudha Shenoy LinkedIn 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. Yamina Berchiche About Dr. Yamina Berchiche Dr. Yamina A. Berchiche is the founder of Dr. GPCR, an ecosystem designed to bring together stakeholders interested in using G-Protein Coupled Receptors (GPCRs) that control virtually everything in the body as drug targets. The mission of Dr. GPCR is to accelerate GPCR drug discovery by sharing the latest research and technology advances in the field and providing exposure to scientists through the Dr. GPCR podcast. Dr. Berchiche obtained her Master’s and Ph.D. in Biochemistry at the University of Montreal in Canada before training at Rockefeller University in New York and the National Institutes of Health in Bethesda, Maryland. She developed expertise over the past two decades studying structure/function relationships of GPCRs using live-cell bioluminescence resonance energy transfer (BRET). Her work focused on chemokine receptors, members of the GPCR family that control cell movement in the body. Dr. Yamina Berchiche on the web Website LinkedIn Facebook Twitter ResearchGate PubMed Google Scholar Dr. GPCR 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. 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 >>

Retreat 2023 About Program Registration Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule Registration Date & Time Thursday, November 2nd / 11:00 AM - 1:30 PM Previous Event Next Event Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec 22nd GPCR Retreat Sponsored by

Retreat 2023 About Program Registration Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule Dinner 1 Date & Time Thursday, November 2nd / 8:00 PM Previous Event Next Event Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec 22nd GPCR Retreat Sponsored by

Dr. GPCR Podcast << Back to podcast list Dr. Françoise Bachelerie About Dr. Françoise Bachelerie " FB leads a team at Paris-Saclay University with expertise in immunology and virology related to Host/Virus interactions and GPCR function. The team’s projects are devoted to the activation/function of CXCR4-ACKR3 (CXCR7) receptors of the CXCL12 chemokine, key effectors of the immune system, including their role in immunological disorders (e.g. WHIM syndrome) and in the innate control of the life cycle of papillomavirus, which are commensal inhabiting the healthy human epithelium (virome) while presenting an oncogenic potential that remains a major health concern. FB is recognized for her expertise and pioneering works in the field of biological and pathological functions of chemokines and their receptors, for which she made important breakthroughs regarding the CXCL12/CXCR4/ACKR3 trio. In particular, FB contributed to the discovery that CXCL12 is the ligand for the CXCR4 receptor and can therefore prevent infection by the Human Immunodeficiency Virus (HIV). FB’ team has identified the orphan CXCR7/ACKR3 receptor as being the 2nd receptor for CXCL12, which behaves as a modulator of CXCL12/CXCR4 functions. FB is a member of various international committees in the field, including the one that reviewed the standard nomenclature for chemokine receptors that are categorized into a large subgroup of G protein–coupled (GPCR) leukocyte chemotactic receptors (including CXCR4), and a smaller subgroup of atypical chemokine receptors (including the CXCR7/ACKR3). " Dr. Françoise Bachelerie on the web INSERM ResearchGate SciSpace Loop 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 >>

Dr. GPCR Podcast << Back to podcast list Dr. Steven Foord About Dr. Steven Foord Steve Foord trained as a Physiologist and Pharmacologist and worked for Glaxo through to GSK from 1986 to 2008. He introduced molecular pharmacology to a wide range of the company's GPCR projects and was able to initiate some projects. These included the identification of RAMPs (solving some CGRP family issues) and the GABA B, carboxylic, and nicotinic acid receptors. He also discovered and championed a novel prostaglandin EP4 drug candidate for development. He finished his career as Head of Bioinformatics for Neuroscience and working on the GSKs novel genetics initiative. Dr. Steven Foord on the web LinkedIn Google Scholar 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. Mark Connor About Dr. Mark Connor Undergraduate BSc with Honours in Pharmacology from University of Sydney (1987, snake neurotoxins), Ph.D. from Department of Pharmacology, University of Washington (1992, mentor Charley Chavkin , sigma receptors). Postdoc with Graeme Henderson (Bristol, opioids and Ca signaling) and Mac Christie (Sydney, opioids in neurons, novel spider toxins). Grant-funded independent research positions from 2001 at University of Sydney (opioids and sensory neurons), Vollum Institute Portland (visiting scientist with Ed McCleskey, sensory neuron properties); Pain Management Research Institute (more opioids, cannabinoids and T-type Ca channels) and Brain and Mind Research Institute (Sydney). 2009, appointed Professor of Pharmacology at Macquarie University. Focus on study of drugs and toxins on GPCR (opioid, cannabinoid receptor) and ion channel (K, Ca, TRP channel) function; mostly electrophysiology and fluorescence-based reporters, but can grind and bind. Currently pursuing molecular pharmacology of phytocannabinoids and novel synthetic cannabinoids, with a focus on efficacy and novel targets. Interested in orthosteric and allosteric interactions, and still looking for some bias ... anywhere ... these days human only. Dr. Mark Connor on the web Researchers Twitter 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 >>

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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 >>

