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Home → Flash News → Ever wondered how we perceive bitterness? 👅🔬 Researchers have unveiled the cryo-EM structure of TAS2R14, the most promiscuous bitter taste receptor, bound to the drug flufenamic acid (FFA) and its signaling partner gustducin! 🌟 This discovery reveals an unusual dual binding mode of FFA and offers tools for site-targeted compound design. 🧪✨ Learn more about this exciting breakthrough in bitter taste signaling. Published on December 5, 2024 Category GPCR Weekly News Ever wondered how we perceive bitterness? 👅🔬 Researchers have unveiled the cryo-EM structure of TAS2R14 , the most promiscuous bitter taste receptor, bound to the drug flufenamic acid (FFA) and its signaling partner gustducin! 🌟 This discovery reveals an unusual dual binding mode of FFA and offers tools for site-targeted compound design . 🧪✨ Learn more about this exciting breakthrough in bitter taste signaling. ➡️ https://www.ecosystem.drgpcr.com/receptor-activation-and-signaling/a-bitter-anti-inflammatory-drug-binds-at-two-distinct-sites-of-a-human-bitter-taste-gpcr?utm_campaign=5d751e7a-3ecb-4719-8ba3-974d17e9f596&utm_source=so&utm_medium=mail&cid=79a6b35e-7ba6-44a0-863b-0842f5a5cfd3 #gpcr #drgpcr #bittertaste Previous Next Recent Articles Why Biotech Fundraising Fails Due to Intellectual Property Gaps 👉 Why has intellectual property become a first-order fundraising signal? Biotech fundraising has undergone a subtle yet significant shift. Capital still exists, but investors are making decisions earlier and filtering more carefully . As a result, intellectual property is no longer something that comes up late in the process. 👉 It has become an early signal of whether a biotech company is fundable at all. This shift does not mean founders need more patents or heavier legal Attila Foris 5 days ago The Hidden Operating Cadence That’s Actually Driving Your Biotech Founders love the idea that a new year, or a new quarter, will reset the company. But here’s the uncomfortable truth: 👉 Your biotech is already running on an operating cadence you didn’t consciously design. And that cadence is shaping everything: timelines, decisions, investor calls, BD traction, internal focus. Most CEOs think they’re steering the strategy. 👉 In reality, their operating cadence is steering them. And until you see it, you can’t change it. Operating cadence Attila Foris Dec 24, 2025 GPCR Binding Affinity Experiments: Interpreting Data With Confidence as We Head Into 2026 As scientists, we know curves don’t equal clarity. As 2025 comes to a close, this final edition of Weekly News focuses on how GPCR binding affinity experiments are interpreted—and how those interpretations quietly shape SAR, lead selection, and development timelines long before anyone notices. The goal isn’t more data. It’s cleaner interpretation. And that’s exactly what carries strong discovery programs into 2026. Dr. GPCR News Dec 18, 2025 Scientific Isolation: The Real Reason Early Biotechs Lose Traction The Quiet Drift You Don’t Feel Until It’s Too Late 👉 Every early-stage biotech reaches a moment where the science finally starts clicking… and the company quietly stops doing anything else. BD conversations stay warm but motionless. Investor updates become thinner. Internal meetings slowly morph into scientific colloquia instead of decision-making forums. 👉 The uncomfortable truth: your company is doing a lot of science and very little building. No drama. No blow-ups.Just Attila Foris Dec 17, 2025 Orthosteric Binding Experiments: How to Avoid the Most Common Data Pitfalls Binding affinity appears straightforward: add ligand, measure signal, fit a curve. Yet discovery teams routinely lose time and misallocate resources because the underlying biology behaves nothing like the idealized systems we learned in textbooks. GPCRs couple, decouple, isomerize, deplete tracers, and shift apparent affinity depending on stoichiometry and time. The result is a recurring pattern across programs—clean data that is not actually telling the truth. Orthosteric bi Terry's Desk Dec 16, 2025

