LOGO CONTEST Adhesion GPCR workshop 2024 CINVESTAV, Mexico City, Mexico October 23-25 Register Rules for the logo contest Design must be based on “Alebrijes” [ah-leh-bree-hez], which are chimeric creatures from Mexican folklore AND contain adhesion GPCRs Avoid copyrighted material unless a CC BY / open-use license has been acquired or generated (Adobe Stock, etc). The Consortium must be free to use the design. Requirements: Resolution 300 ppi max, JPEG/TIFF/EPS/PNG/PDF formats, 5MB max Open to all adhesion GPCR community members. Artist-scientists must be registered to attend the adhesion GPCR workshop 2024 in Mexico City. The contest deadline is August 15th, 2024, 11:59 PM CST (designs received after the deadline will not be considered) Designs or inquiries should be sent to this email The prize for the selected design will include free registration and more! Register for the Adhesion GPCR 2024 Learn more about the Adhesion GPCR workshop 2024 Up About the event Learn more about the Adhesion GPCR workshop 2024 and its preliminary program. Up About the venue Discover Cinvestav, the host venue for the upcoming workshop. Up Abstract Submission Submit your research abstracts following our guidelines to present at the conference. Up Traveling Tips Find essential tips about Mexico City, including transportation options and local insights.

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

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Dr. GPCR Podcast << Back to podcast list Dr. Terry Kenakin About Dr. Terry Kenakin After obtaining a BSc in chemistry at the University of Alberta Edmonton Canada, Terry received his Ph.D. in Pharmacology from the University of Alberta, Department of Chemistry, Canada. Dr. Kenakin then moved to the UK, where he did a post-doctoral fellowship in University College London with Sir James Black. His next stop took him to Burroughs-Wellcome (BW) in Research Triangle Park (RTP) in North Carolina USA. After 7 years at BW, Dr. Kenakin joined Glaxo Inc in RTP where he remained for 25 years through iterations of Glaxo Inc, GlaxoWellcome , and finally GlaxoSmithKline . Since 2011, Terry works at the Department of Pharmacology at the University of North Carolina School of Medicine Chapel Hill NC. His interests are in receptor pharmacology, allosteric protein function, and drug discovery. Dr. Terry Kenakin on the web LinkedIn UNC Department of Pharmacology Amazon 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 >>

Retreat 2023 About Program Registration Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule Developing a PROTAC to Degrade the Constitutively Active Onco-GPCR in Uveal Melanoma Date & Time Friday, November 3rd / 4:20 PM About Victoria Rasmussen "Victoria Rasmussen is a graduate fellow in Dr. Thomas Sakmar’s laboratory at Rockefeller University, where she studies the signaling and degradation of G protein-coupled receptors. She completed her undergraduate education at Providence College, receiving a B.S. in Biology and a B.A. in Psychology. During her time at Providence College, she received the Walsh Grant Fellowship to develop novel methods of synthesizing 2-imidazoline scaffolds to be used as proteasome modulators in the laboratory of Travis Bethel. Victoria started her Ph.D. at the Tri-Institutional Ph.D. program in Chemical Biology, where she joined the lab of Thomas Sakmar at Rockefeller University. She is currently working to understand the signaling and degradation of GPCRs in disease states to help test the feasibility of using protein-targeted degradation as a therapeutic strategy. " Victoria Rasmussen on the web Tri-Institutional PhD Program Chemical Biology LinkedIn Dr. GPCR Previous Event Next Event Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec 22nd GPCR Retreat Sponsored by