Dr. GPCR Podcast << Back to podcast list Dr. Richard Premont About Dr. Richard Premont "Dr. Premont obtained his B.S. in Biology and Chemistry at the California Institute of Technology in 1985, and M.Ph . and Ph.D. in Biomedical Sciences (Pharmacology) at Mount Sinai School of Medicine (City University of New York) in 1990 and 1992, working with Ravi Iyengar on regulation/desensitization of the liver glucagon receptor and glucagon-stimulated adenylyl cyclase system. In 1992, he won a Helen Hay Whitney Foundation fellowship to support his post-doctoral work with Robert Lefkowitz and Marc Caron at Duke University. His initial project to identify and clone taste receptors was unsuccessful, but led to the identification of GRK5 and continued focus on GRKs (particularly GRKs 4,5,6) and arrestins as GPCR regulators and as mediators of distinct signaling pathways through partners including GIT1. In 1999, obtained an independent faculty position at Duke in Gastroenterology, where he remained until 2018 studying GPCRs and their signaling pathways in the liver and in liver disease. In 2018, he moved to Harrington Discovery Institute and Case Western Reserve University, where he studies GPCR regulation by S-nitrosylation. My research focus is on understanding how distinct cellular signaling pathways interact and are coordinated to produce integrated physiological responses, and how dysregulation of this coordination results in pathophysiology. For this, we have worked in three main areas: the regulation of G protein-coupled receptor signaling particularly by the G protein-coupled receptor kinase (GRK) – beta-arrestin system, the coordination of heterotrimeric G protein, small GTP-binding protein and protein kinase pathways by GIT/PIX scaffolding complexes during cellular signaling, and characterizing the role of protein S-nitrosylation as a signaling post-translational modification in mediating and regulating cellular signaling pathways, particularly in conjunction with better characterized signaling systems. In our work, we utilize methods including structural biology and proteomics, molecular biology and biochemical enzymology, primary and model cell culture, and transgenic, knockout, knock-in and conditional models of mouse physiology and behavior." Dr. Richard Premont on the web 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 >>

Retreat 2023 About Program Registration Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule Lunch 1 Date & Time Friday, November 3rd / 12:10 PM Previous Event Next Event Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec 22nd GPCR Retreat Sponsored by

< GPCR News < GPCRs in Oncology and Immunology Metabolic crosstalk: Extracellular ATP and the tumor microenvironment in cancer progression and therapy Published date June 28, 2024 Abstract "Adenosine 5'-triphosphate (ATP) is a vital element in energy information. It plays a critical role in transmitting signals inside the body, which is necessary for controlling the life activities of all cells, including tumor cells [1]. Its significance extends from intracellular signaling pathways to tumor regression. Purinergic signaling, a form of extracellular paracrine signaling, relies on purine nucleotides. Extracellular ectonucleotidases convert these purine nucleotides to their respective di and mono-phosphate nucleoside forms, contributing significantly to immune biology, cancer biology, and inflammation studies. ATP functions as a mighty damage-linked molecular pattern when released outside the cell, accumulating in inflammatory areas. In the tumor microenvironment (TME), purinergic receptors such as ATP-gated ion channels P2X1-5 and G protein-coupled receptors (GPCR) (P2Y) interact with ATP and other nucleotides, influencing diverse immune cell activities. CD39 and CD73-mediated extracellular ATP degradation contributes to immunosuppression by diminishing ATP-dependent activation and generating adenosine (ADO), potentially hindering antitumor immunity and promoting tumor development. Unraveling the complexities of extracellular ATP (e-ATP) and ADO effects on the TME poses challenges in identifying optimal treatment targets, yet ongoing investigations aim to devise strategies combating e-ATP/ADO-induced immunosuppression, ultimately enhancing anti-tumor immunity. This review explores e-ATP metabolism, its purinergic signaling, and therapeutic strategies targeting associated receptors and enzymes." Authors Sourav Shukla, Parameswar Dalai, Reena Agrawal-Rajput Tags Extracellular ATP (e-ATP) , Immunosuppression , Purinergic receptors , Purinergic signaling , Therapeutic potential , Tumor microenvironment (TME) 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 >