Home → Flash News → Did you know registrations are already open for all our 2025 Dr.GPCR University Courses? Check out what you can learn this year from the master, Dr. Terry Kenakin 😉and save your spot soon! Remember Premium Members get a 25% discount 🙌 ✳️Click here and start your next learning experience https://www.ecosystem.drgpcr.com/gpcr-courses #gpcr #drgpcr Published on February 18, 2025 Category GPCR Weekly News Did you know registrations are already open for all our 2025 Dr.GPCR University Courses? Check out what you can learn this year from the master, Dr. Terry Kenakin 😉and save your spot soon! Remember Premium Members get a 25% discount 🙌 ✳️ Click here and start your next learning experience https://www.ecosystem.drgpcr.com/gpcr-courses #gpcr #drgpcr Previous Next Recent Articles Why Biotech Fundraising Fails Due to Intellectual Property Gaps 👉 Why has intellectual property become a first-order fundraising signal? Biotech fundraising has undergone a subtle yet significant shift. Capital still exists, but investors are making decisions earlier and filtering more carefully . As a result, intellectual property is no longer something that comes up late in the process. 👉 It has become an early signal of whether a biotech company is fundable at all. This shift does not mean founders need more patents or heavier legal Attila Foris 5 days ago The Hidden Operating Cadence That’s Actually Driving Your Biotech Founders love the idea that a new year, or a new quarter, will reset the company. But here’s the uncomfortable truth: 👉 Your biotech is already running on an operating cadence you didn’t consciously design. And that cadence is shaping everything: timelines, decisions, investor calls, BD traction, internal focus. Most CEOs think they’re steering the strategy. 👉 In reality, their operating cadence is steering them. And until you see it, you can’t change it. Operating cadence Attila Foris Dec 24, 2025 GPCR Binding Affinity Experiments: Interpreting Data With Confidence as We Head Into 2026 As scientists, we know curves don’t equal clarity. As 2025 comes to a close, this final edition of Weekly News focuses on how GPCR binding affinity experiments are interpreted—and how those interpretations quietly shape SAR, lead selection, and development timelines long before anyone notices. The goal isn’t more data. It’s cleaner interpretation. And that’s exactly what carries strong discovery programs into 2026. Dr. GPCR News Dec 18, 2025 Scientific Isolation: The Real Reason Early Biotechs Lose Traction The Quiet Drift You Don’t Feel Until It’s Too Late 👉 Every early-stage biotech reaches a moment where the science finally starts clicking… and the company quietly stops doing anything else. BD conversations stay warm but motionless. Investor updates become thinner. Internal meetings slowly morph into scientific colloquia instead of decision-making forums. 👉 The uncomfortable truth: your company is doing a lot of science and very little building. No drama. No blow-ups.Just Attila Foris Dec 17, 2025 Orthosteric Binding Experiments: How to Avoid the Most Common Data Pitfalls Binding affinity appears straightforward: add ligand, measure signal, fit a curve. Yet discovery teams routinely lose time and misallocate resources because the underlying biology behaves nothing like the idealized systems we learned in textbooks. GPCRs couple, decouple, isomerize, deplete tracers, and shift apparent affinity depending on stoichiometry and time. The result is a recurring pattern across programs—clean data that is not actually telling the truth. Orthosteric bi Terry's Desk Dec 16, 2025

Home → Flash News → Check out the latest GPCR news in the Ecosystem today! You’ll need to register but don’t worry, it’s Free! Cutting-edge cryo-EM reveals how LYCHOS, a lysosomal protein, senses cholesterol to regulate metabolism and cell growth ➡️https://www.ecosystem.drgpcr.com/structural-and-molecular-insights-into-gpcr-function/cryo-em-reveals-cholesterol-binding-in-the-lysosomal-gpcr-like-protein-lychos #gpcr #drgpcr Published on February 4, 2025 Category GPCR Weekly News Check out the latest GPCR news in the Ecosystem today! You’ll need to register but don’t worry, it’s Free! Cutting-edge cryo-EM reveals how LYCHOS, a lysosomal protein, senses cholesterol to regulate metabolism and cell growth ➡️ https:// www.ecosystem.drgpcr.com/structural-and-molecular-insights-into-gpcr-function/cryo-em-reveals-cholesterol-binding-in-the-lysosomal-gpcr-like-protein-lychos #gpcr #drgpcr Previous Next Recent Articles

Home → Flash News → Behind every great discovery is a great question 🚀 Dr. Dmitry Veprintsev shares how asking the right GPCR questions and dreaming big have shaped his work, in the latest Dr. GPCR podcast episode. If you’re passionate about GPCRs and drug discovery, this episode is a must-listen! ✳️Listen at Ep 163 with Dr. Dmitry Veprintsev #DrGPCR #GPCRPodcast #Biotech #Pharmacology #GPCRScience Published on April 10, 2025 Category Dr. GPCR Podcast Behind every great discovery is a great question 🚀 Dr. Dmitry Veprintsev shares how asking the right GPCR questions and dreaming big have shaped his work, in the latest Dr. GPCR podcast episode. If you’re passionate about GPCRs and drug discovery, this episode is a must-listen! ✳️Listen at Ep 163 with Dr. Dmitry Veprintsev #DrGPCR #GPCRPodcast #Biotech #Pharmacology #GPCRScience Previous Next Recent Articles

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

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

Every receptor tells a story but GPCRs speak a language of organization. Dr. Michelle Halls unpacks how GPCR signaling isn’t just about ligand–receptor interaction. Home → Flash News → Every receptor tells a story Every receptor tells a story Published on November 11, 2025 Category Dr.GPCR Podcast Every receptor tells a story — but GPCRs speak a language of organization. Dr. Michelle Halls unpacks how GPCR signaling isn’t just about ligand–receptor interaction. It’s about where and how signaling happens — spatially confined microdomains, scaffolding proteins, and preassembled complexes that fine-tune the cell’s response. This level of organization defines specificity in signaling, and understanding it changes how we think about drug targeting and disease mechanisms. It’s a moment that reframes GPCR biology from static pathways to dynamic, organized systems — where complexity is the key to precision. 🎧 Watch this moment from our conversation, then listen to the full episode on leadership, luck, and GPCR signaling: 👉 https://www.ecosystem.drgpcr.com/dr-gpcr-podcast/leadership-luck-and-gpcr-signaling #GPCR #DrGPCR Previous Next Recent Articles