Retreat 2023 About Program Registration Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule Atypical Structure and Function of Typical Chemokine Receptors Date & Time Saturday, November 4th / 11:00 AM Abstract Coming Soon About Amy Ramsey "One of the principal efforts of our laboratory is to understand the physiological consequences of NMDA receptor deficiency using genetic mouse models. The NMDA receptor is a subtype of glutamate neurotransmitter receptor that regulates the formation and maintenance of synaptic connections between neurons. It plays an important role in the way that neurons wire together and change the strength of synaptic connections with experience. Our laboratory is interested in the role of NMDA receptors not only on neurons, but also on other cells of the brain such as astrocytes, oligodendrocytes, and endothelial cells. NMDA receptors are implicated in a number of brain disorders including schizophrenia, autism, and epilepsy. Our laboratory has a long-standing interest in the way that NMDA receptors contribute to the symptoms of schizophrenia. Recently, we have focused our efforts on GRIN disorder. This is a rare neurodevelopmental disorder caused by de novo mutations in the GRIN genes that encode NMDA receptors. Although symptoms of GRIN disorder appear very early in childhood, it can take years to reach the right diagnosis through genetic tests. Children with GRIN disorder experience developmental delays, intellectual impairment, visual impairments, and difficulties with daily tasks like talking and walking, feeding and toileting. Many children experience seizures that can be life-threatening. Our laboratory is working to help patients by developing genetically-modified mice that have disease-causing variants in their Grin1 gene. These mice can then be used to test dietary regimens, drugs, and adenoviral gene therapies for their ability to improve specific symptoms. The Ramsey lab uses a combination of biochemical and behavioural approaches to understand the many roles of NMDA receptors and to find treatments for debilitating brain disorders." The Ramsey Lab Amy Ramsey on the web University of Toronto Pubmed Google Scholar LinkedIn Twitter Dr. GPCR Previous Event Next Event Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec 22nd GPCR Retreat Sponsored by

Retreat 2023 About Program Registration Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule Dopamine-Mediated Motor Recovery after Ischemic Stroke Date & Time Friday, November 3rd / 8:30 AM Abstract Coming Soon About Mario Tiberi "I did my graduate research on the regulation of axonal transport by tricyclic antidepressants (M.Sc.) and molecular pharmacology of opioid receptors (Ph.D.) in the Department of Pharmacology at the Université de Montréal under the mentorship of Dr. Pierre-André Lavoie and Dr. Jacques Magnan, respectively. I then pursued my postdoctoral training at Duke University in the laboratory of Dr. Marc Caron, where I cloned the dopamine D5 receptor gene and investigated the regulation of dopaminergic and adrenergic receptors. My addiction for dopamine led me to the Ottawa Hospital Research Institute (then the Moses and Rose Loeb Research Institute) to develop my independent research program. The Tiberi Lab pursues the study of the molecular, structural, pharmacological and signaling features of dopamine (DA) receptors. We are also currently developing the translational component of our research to capitalize on the druggability potential of GPCRs. More specifically, we investigate the druggability potential of new signaling partners we identified that drive the formation of different DA receptor complexes. We hope our research will aid in the development of new therapeutic interventions for the alleviation of L-DOPA-induced dyskinesia in Parkinson’s Disease and improvement of post-stroke recovery." Mario Tiberi on the web University of Ottawa Pubmed Google Scholar ResearchGate 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

Meet the Organizers behind the AGPCR24 Antony Boucard Jr, PhD Host and Organizer Cinvestav, Mexico City Yamina Berchiche, PhD Co-organizer Dr. GPCR, Boston Andreína Martín Website & Social Media Coordinator Dr. GPCR, Boston Ivanna Rey Executive Assistant Dr. GPCR, Boston