< GPCR News < GPCRs in Oncology and Immunology Identification of S1PR4 as an immune modulator for favorable prognosis in HNSCC through machine learning Published date September 15, 2023 Abstract "The multikinase inhibitor sorafenib improves event-free survival (EFS) when used with 7 + 3 in adults with newly-diagnosed acute myeloid leukemia (AML), irrespective of the FLT3-mutation status. Here, we evaluated adding sorafenib to cladribine, high-dose cytarabine, granulocyte colony-stimulating factor, and mitoxantrone (CLAG-M) in a phase 1/2 trial of 81 adults aged ≤60 years with newly diagnosed AML. Forty-six patients were treated in phase 1 with escalating doses of sorafenib and mitoxantrone. No maximum tolerated dose was reached, and a regimen including mitoxantrone 18 mg/m2 per day and sorafenib 400 mg twice daily was declared the recommended phase 2 dose (RP2D). Among 41 patients treated at RP2D, a measurable residual disease-negative complete remission (MRD- CR) rate of 83% was obtained. Four-week mortality was 2%. One-year overall survival (OS) and EFS were 80% and 76%, without differences in MRD- CR rates, OS, or EFS between patients with or without FLT3-mutated disease. Comparing outcomes using CLAG-M/sorafenib with those of a matched cohort of 76 patients treated with CLAG-M alone, multivariable-adjusted survival estimates were improved for 41 patients receiving CLAG-M/sorafenib at RP2D (OS: hazard ratio,0.24 [95% confidence interval, 0.07-0.82]; P = .023; EFS: hazard ratio, 0.16 [95% confidence interval, 0.05-0.53]; P = .003). Benefit was limited to patients with intermediate-risk disease (univariate analysis: P = .01 for OS; P = .02 for EFS). These data suggest that CLAG-M/sorafenib is safe and improves OS and EFS relative to CLAG-M alone, with benefits primarily in patients with intermediate-risk disease. The trial was registered at www.clinicaltrials.gov as #NCT02728050." Authors Chenshen Huang , Fengshuo Zhu , Hao Zhang , Ning Wang , Qi Huang Tags Cancer , Machine learning , Molecular biology 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 >

< GPCR News < GPCRs in Oncology and Immunology Purinergic GPCR-integrin interactions drive pancreatic cancer cell invasion Published date March 21, 2023 Abstract " Pancreatic ductal adenocarcinoma (PDAC) continues to show no improvement in survival rates. One aspect of PDAC is elevated ATP levels, pointing to the purinergic axis as a potential attractive therapeutic target. Mediated in part by highly druggable extracellular proteins, this axis plays essential roles in fibrosis, inflammation response and immune function. Analysing the main members of the PDAC extracellular purinome using publicly available databases discerned which members may impact patient survival. P2RY2 presents as the purinergic gene with the strongest association with hypoxia, the highest cancer cell-specific expression and the strongest impact on overall survival. Invasion assays using a 3D spheroid model revealed P2Y 2 to be critical in facilitating invasion driven by extracellular ATP. Using genetic modification and pharmacological strategies we demonstrate mechanistically that this ATP-driven invasion requires direct protein-protein interactions between P2Y 2 and αV integrins. DNA-PAINT super-resolution fluorescence microscopy reveals that P2Y 2 regulates the amount and distribution of integrin αV in the plasma membrane. Moreover, receptor-integrin interactions were required for effective downstream signalling, leading to cancer cell invasion. This work elucidates a novel GPCR-integrin interaction in cancer invasion, highlighting its potential for therapeutic targeting. " Authors Elena Tomas Bort , Megan Daisy Joseph , Qiaoying Wang , Edward Philip Carter , Nicolas Jaime Roth , Jessica Gibson , Ariana Samadi , Hemant M Kocher , Sabrina Simoncelli , Peter J McCormick , Richard Philip Grose Tags cancer biology , cell biology , human. 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 >

< GPCR News < GPCRs in Oncology and Immunology Prediction of survival and immunotherapy response by the combined classifier of G protein-coupled receptors and tumor microenvironment in melanoma Published date September 16, 2023 Abstract "Background: In this study, we aimed to investigate the potential of miR-19a as a biomarker of OSCC and its underlying molecular mechanisms. Methods: We collected serum and saliva samples from 66 OSCC patients and 66 healthy control subjects. Real-time PCR analysis, bioinformatic analysis and luciferase assays were performed to establish a potential signaling pathway of miR-19a/GRK6/GPCRs/PKC. Flowcytometry and Transwell assays were performed to observe the changes in cell apoptosis, metastasis and invasion. Results: We found that miR-19a, GPR39 mRNA and PKC mRNA were upregulated while GRK6 mRNA was downregulated in the serum and saliva samples collected from OSCC patients. Moreover, in silico analysis confirmed a potential binding site of miR-19a on the 3'UTR of GRK6 mRNA, and the subsequent luciferase assays confirmed the molecular binding between GRK6 and miR-19a. We further identified that the over-expression of miR-19a could regulate the signaling between GRK6, GPR39 and PKC via the signaling pathway of miR-19a/GRK6/GPR39/PKC, which accordingly resulted in suppressed cell apoptosis and promoted cell migration and invasion. Conclusion: Collectively, the findings of our study propose that miR-19a is a crucial mediator in the advancement of OSCC, offering a potential avenue for the development of innovative therapeutic interventions aimed at regulating GRK6 and its downstream signaling pathways." Authors Kangjie Shen , Qiangcheng Wang , Lu Wang , Yang Yang , Min Ren , Yanlin Li , Zixu Gao , Shaoluan Zheng , Yiteng Ding , Jiani Ji , Chenlu Wei , Tianyi Zhang , Yu Zhu , Jia Feng , Feng Qin , Yanwen Yang , Chuanyuan Wei , Jianying Gu Tags G protein-coupled receptors , Immunotherapy , Melanoma , Multi-omics , Pan-cancer , Tumor microenvironment , scRNA-seq 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 >