Discover how organizations in the GPCR field can leverage the Dr. GPCR Ecosystem to enhance their impact. Learn more about the benefits today! Become Dr. GPCR Strategic Partner Request Your Quote How Organizations can benefit from Dr. GPCR Ecosystem? Company Page Create your company page today and share who you are with the Ecosystem Discover Product Listings Add your company's GPCR products here today! Discover Learning Center Do you have protocols, posters, white papers or an interactive course? Share it here! Discover Service Listings Do you offer services? List them here Discover Events Going to an event? Let the Ecosystem know and meet your customers at these events Discover Job Listings Looking to hire a GPCR scientist? Share your job description here today Discover Request Your Quote Learn more Company Page Your company gets to create a searchable company page highlighting products, services and any resources you think will benefit the Ecosystem and its members Discover Learning Center This space is great to share any resources you've already created or plan on creating to showcase your company products and help your customers use the technology effectively Discover Events Meet your customers and members of the Ecosystem by letting them know when and where your company is going to events Discover Product Listings Get your products in front of your GPCR customers, answer any questions they may have and get direct and live feedback. You'll only have to answer the same question once here but have the entire Ecosystem benefit Discover Service Listings List the services you offer and answer any questions customers may have directly. This will help you and members find answers to their questions faster and you'll only have to answer the same question once Discover Job Listings There is no better place to find a GPCR scientist for your team than the Dr. GPCR Ecosystem. Post you job description and since this is a closed Ecosystem, you can (if you'd like) share the contact information of anyone at your company such as the hiring manager Discover Sign Up

Retreat 2023 About Program Registration Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule Targeting adenosine signaling for immuno-oncology Date & Time Friday, November 3rd / 4:35 PM Abstract "Adenosine (ADO) signaling through A2A and A2B G protein-coupled receptors is increasingly recognized as an important immune checkpoint in the generation of anti-tumor immunity. Potent inhibitors of ADO signaling are currently being tested in cancer patients, including in randomized Phase 3 trial. I will present our recent work on adenosine-producing ectonucleotidases and adenosine signaling and discuss unexpected links between the adenosinergic pathway, DNA damage response and metabolic regulation." Authors and Affiliations John Stagg , David Allard . Centre de Recherche du Centre Hospitalier de l'Université de Montréal; Faculté de Pharmacie. 900 St-Denis, Montréal, QC, H2X 0A9. About John Stagg "John Stagg is a Professor of Pharmacy at Université de Montréal and researcher at the CHUM Research Centre. Distinguished immunologist, Dr Stagg is recognized for having identified the adenosine-producing enzyme CD73 as a new cancer target, and for his translational work in immuno-oncology. Dr Stagg has served as an expert consultant in the development of adenosine-targeting drugs, several of which now in clinical trials. Dr Stagg is a member of the Board of Directors of BioCanRx, Canada's Immunotherapy Network, co-founder and permanent member of the Scientific Advisory Board (SAB) of Surface Oncology, a clinical stage company developing next generation immunotherapies, and member of the SAB of Domain Therapeutics, a biopharmaceutical company focused on GPCR in immuno-oncology." John Stagg on the web University of Montréal Québec Cancer Consortium The University of Montreal Hospital Research Centre 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

Retreat 2023 About Program Registration Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule Check In Date & Time Thursday, November 2nd / 4:00 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

Home → Flash News → 🎯 Crack the code of GPCR ligand development! In case you haven’t heard, Dr. Terry Kenakin is hosting a 4-week course on GPCR drug development—and registration closes in 3 days! ⚠️ What you’ll learn: ✅ Drug absorption, metabolism & clearance ✅ PK-PD modeling & therapeutic profiles ✅ Early safety assessments & toxicity risks 📌 Limited spots—sign up before March 18th! 👉 Development of GPCR Ligands as Therapeutic Drugs | Dr. GPCR Ecosystem #GPCR #DrGPCR #Pharma #Biotech #Research Published on March 15, 2025 Category Dr. GPCR Courses 🎯 Crack the code of GPCR ligand development! In case you haven’t heard, Dr. Terry Kenakin is hosting a 4-week course on GPCR drug development —and registration closes in 3 days! ⚠️ What you’ll learn: ✅ Drug absorption, metabolism & clearance✅ PK-PD modeling & therapeutic profiles✅ Early safety assessments & toxicity risks 📌 Limited spots—sign up before March 18th! 👉 Development of GPCR Ligands as Therapeutic Drugs | Dr. GPCR Ecosystem #GPCR #DrGPCR #Pharma #Biotech #Research Previous Next Recent Articles