Retreat 2023 About Program Registration Logo Contest Committee Sponsors 22nd GPCR Retreat Fairmont Le Château Montebello, Québec, Canada November 2-4, 2023 We are pleased to welcome you at Le Château Montebello , the 22nd Annual Great Lakes G Protein-Coupled Receptor Retreat held jointly with the Club des Récepteurs à Sept Domaines Transmembranaires du Québec. The meeting will be held on Nov. 2-4, 2023 at the Chateau Montebello, Québec. The Chateau Montebello is an exceptional venue, and is located 1 hr from Ottawa, or 1.5 hr from Montreal in the beautiful Laurentian Mountains of Canada. The fall colors of the leaves are spectacular, and the weekend of science is an intense and interactive experience, and a great training environment for our students and post-doctoral fellows. The meeting is launched on Thursday with two Trainee Symposia and the Plenary Lecture, followed by 6 symposia on Friday and Saturday and the closing Keynote Lecture. The deadline for registration is September 21, 2023. For the 22nd edition, the Organizing Committee has again lived up to the expectations by putting together an outstanding program with a special thought for Marc Caron (1946-2022) to commemorate his great contributions to the GPCR and Neurosciences fields. Dr. Kathleen Caron of the University of North Carolina at Chapel Hill, unquestionably one of the pioneers involved in deciphering how receptor activity-modifying proteins or RAMPs regulate GPCR function, is confirmed as Plenary Speaker of the inaugural Marc G. Caron keynote lecture on November 2nd. Additionally, there will be a Marc G. Caron Honorary Symposium by Caron Lab alumni to honor his memory. We have also confirmed Dr. Arthur Christopoulos of Monash University in Australia, one of the pioneers in the medicinal chemistry, computational and mathematical modelling of GPCRs, as Plenary Speaker of the Hyman B. Niznik keynote lecture , which will close the conference. The program will include also world-class and diverse GPCR scientists working in the arenas of structure and signaling, neuroscience, cancer, translational and model systems. As in previous editions, trainees are more than welcome to this unique meeting. Indeed, for the Montebello 2023 edition, we have organized two trainee symposiums to acknowledge formally the participation of our graduate students and post-doctoral fellows. Additionally, each symposium of the GPCR Retreat 2023 will include one trainee short talk selected from abstracts. Trainees of diversity groups are strongly encouraged to register to the meeting and submit an abstract for consideration for the trainee symposia and selected trainee short talks. Your participation has already made this unique event a success. We are thrilled by the overwhelming interest in this event by the GPCR research community. We trust that the collegial and intimate atmosphere provided by Le Château Montebello will be suited for an environment where graduate students, postdoctoral fellows and principal investigators can have stimulating discussions and debates on GPCR research presented at this meeting. We would like to thank all our Sponsors for their ongoing generous support of the meeting. Without their support, this meeting will not be possible. If you have any suggestions or comments for either this Retreat or future meetings, we look forward to receiving your feedback. Finally, Bienvenue and we hope you will enjoy your stay in Montebello and find the Retreat stimulating and satisfying. Sincerely , The Organizing Committee 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. JoAnn Trejo About Dr. JoAnn Trejo Dr. JoAnn Trejo earned her Ph.D. at UC San Diego. She completed her postdoctoral fellowship at UC San Francisco under the guidance of Professor Shaun Coughlin where she worked on the newly discovered protease-activated GPCRs. Dr. Trejo joined the faculty in the Department of Pharmacology at the University of North Carolina in 2000 and then moved to UC San Diego School Medicine, Department of Pharmacology in 2008, where she quickly rose through the ranks to tenured professor in 2012. In 2014, she was appointed Vice-Chair of the Department of Pharmacology. The long-term goal of Dr. Trejo’s research program is to gain a thorough and mechanistic understanding of processes that control cell signaling by protease-activated receptors (PARs) and the impact on vascular inflammation and cancer progression. PARs are GPCRs that are activated through an atypical irreversible proteolytic mechanism. The precise control of PAR signaling is critical for proper temporal and spatial dynamics of signaling and appropriate cellular responses. Discovering new aspects of PAR signaling is important for increasing the fundamental knowledge of GPCR biology and for the identification of drug targets and future drug development. Dr. Trejo’s research has focused on PAR1, which has important functions in hemostasis, thrombosis, inflammation, and cancer and is an important drug target. She has made numerous important discoveries related to the mechanisms that control PAR1 signaling and closely related family members and published extensively on this topic. Dr. Trejo has been continuously funded by the NIH for >20 years and was a recipient of the prestigious American Heart Association Established Investigator Award. Her laboratory is the recognized expert on protease-activated receptors, particularly