Home → Flash News → 🚨 Exciting Opportunity for Professionals in Drug Development! 🚨 Register today for a one-of-a-kind online course at Dr. GPCR University: "Development of GPCR Ligands as Therapeutic Drugs." 🗓 Dates: March 20 - April 10, 2025 ⏰ Time: Thursdays, 10:00 AM - 11:30 AM (EST) This advanced course is essential for anyone working in drug development and focuses on: The essentials of new drug development Key pharmacokinetic elements (absorption, distribution, clearance) Hepatic metabolism and the Cytochrome P450 system Drug safety and toxicology (including drug-drug interactions) And much more! Gain deep insights into GPCR drug candidates and learn the critical assays and techniques required to bring therapeutic molecules to life. 🚨 Only 25 spots available — register now! 💡 This is a great opportunity for both academia and industry professionals. Sessions will be live, and you’ll also have 1:1 discussion time with the instructor. Full PDFs of the slides will be available! 🔗 https://buff.ly/lVEcRUc #GPCR #DrugDevelopment #Pharmacokinetics #TherapeuticDrugs #OnlineCourse #DrGPCRUniversity #PharmaceuticalIndustry Published on March 12, 2025 Category Dr. GPCR Courses 🚨 Exciting Opportunity for Professionals in Drug Development! 🚨 Register today for a one-of-a-kind online course at Dr. GPCR University: "Development of GPCR Ligands as Therapeutic Drugs." 🗓 Dates: March 20 - April 10, 2025 ⏰ Time: Thursdays, 10:00 AM - 11:30 AM (EST) This advanced course is essential for anyone working in drug development and focuses on: The essentials of new drug development Key pharmacokinetic elements (absorption, distribution, clearance) Hepatic metabolism and the Cytochrome P450 system Drug safety and toxicology (including drug-drug interactions) And much more! Gain deep insights into GPCR drug candidates and learn the critical assays and techniques required to bring therapeutic molecules to life. 🚨 Only 25 spots available — register now! 💡 This is a great opportunity for both academia and industry professionals. Sessions will be live, and you’ll also have 1:1 discussion time with the instructor. Full PDFs of the slides will be available! 🔗 https://buff.ly/lVEcRUc #GPCR #DrugDevelopment #Pharmacokinetics #TherapeuticDrugs #OnlineCourse #DrGPCRUniversity #PharmaceuticalIndustry Previous Next Recent Articles

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

Retreat 2023 About Program Registration Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule A positive Allosteric Modulator of M1 Acetylcholine Receptors Improves Cognitive Deficits in Male and Female Alzheimer’s Mice Date & Time Friday, November 3rd / 1:55 PM About Khaled Abdelrahman Dr. Khaled Abdelrahman graduated in 2006 with a BSc in Pharmaceutical Sciences from Alexandria University (Egypt) followed by MSc in Pharmacology in the same university that was conferred in 2009. He joined the laboratory of Dr. William Cole at the University of Calgary in 2010 for his Ph.D. where he studied the molecular basis underlying altered cerebrovascular function and blood flow in type 2 diabetes. In 2015, He joined Dr. Stephen Ferguson’s laboratory in the Departments of Cellular & Molecular Medicine and Neuroscience at the University of Ottawa as a Postdoctoral Fellow to explore novel G protein-coupled receptor (GPCR) candidates that can be targeted pharmacologically to slow neurodegeneration. He has been also studying what aspects of GPCR signaling are regulated in a sex-selective manner and how this can influence drug discovery in the area of neurodegenerative diseases. He is also a Registered Pharmacist in Canada and held two of the most prestigious Clinician Postdoctoral Fellowships offered by Alberta Innovates and Canadian Institutes of Health Research. He received the Canadian Society of Pharmacology and Therapeutics Postdoctoral and Publication awards along with many Young Scientist Awards from the American Society for Pharmacology and Experimental Therapeutics. Khaled Abdelrahman on the web University of British Columbia Twitter PubMed Google Scholar 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

Home → Flash News → Exploring the combination of molecular simulation, pharmacological assays, and NMR to reveal the molecular mechanism of biased activation at the vasopressin V2 receptor. Did you know that we work hard to bring you the most recent GPCR News, weekly? Catch up today in the Ecosystem using your free site membership! Published on December 10, 2024 Category GPCR Weekly News Exploring the combination of molecular simulation, pharmacological assays, and NMR to reveal the molecular mechanism of biased activation at the vasopressin V2 receptor. Did you know that we work hard to bring you the most recent GPCR News, weekly? Catch up today in the Ecosystem using your free site membership! ➡️ https://www.ecosystem.drgpcr.com/receptor-activation-and-signaling/high-affinity-elr%2B-chemokine-ligands-show-g-protein-bias-over-%CE%B2-arrestin-recruitment-and-receptor-internalization-in-cxcr1-signalling #gpcr #drgpcr Previous Next Recent Articles

Home → Flash News → Can we preserve opioid pain relief without the side effects? 🔬 On Ep.166 of the Dr.GPCR Podcast, Ben Clements shares how positive allosteric modulators (PAMs) at the mu-opioid receptor could revolutionize treatment —with a 10x boost in methadone efficacy. Tune in for a masterclass on translational pharmacology, curiosity-driven science, and meaningful mentorship. 🎧 Full episode: Ep 166 with Dr. Ben Clements #GPCRresearch #DrGPCR #GPCRpodcast #OpioidPharmacology #DrugDiscovery Published on May 15, 2025 Category Dr. GPCR Podcast Can we preserve opioid pain relief without the side effects? 🔬 On Ep.166 of the Dr.GPCR Podcast, Ben Clements shares how positive allosteric modulators (PAMs) at the mu-opioid receptor could revolutionize treatment —with a 10x boost in methadone efficacy. Tune in for a masterclass on translational pharmacology, curiosity-driven science, and meaningful mentorship. 🎧 Full episode: Ep 166 with Dr. Ben Clements #GPCRresearch #DrGPCR #GPCRpodcast #OpioidPharmacology #DrugDiscovery Previous Next Recent Articles Why Biotech Fundraising Fails Due to Intellectual Property Gaps 👉 Why has intellectual property become a first-order fundraising signal? Biotech fundraising has undergone a subtle yet significant shift. Capital still exists, but investors are making decisions earlier and filtering more carefully . As a result, intellectual property is no longer something that comes up late in the process. 👉 It has become an early signal of whether a biotech company is fundable at all. This shift does not mean founders need more patents or heavier legal Attila Foris 5 days ago The Hidden Operating Cadence That’s Actually Driving Your Biotech Founders love the idea that a new year, or a new quarter, will reset the company. But here’s the uncomfortable truth: 👉 Your biotech is already running on an operating cadence you didn’t consciously design. And that cadence is shaping everything: timelines, decisions, investor calls, BD traction, internal focus. Most CEOs think they’re steering the strategy. 👉 In reality, their operating cadence is steering them. And until you see it, you can’t change it. Operating cadence Attila Foris Dec 24, 2025 GPCR Binding Affinity Experiments: Interpreting Data With Confidence as We Head Into 2026 As scientists, we know curves don’t equal clarity. As 2025 comes to a close, this final edition of Weekly News focuses on how GPCR binding affinity experiments are interpreted—and how those interpretations quietly shape SAR, lead selection, and development timelines long before anyone notices. The goal isn’t more data. It’s cleaner interpretation. And that’s exactly what carries strong discovery programs into 2026. Dr. GPCR News Dec 18, 2025 Scientific Isolation: The Real Reason Early Biotechs Lose Traction The Quiet Drift You Don’t Feel Until It’s Too Late 👉 Every early-stage biotech reaches a moment where the science finally starts clicking… and the company quietly stops doing anything else. BD conversations stay warm but motionless. Investor updates become thinner. Internal meetings slowly morph into scientific colloquia instead of decision-making forums. 👉 The uncomfortable truth: your company is doing a lot of science and very little building. No drama. No blow-ups.Just Attila Foris Dec 17, 2025 Orthosteric Binding Experiments: How to Avoid the Most Common Data Pitfalls Binding affinity appears straightforward: add ligand, measure signal, fit a curve. Yet discovery teams routinely lose time and misallocate resources because the underlying biology behaves nothing like the idealized systems we learned in textbooks. GPCRs couple, decouple, isomerize, deplete tracers, and shift apparent affinity depending on stoichiometry and time. The result is a recurring pattern across programs—clean data that is not actually telling the truth. Orthosteric bi Terry's Desk Dec 16, 2025

Home → Flash News → Dr. Maria Majellaro perfected her focaccia recipe. Then, with Celtarys, the team did the same for ligand-linker-fluorophore chemistry. It’s not just culinary precision, it’s a metaphor for drug discovery done right. In Ep. 168, she shares how Celtarys went from a thesis idea to a biotech reality. Meet Dr.GPCR’s new partner: Celtarys 🙌 👉 See what they’re cooking up now: Ep 168 with Dr. Maria Majellaro from Celtarys #GPCRresearchCommunity #DrGPCR #StartupScience #BiotechFounders #GPCRscientistNetwork Published on June 12, 2025 Category Dr. GPCR Podcast Dr. Maria Majellaro perfected her focaccia recipe. Then, with Celtarys, the team did the same for ligand-linker-fluorophore chemistry. It’s not just culinary precision, it’s a metaphor for drug discovery done right. In Ep. 168, she shares how Celtarys went from a thesis idea to a biotech reality. Meet Dr.GPCR’s new partner: Celtarys 🙌 👉 See what they’re cooking up now: Ep 168 with Dr. Maria Majellaro from Celtarys #GPCRresearchCommunity #DrGPCR #StartupScience #BiotechFounders #GPCRscientistNetwork Previous Next Recent Articles

Home → Flash News → From aspiring doctor to GPCR scientist! 🔬In this episode, Ian Chronis shares his journey from med school dreams to a PhD in pharmacology, diving into the fascinating world of receptor signaling. Can you guess what’s his favorite GPCR? ✅ Hear his response: Ep 164 with Dr. Ian Chronis #SciencePodcast #GPCR #PhDLife #DrGPCR Published on April 17, 2025 Category Dr. GPCR Podcast From aspiring doctor to GPCR scientist! 🔬In this episode, Ian Chronis shares his journey from med school dreams to a PhD in pharmacology, diving into the fascinating world of receptor signaling. Can you guess what’s his favorite GPCR? ✅ Hear his response: Ep 164 with Dr. Ian Chronis #SciencePodcast #GPCR #PhDLife #DrGPCR Previous Next Recent Articles Why Biotech Fundraising Fails Due to Intellectual Property Gaps 👉 Why has intellectual property become a first-order fundraising signal? Biotech fundraising has undergone a subtle yet significant shift. Capital still exists, but investors are making decisions earlier and filtering more carefully . As a result, intellectual property is no longer something that comes up late in the process. 👉 It has become an early signal of whether a biotech company is fundable at all. This shift does not mean founders need more patents or heavier legal Attila Foris 5 days ago The Hidden Operating Cadence That’s Actually Driving Your Biotech Founders love the idea that a new year, or a new quarter, will reset the company. But here’s the uncomfortable truth: 👉 Your biotech is already running on an operating cadence you didn’t consciously design. And that cadence is shaping everything: timelines, decisions, investor calls, BD traction, internal focus. Most CEOs think they’re steering the strategy. 👉 In reality, their operating cadence is steering them. And until you see it, you can’t change it. Operating cadence Attila Foris Dec 24, 2025 GPCR Binding Affinity Experiments: Interpreting Data With Confidence as We Head Into 2026 As scientists, we know curves don’t equal clarity. As 2025 comes to a close, this final edition of Weekly News focuses on how GPCR binding affinity experiments are interpreted—and how those interpretations quietly shape SAR, lead selection, and development timelines long before anyone notices. The goal isn’t more data. It’s cleaner interpretation. And that’s exactly what carries strong discovery programs into 2026. Dr. GPCR News Dec 18, 2025 Scientific Isolation: The Real Reason Early Biotechs Lose Traction The Quiet Drift You Don’t Feel Until It’s Too Late 👉 Every early-stage biotech reaches a moment where the science finally starts clicking… and the company quietly stops doing anything else. BD conversations stay warm but motionless. Investor updates become thinner. Internal meetings slowly morph into scientific colloquia instead of decision-making forums. 👉 The uncomfortable truth: your company is doing a lot of science and very little building. No drama. No blow-ups.Just Attila Foris Dec 17, 2025 Orthosteric Binding Experiments: How to Avoid the Most Common Data Pitfalls Binding affinity appears straightforward: add ligand, measure signal, fit a curve. Yet discovery teams routinely lose time and misallocate resources because the underlying biology behaves nothing like the idealized systems we learned in textbooks. GPCRs couple, decouple, isomerize, deplete tracers, and shift apparent affinity depending on stoichiometry and time. The result is a recurring pattern across programs—clean data that is not actually telling the truth. Orthosteric bi Terry's Desk Dec 16, 2025