PAR1, and over the years she has discovered novel aspects of GPCR biology, acquired critical expertise, and rigorous approaches to examine PAR1 function using human cultured cells and mouse models. Dr. Trejo has presented her studies at 52 national/international meetings and 66 academic seminars across the U.S. Dr. JoAnn Trejo on the web UC San Diego Trejo Lab Wikipedia ​​​​LinkedIn Google Scholar Orcid Twitter UC San Diego School of Medicine 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 A virally encoded GPCR drives glioblastoma through feed-forward activation of the SK1-S1P1 signaling axis Published date August 15, 2023 Abstract "The G protein-coupled receptor (GPCR) US28 encoded by the human cytomegalovirus (HCMV) is associated with accelerated progression of glioblastomas, aggressive brain tumors with a generally poor prognosis. Here, we showed that US28 increased the malignancy of U251 glioblastoma cells by enhancing signaling mediated by sphingosine-1-phosphate (S1P), a bioactive lipid that stimulates oncogenic pathways in glioblastoma. US28 expression increased the abundance of the key components of the S1P signaling axis, including an enzyme that generates S1P [sphingosine kinase 1 (SK1)], an S1P receptor [S1P receptor 1 (S1P1)], and S1P itself. Enhanced S1P signaling promoted glioblastoma cell proliferation and survival by activating the kinases AKT and CHK1 and the transcriptional regulators cMYC and STAT3 and by increasing the abundance of cancerous inhibitor of PP2A (CIP2A), driving several feed-forward signaling loops. Inhibition of S1P signaling abrogated the proliferative and anti-apoptotic effects of US28. US28 also activated the S1P signaling axis in HCMV-infected cells. This study uncovers central roles for S1P and CIP2A in feed-forward signaling that contributes to the US28-mediated exacerbation of glioblastoma." Authors Nick D Bergkamp , Jeffrey R van Senten , Hendrik J Brink , Maarten P Bebelman , Jelle van den Bor , Tuğçe S Çobanoğlu , Kasper Dinkla , Johannes Köster , Gunnar Klau , Marco Siderius , Martine J Smit 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 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. Robert F. Bruns About Dr. Robert F. Bruns Fred Bruns discovered the first positive allosteric modulator (PAM) of a GPCR in the late 1980s while working at Warner-Lambert/Parke-Davis. The work was published in 1990. After 7 years at WL/PD and 26 years at Eli Lilly & Co., he retired at the end of 2014 and since then has been writing papers on his final major project at Lilly, a dopamine D1 PAM series that has advanced through Phase 2 clinical trials. Fred obtained an A.B. in Psychology from Washington University in St. Louis, followed by a Ph.D. in Neurosciences at the University of California, San Diego. His doctoral dissertation was the first large-scale study of structure-activity relationships for adenosine receptors. During a joint postdoc with John W Daly at NIH and Solomon Snyder at Johns Hopkins, he developed the first adenosine receptor binding assay. He then joined WL/PD, where his lab demonstrated the existence of two subtypes of the adenosine A2 receptor, A2a and A2b. In 1988, he joined Lilly as a receptor biologist in charge of a high-throughput screening lab. He taught himself chemoinformatics as a way to optimize compound selection for screening, and in 1997 switched to computational chemistry full-time. He supported the D1 PAM project in various roles from its inception in 2002 until selection of a clinical candidate in 2013. Dr. Bruns has over 80 publications and 11,000 citations, with an h-index of 47. Dr. Robert F. Bruns on the web ResearchGate 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. Katarina Nemec About Dr. Katarina Nemec " I am a pharmacist with an interest in systems pharmacology and precision medicine. Since my undergraduate studies, I have been engaged in researching molecular mechanisms that govern human (patho-)physiology and their interplay with drugs. I aim to discover new therapeutic approaches, and druggable molecules or refine canonical drug targets to create drugs with fewer adverse effects. I studied Pharmacy at the University in Ljubljana, Slovenia, and at the University of Bonn, Germany, working initially on the role of prostaglandin receptor EP4 in chronic lymphocytic leukemia. During my PhD studies in Martin Lohse lab at the Max Delbrueck Center in Berlin, I consolidated my knowledge of GPCRs pharmacology while performing various cell-based experiments to understand the binding, activation, and signaling of therapeutically relevant GPCRs. In addition, I generated various optical biosensors based on fluorescence or bioluminescence resonance energy transfer technologies (FRET, BRET) that were used for functional screens with state-of-the-art microscopy and high throughput screening to explain novel ways of GPCR modulation. I am continuing with the development of advanced screening approaches in the Madan Babu lab to progress in the understanding of spatiotemporal regulation of biased GPCR activation and signaling. I want to combine experimental approaches with data-driven discovery and adopt data science methodology to tackle relevant scientific questions on the systems pharmacology level. " Dr. Katarina Nemec on the web Babu Lab ResearchGate Google Scholar ORCID LinkedIn Twitter 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 >>

Ecosystem Contributor - Coming Soon -

< GPCR News < GPCRs in Oncology and Immunology Observational Study of Repeat Immunoadsorption (RIA) in Post-COVID ME/CFS Patients with Elevated ß2-Adrenergic Receptor Autoantibodies-An Interim Report Published date October 9, 2023 Abstract "There is increasing evidence for an autoimmune aetiology in post-infectious Myalgic Encephalomyelitis/Chronic Fatigue Syndrome (ME/CFS). SARS-CoV-2 has now become the main trigger for ME/CFS. We have already conducted two small proof-of-concept studies on IgG depletion by immunoadsorption (IA) in post-infectious ME/CFS, which showed efficacy in most patients. This observational study aims to evaluate the efficacy of IA in patients with post-COVID-19 ME/CFS. The primary objective was to assess the improvement in functional ability. Due to the urgency of finding therapies for post-COVID-Syndrome (PCS), we report here the interim results of the first ten patients, with seven responders defined by an increase of between 10 and 35 points in the Short-Form 36 Physical Function (SF36-PF) at week four after IA. The results of this observational study will provide the basis for patient selection for a randomised controlled trial (RCT), including sham apheresis, and for an RCT combining IA with B-cell depletion therapy. Trial registration number: NCT05629988." Authors Elisa Stein , Cornelia Heindrich , Kirsten Wittke , Claudia Kedor , Laura Kim , Helma Freitag , Anne Krüger , Markus Tölle , Carmen Scheibenbogen Tags GPCR-antibodies , Myalgic Encephalomyelitis/Chronic Fatigue Syndrome , SF-36 , autoantibodies , immunoadsorption , long COVID , physical function , post-COVID syndrome 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. Antonella Di Pizio About this episode In this episode of the Dr. GPCR podcast , we meet with Dr. Antonella Di Pizio, an independent research group leader at the Leibniz Institute for Food Systems Biology at the Technical University of Munich. Antonella trained as a medicinal chemist in Italy, followed by a Ph.D. in computational medicinal chemistry, during which she developed a taste for structural biology. Antonella then moved to Israel, where she first started working on bitter taste GPCRs in Dr. Masha Niv's lab . Today, Antonella has expanded her research to olfactory GPCRs and trace amine receptors. Join us to learn more about chemosensory GPCRs and how computational pharmacology can help better understand their function. Dr. Antonella Di Pizio on the web Leibniz-Institute for Food Systems Biology at the Technical University of Munich Google Scholar PubMed LinkedIn Dr. GPCR Ecosystem Thanks for listening to this podcast episode This short survey will help us understand your needs to bring you exciting and informative content; this short survey should take 5 minutes to fill. Listen and subscribe to where you get your podcasts. << Previous Podcast Episode Next Podcast Episode >>

Retreat 2023 About Program Registration Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule Coffee Break 5 Date & Time Saturday, November 4th / 9:55 AM Previous Event Next Event Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec 22nd GPCR Retreat Sponsored by

Retreat 2023 About Program Registration Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule Using food perception and bioamine signaling networks to slow aging Date & Time Saturday, November 4th / 10:10 AM Abstract Coming Soon Authors and Affiliations Hillary A. Miller 1, Shijiao Huang 1, Elizabeth S. Dean 1, and Scott F. Leiser 1 1. University of Michigan About Scott Leiser "Scott Leiser is an Assistant Professor in the Research in the Molecular & Integrative Physiology Department at the University of Michigan. The Leiser laboratory is focused on the molecular mechanisms of aging, with an emphasis on stress response and metabolism. The lab works with multiple models, including Caenorhabditis elegans, in vitro tissue culture, and mice, to better understand the conserved mechanisms of aging. Recent research in his laboratory focuses on how organisms perceive and respond to environmental stress though cell non autonomous signaling mechanisms, and how these signals affect the health and longevity of the animal." Scott Leiser on the web University of Michigan Pubmed ResearchGate 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