Home → Flash News → A large-scale analysis of GPCR molecular dynamics reveals hidden allosteric sites and lateral gateways, unlocking new possibilities for drug discovery. Subscribe to the Dr. GPCR Newsletter 📰 and get the latest GPCR News delivered to your inbox ➡️https://www.ecosystem.drgpcr.com/structural-and-molecular-insights-into-gpcr-function/large-scale-investigation-of-gpcr-molecular-dynamics-data-uncovers-allosteric-sites-and-lateral-gateways #gpcr#drgpcr Published on March 17, 2025 Category GPCR Weekly News A large-scale analysis of GPCR molecular dynamics reveals hidden allosteric sites and lateral gateways, unlocking new possibilities for drug discovery. Subscribe to the Dr. GPCR Newsletter 📰 and get the latest GPCR News delivered to your inbox ➡️ https:// www.ecosystem.drgpcr.com/structural-and-molecular-insights-into-gpcr-function/large-scale-investigation-of-gpcr-molecular-dynamics-data-uncovers-allosteric-sites-and-lateral-gateways #gpcr#drgpcr Previous Next Recent Articles Why Biotech Fundraising Fails Due to Intellectual Property Gaps 👉 Why has intellectual property become a first-order fundraising signal? Biotech fundraising has undergone a subtle yet significant shift. Capital still exists, but investors are making decisions earlier and filtering more carefully . As a result, intellectual property is no longer something that comes up late in the process. 👉 It has become an early signal of whether a biotech company is fundable at all. This shift does not mean founders need more patents or heavier legal Attila Foris 5 days ago The Hidden Operating Cadence That’s Actually Driving Your Biotech Founders love the idea that a new year, or a new quarter, will reset the company. But here’s the uncomfortable truth: 👉 Your biotech is already running on an operating cadence you didn’t consciously design. And that cadence is shaping everything: timelines, decisions, investor calls, BD traction, internal focus. Most CEOs think they’re steering the strategy. 👉 In reality, their operating cadence is steering them. And until you see it, you can’t change it. Operating cadence Attila Foris Dec 24, 2025 GPCR Binding Affinity Experiments: Interpreting Data With Confidence as We Head Into 2026 As scientists, we know curves don’t equal clarity. As 2025 comes to a close, this final edition of Weekly News focuses on how GPCR binding affinity experiments are interpreted—and how those interpretations quietly shape SAR, lead selection, and development timelines long before anyone notices. The goal isn’t more data. It’s cleaner interpretation. And that’s exactly what carries strong discovery programs into 2026. Dr. GPCR News Dec 18, 2025 Scientific Isolation: The Real Reason Early Biotechs Lose Traction The Quiet Drift You Don’t Feel Until It’s Too Late 👉 Every early-stage biotech reaches a moment where the science finally starts clicking… and the company quietly stops doing anything else. BD conversations stay warm but motionless. Investor updates become thinner. Internal meetings slowly morph into scientific colloquia instead of decision-making forums. 👉 The uncomfortable truth: your company is doing a lot of science and very little building. No drama. No blow-ups.Just Attila Foris Dec 17, 2025 Orthosteric Binding Experiments: How to Avoid the Most Common Data Pitfalls Binding affinity appears straightforward: add ligand, measure signal, fit a curve. Yet discovery teams routinely lose time and misallocate resources because the underlying biology behaves nothing like the idealized systems we learned in textbooks. GPCRs couple, decouple, isomerize, deplete tracers, and shift apparent affinity depending on stoichiometry and time. The result is a recurring pattern across programs—clean data that is not actually telling the truth. Orthosteric bi Terry's Desk Dec 16, 2025

Home → Flash News → Did you know that certain ergot derivatives can produce wash-resistant signalling through the 5-HT2B receptor persisting for many hours without losing potency or efficacy? By using signalling assays, radioligand binding assay, and microscopy, Gaidarov et al. suggested that this phenomenon results from persistently/irreversibly internalised signalling receptor complexes. Check out the latest GPCR news in the Ecosystem today! You’ll need to register but don’t worry, it’s Free! ➡️ https://www.ecosystem.drgpcr.com/receptor-activation-and-signaling/mechanisms-of-constitutive-and-agonist-induced-5-ht2b-internalization%2C-persistent-endosomal-signaling-and-paradoxical-regulation-of-agonist-pharmacology #gpcr#drgpcr Published on May 19, 2025 Category GPCR Weekly News Did you know that certain ergot derivatives can produce wash-resistant signalling through the 5-HT2B receptor persisting for many hours without losing potency or efficacy? By using signalling assays, radioligand binding assay, and microscopy, Gaidarov et al. suggested that this phenomenon results from persistently/irreversibly internalised signalling receptor complexes. Check out the latest GPCR news in the Ecosystem today! You’ll need to register but don’t worry, it’s Free! ➡️ https://www.ecosystem.drgpcr.com/receptor-activation-and-signaling/mechanisms-of-constitutive-and-agonist-induced-5-ht2b-internalization%2C-persistent-endosomal-signaling-and-paradoxical-regulation-of-agonist-pharmacology #gpcr#drgpcr Previous Next Recent Articles

Home → Flash News → Seeking to gain more knowledge on signaling bias? We’ve got the perfect opportunity for you 🚀 Registrations open until February 14th ⚠️ Last spots available for “The Practical Assessment of Signaling Bias” with Dr. Terry Kenakin ✳️Register today at https://www.ecosystem.drgpcr.com/event-details-registration/the-practical-assessment-of-signaling-bias #gpcr #drgpcr Published on February 8, 2025 Category Dr. GPCR Courses Seeking to gain more knowledge on signaling bias? We’ve got the perfect opportunity for you 🚀 Registrations open until February 14th ⚠️ Last spots available for “The Practical Assessment of Signaling Bias” with Dr. Terry Kenakin ✳️Register today at https://www.ecosystem.drgpcr.com/event-details-registration/the-practical-assessment-of-signaling-bias #gpcr #drgpcr Previous Next Recent Articles