Dr. GPCR Podcast << Back to podcast list Dr. J. Silvio Gutkind About this episode Have you had moments that defined your scientific tastes? For Dr. J Silvio Gutkind, a class on oncogenes and his interests for GPCRs helped shape his scientific interests. These took him from the University of Buenos Aires in Argentina to UC San Diego and through the National Institutes of Health in Bethesda, Maryland. In this episode, Silvio discusses G protein signaling in the context of cancer, immunotherapies, and combination therapies that could help improve patients’ lives. Dr. J. Silvio Gutkind on the web Dr. J Silvio Gutkind on LinkedIn Gutkind Lab – UC San Diego Moores Cancer Center Gutkind Lab publications Gutkind Lab on Pubmed Gutkind Lab on Twitter UCSD Moores Cancer Center 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 GprC of the nematode-trapping fungus Arthrobotrys flagrans activates mitochondria and reprograms fungal cells for nematode hunting Published date June 14, 2024 Abstract "Initiation of development requires differential gene expression and metabolic adaptations. Here we show in the nematode-trapping fungus, Arthrobotrys flagrans, that both are achieved through a dual-function G-protein-coupled receptor (GPCR). A. flagrans develops adhesive traps and recognizes its prey, Caenorhabditis elegans, through nematode-specific pheromones (ascarosides). Gene-expression analyses revealed that ascarosides activate the fungal GPCR, GprC, at the plasma membrane and together with the G-protein alpha subunit GasA, reprograms the cell. However, GprC and GasA also reside in mitochondria and boost respiration. This dual localization of GprC in A. flagrans resembles the localization of the cannabinoid receptor CB1 in humans. The C. elegans ascaroside-sensing GPCR, SRBC66 and GPCRs of many fungi are also predicted for dual localization, suggesting broad evolutionary conservation. An SRBC64/66-GprC chimaeric protein was functional in A. flagrans, and C. elegans SRBC64/66 and DAF38 share ascaroside-binding sites with the fungal GprC receptor, suggesting 400-million-year convergent evolution." Authors Xiaodi Hu, David S Hoffmann, Mai Wang, Lars Schuhmacher, Maria C Stroe, Birgit Schreckenberger, Marcus Elstner, Reinhard Fischer 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 >

Principles of Pharmacology in Drug Discovery I Techniques for Effective Lead Optimization of Candidate Molecules Dr. Terry Kenakin Techniques for Effective Lead Optimization of Candidate Molecules GPCRs have been and arguably still are the most prolific and fertile therapeutic drug targets; this course describes the essential pharmacologic techniques and knowledge required to create a GPCR Target Program aimed at the discovery of new Drugs. The course will focus on the methods used to quantify GPCR ligand activity (agonists, antagonists, modulators) and the process of characterizing the mechanism of action of ligands to enable the prediction of activity in vivo systems. In general, registrants will receive a comprehensive understanding of the unique science of pharmacology and how it can describe drug action in system-independent ways. Registrants will learn: Essentials of measuring pharmacologic activity of ligands (affinity, efficacy, co-operativity). Application of this knowledge to determine the mechanism of action of new GPCR ligands. The required elements of a comprehensive and effective GPCR Discovery. Modules: October 3rd: GPCR Project Initiation and Design for Discovery of New Molecules. October 10th: Drug Affinity: Measurement of Antagonism (Binding and Function) / Classifying Antagonists. October 17th: Agonists and Efficacy: A New World of GPCR Efficacies / Biased Signaling. October 24th: Allosteric Modulators: NAMs, PAMs, Special Properties, Methods to quantify the allosteric effect. Registrations start on Monday, July 15th, 2024. Classes will be live from Zoom on Thursdays from 10 am to 11:30 am EST. Sessions will include a 1-hour live lecture plus 30 minutes of Q&A. Participants who complete the course will get an online certification signed by the professor and the Dr.GPCR Team. A splendid time is guaranteed for all. What are the main objectives of the course? To help registrants understand the value of Pharmacology in the drug discovery process. What will students gain from taking this course? Students will gain an understanding of how pharmacology can greatly extend the ability to predict a candidate's therapeutic value in a range of different physiological conditions. Are there any specific textbooks or readings students should be aware of? Pharmacology in Drug Discovery and Development (3rd ed.) T.P. Kenakin, Elsevier 2024 or 'A Pharmacology Primer' (6th ed.) T.P. Kenakin, Elsevier, 2022. Principles of Pharmacology I $450 $ 450 ​ +$13.50 Transaction fee Techniques for Effective Lead Optimization of Candidate Molecules Valid for 6 months Select Register today Become a Premium Member and enjoy Early-Bird pricing in Principles of Pharmacology II before Friday, September 27th To register as a team , one of you must be a Premium Member . This person must email hello@drgpcr.com indicating how many people will register for the course, the names of the participants, and their emails. What would you like to learn today?

Dr. GPCR Podcast << Back to podcast list Dr. Josh Pottel About Dr. Josh Pottel "I lead Molecular Forecaster Inc. (MFI): a reliable, self-sustaining computational chemistry service provider, developing its own software for application in various drug discovery campaigns. I have extensive training in computer-aided drug design. I completed my PhD at McGill University in the lab of Prof. Nicolas Moitessier, and went on to a postdoc with Prof. Brian Shoichet at UCSF. While in San Francisco, I completed Startup101 - a course a offered by the entrepreneurship center. I am now combining my training as a chemist and as an entrepreneur to grow a sustainable service and software provider in drug discovery. More broadly, I hope to be a critical contributor to a growing Canadian biotech sector in both scientific research and fostering entrepreneurship." Dr. Josh Pottel on the web Molecular Forecaster LinkedIn BlueSky Google Scholar Twitter 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 Biochemical Mechanisms Underlying Location Bias in GPCR Signaling Date & Time Saturday, November 4th / 8:40 AM Abstract Coming Soon About Sudarshan Rajagopal "Dr. Sudarshan Rajagopal is a physician-scientist and is currently an Associate Professor of Medicine and Biochemistry at Duke University School of Medicine. He obtained his B.S. in Chemistry from The University of Chicago in 1998 and subsequently enrolled in the Medical Scientist Training Program at The University of Chicago. During his doctoral work in the lab of Prof. Keith Moffat, he studied the structural mechanisms of bacterial photoreceptors using time-resolved Laue crystallography. He was awarded his PhD in 2004 and his MD in 2006. He then joined the Internal Medicine Residency training program at Duke University Medical Center. During his Cardiology fellowship, he trained in the lab of Dr. Robert J. Lefkowitz, where his research focused on biased agonism, with the development of approaches to quantify ligand bias and the identification of ACKR3 as an endogenously beta-arrestin-biased receptor. After completing his training, he joined the faculty at Duke, with a focus on the mechanisms underlying biased agonism at GPCRs and its contribution inflammation and cardiovascular disease. His group and others have shown that many of these ligands act as biased agonists for the same receptor. His lab is also interested in identifying novel signal transduction mechanisms of GPCRs, such as the formation of complexes between G proteins and beta-arrestins. His clinical focus is on pulmonary arterial hypertension, a disease of the pulmonary arterioles that causes right heart failure, and he serves as co-director of the Duke Pulmonary Vascular Disease Center." Sudarshan Rajagopal on the web The Rajagopal Lab Google Scholar Pubmed LinkedIn Dr. GPCR Previous Event Next Event Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec 22nd GPCR Retreat Sponsored by

Dr. GPCR Podcast << Back to podcast list Dr. Kari Johnson About this episode Dr. Kari Johnson is currently an assistant professor at the Uniformed Services University of the Health Sciences in Bethesda, Maryland. She is a neuropharmacologist with an interest in the long-term effects of alcohol abuse on neural circuits. Kari completed her Ph.D. in Pharmacology at Vanderbilt University before continuing her training as a postdoctoral fellow at the Vanderbilt Center for Neuroscience Drug Discovery, the National Institute of General Medical Sciences, and the National Institute on Alcohol Abuse and Alcoholism. All through her career, the recurring theme in Kari’s work has been GPCRs and more specifically Metabotropic Glutamate Receptors. Join me and learn more about how Kari studies GPCRs in basal ganglia circuits following chronic alcohol exposure in mice. Dr. Kari Johnson on the web LinkedIn Google Scholar Research Gate USU Twitter 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 Removing the GPCR-mediated brake on exocytosis enhances insulin action, promotes adipocyte browning, and protects against diet-induced obesity Date & Time Friday, November 3rd / 2:45 PM Abstract Coming Soon Authors and Affiliations Ryan P. Ceddia 1, *, Zack Zurawski 2,3,*, Analisa Thompson Gray 2, Feyisayo Adegboye 2, Ainsley McDonald-Boyer 3, Fubiao Shi 1, Dianxin Liu 1, Jose Maldonado 5, Jiesi Feng 4, Yulong Li 4, Simon Alford 5, Julio E. Ayala 5, Owen P. McGuinness 5, Sheila Collins 1,5, Heidi E. Hamm 2 1 Department of Medicine, Division of Cardiovascular Medicine, Vanderbilt University Medical Center, Nashville, TN 37232, USA 2 Department of Pharmacology, Vanderbilt University, Nashville, TN 37232, USA 3, 5 Department of Molecular Physiology and Biophysics, Vanderbilt University, Nashville, TN 37232, USA 4 Peking University, China 5 Department of Anatomy and Cell Biology, University of Illinois at Chicago, Chicago, IL 60612, USA. About Heidi Hamm "Heidi E. Hamm, Ph.D. is the Aileen M. Lange and Annie Mary Lyle Chair in Cardiovascular Research, and Professor of Pharmacology, Ophthalmology and Visual Sciences, and Orthopedics at Vanderbilt University. This is one of the top Pharmacology departments in the country, judged by reputation, citation analysis, and NIH funding. She oversaw an increase of the size of the Department, as well as a quintupling of its NIH funding, in her 14 years as Chair. The Department’s strengths lie in GPCR signal transduction and neuroscience, and she has expanded it in the areas of drug discovery and structural biology of membrane proteins. Her research focuses on the structure and function of GTP binding proteins and the molecular mechanisms of signal transduction. Her laboratory has been involved in studying G protein coupled signal transduction for many years and has made key discoveries in G protein structure and mechanisms of activation by GPCRs and activation of effectors. Current areas of interest include Protease Activated Receptor signaling in the cardiovascular system and regulation of vesicular exocytosis mediated by Gi/o-coupled receptors by G subunit binding to SNAREs. Dr. Hamm obtained her Ph.D. in 1980 from the Department of Zoology at the University of Texas-Austin and did postdoctoral training in the University of Wisconsin-Madison from 1980-1983. Her initial research centered around circadian clocks and melatonin synthesis in the avian retina; her postdoctoral work investigated the role of the G protein transducin in visual transduction using blocking monoclonal antibodies. She held faculty appointments at the University of Illinois at Chicago School of Medicine and Northwestern University before moving to Vanderbilt in 2000. She has received numerous awards, including the Glaxo Cardiovascular Discovery Award, the Distinguished Investigator Award from the National Alliance for Research in Schizophrenia and Depression, the Faculty of the Year award from the University of Illinois College of Medicine, and the Stanley Cohen Award “For Research Bringing Diverse Disciplines, such as Chemistry or Physics, to Solving Biology’s Most Important Fundamental Problems” from Vanderbilt University in 2003. She gave the Fritz Lipmann Lecture at ASBMB in 2001. " Heidi Hamm on the web The Hamm Lab Vanderbilt School of Medicine Pubmed Google Scholar LinkedIn 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 >>

Retreat 2023 About Program Registration Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule Welcome Remarks Date & Time Thursday, November 2nd / 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