Full Agenda Adhesion GPCR workshop 2024 CINVESTAV, Mexico City, Mexico October 23-25 Download PDF Program HERE < Back to Full Agenda Student Flash Presentations Health and Disease, Metabolism, Nervous System, Proteomics and Transcriptomics, Receptor Structure, Signaling and Activation Mechanism Adgrg6/Gpr126 is Required for Myocardial Notch Activity and N-cadherin Localization to Attain Trabecular Identity Abhishek Kumar Singh Investigating The Role of ADGRB3 Loss of Expression in Brain Tumor Formation in Li-Fraumeni Syndrome Alex Torrelli-Diljohn GPR124 Mediates Adhesion Of Leukemic Stem Cells To Their Niche And Leads To Myeloid Skewing Emmanouil Kyrloglou A single cell GPCR map of thermogenic fat Vasiliki Karagiannakou GAIN Domain Dynamics And Its Relevance For Adhesion GPCR Signaling In Vivo Lara-Sophie Brodmerkel Novel isoforms of adhesion G protein coupled receptor B1 (ADGRB1/BAI1) generated from an alternative promoter in intron 17 Rashed Rezwan Parag Identification of Differentially Expressed Gpr116 (Adgrf5) Transcript Variants in Mouse Kidney Hailey Steichen Elucidating The Role Of GPR97/ADGRG3 In Neutrophil Biology Tyler Bernadyn Next Generation MBD2 inhibitors for Brain Cancer Therapy Jesse Stillwell Adgrg6/Gpr126 is Required for Myocardial Notch Activity and N-cadherin Localization to Attain Trabecular Identity Abhishek Kumar Singh Abstract Only available for AGPCR 24 Workshop Attendees Authors & Affiliations "Srivastava, Swati1; Singh, Abhishek Kumar1; Gunawan, Felix2; Gentile, Alessandra2; Petersen, Sarah C.3; Stainier, Didier Y.R.2; Engel, Felix B.1 1 Experimental Renal and Cardiovascular Research, Department of Nephropathology, Institute of Pathology, Friedrich-Alexander-Universität Erlangen-Nürnberg, Kussmaulallee 12, 91054 Erlangen, Germany 2 Developmental Genetics, Max-Planck-Institute for Heart and Lung Research, Ludwigstrasse 43, 61231 Bad Nauheim, Germany 3 Department of Developmental Biology, Washington University in St. Louis, 660 S. Euclid Ave, St. Louis, MO 63108, USA. Present address: Department of Neuroscience, Kenyon College, 203 North College Road, Gambier, OH 43022, USA" About Abhishek Kumar Singh "I am a doctoral student in the lab of Prof. Felix B. Engel. Since my undergraduate studies, I became fascinated with the class of adhesion GPCRs, owing to their potential, scarcity of knowledge on them, diverse expression profile, and the complexity with which they seem to be working. This made me pursue my higher education in the field of adhesion GPCRs. Accordingly, I worked with Prof. Hsi-Hsien Lin as summer intern twice, and finally joined the lab of Prof. Engel. I hope to develop my skillsets so as to be able to establish my own lab in future to work on adhesion GPCRs employing highly interdisciplinary field." Abhishek Kumar Singh on the web Uniklinikum Erlangen Google Scholar X (Twitter) Investigating The Role of ADGRB3 Loss of Expression in Brain Tumor Formation in Li-Fraumeni Syndrome Alex Torrelli-Diljohn Abstract "Li-Fraumeni syndrome (LFS) is a rare cancer predisposition syndrome caused by a germline mutation in the TP53 tumor suppressor gene. Glioblastoma (GBM) is the most prevalent central nervous system tumor in LFS, with TP53 mutations detected in 30% of sporadic GBMs. GBM is the most aggressive primary brain neoplasm that affects adults, with a median survival of 12-15 months. Recent studies implicate the dysregulation of adhesion G-Protein coupled receptors (GPCRs) in GBM development. Brain angiogenesis inhibitor 3 (BAI3/ADGRB3), a member of the BAI1-3 subfamily of adhesion GPCRS, has been observed to have low expression in brain tumors according to TCGA data, but the significance of this observation has not been explored. However, while its sister protein BAI1 has demonstrated tumor suppressor functions in the brain, it remains unclear whether BAI3 shares this role. To test this, an LFS mouse model (germline Tp53 deletion) with a second floxed allele under the control of Nestin-Cre was crossed to Bai3-/- mice. Preliminary findings indicate that the simultaneous loss of Bai3 and Tp53 expression in our mouse model increased spontaneous brain tumor formation incidence from 34% to 71%, in contrast to the loss of p53 alone. These observations lead me to hypothesize that ADGRB3 functions as a tumor suppressor in the brain, and its silencing, in the context of p53 mutation, facilitates GBM formation. Isolated GBM stem cells were collected for further genomic analyses and to test whether overexpression of BAI3 will save the tumor phenotype." Authors & Affiliations "Vukadin L, Park B, Mohamed M, Li H, Elkholy A, Torrelli-Diljohn A, Kim JH, Jeong K, Murphy JM, Harvey CA, Dunlap S, Gehrs L, Lee H, Kim HG, Sah JP, Lee SN, Stanford D, Barrington RA, Foote JB, Sorace AG, Welner RS, Hildreth BE 3rd, Lim SS, Ahn EE. A mouse model of Zhu-Tokita-Takenouchi-Kim syndrome reveals indispensable SON functions in organ development and hematopoiesis. JCI Insight. 2024 Mar 8;9(5):e175053. doi: 10.1172/jci.insight.175053. PMID: 38290089; PMCID: PMC10972584. University of Alabama at Birmingham" About Alex Torrelli-Diljohn "Alex completed his undergraduate & master’s degrees in Neurobiology & Cognitive sciences from the University of South Florida, where he researched early-onset Alzheimer’s disease in the lab of Dr. Angele Parent. He is interested in working on Li-Fraumeni syndrome and helping patients afflicted with this condition. He is also interested in working on Glioma Brain Organoid models." Alex Torrelli-Diljohn on the web The University of Alabama at Birmingham LinkedIn GPR124 Mediates Adhesion Of Leukemic Stem Cells To Their Niche And Leads To Myeloid Skewing Emmanouil Kyrloglou Abstract Only available for AGPCR 24 Workshop Attendees About Emmanouil Kyrloglou "Studied medicine at the University of Groningen. Now PhD-candidate at the Experimental Hematology lab of the University Medical Center Groningen (UMCG)." Emmanouil Kyrloglou on the web Adhesion GPCR Consortium LinkedIn A single cell GPCR map of thermogenic fat Vasiliki Karagiannakou Abstract Only available for AGPCR 24 Workshop Attendees Authors & Affiliations "Karagiannakou Vasiliki, El Merahbi Rabih, Herzig Stephan , Georgiadi A , Helmholtz Center Munich, Institute of Diabetes and Cancer" About Vasiliki Karagiannakou "MSc in Bioinformatics, PhD student since 2022 in the Institute for Diabetes and Cancer IDC, Helmholtz Centre Munich" Vasiliki Karagiannakou on the web Helmholtz Centre Munich GAIN Domain Dynamics And Its Relevance For Adhesion GPCR Signaling In Vivo Lara-Sophie Brodmerkel Abstract "Over the last years, Adhesion G Protein-coupled receptors (aGPCR) have been shown to play a crucial role in the perception of mechanical signals. However, the molecular details underlying their activation and how mechanical forces are translated into an intracellular response remains largely unknown. Recent Molecular Dynamics (MD) simulations of several aGPCRs predicted two flexible regions, termed flaps, located within the GPCR autoproteolysis inducing (GAIN) domain. These flaps could theoretically enable partial decryption of the Stachel through lateral movement and affect activation of the receptor independent of NTF-CTF dissociation. However, the physiological relevance of flap flexibility on receptor activation and signaling remains unclear. To investigate whether flexibility of GAIN flaps affects aGPCR function under native conditions, we strategically inserted specific mutations into the GAIN domain of the Latrophilin homologue Cirl in Drosophila melanogaster, with the intention to alter flap dynamics. Our goal is to understand if and how flap dynamics influence Cirl function and consequently the mechanosensory faculty of neurons in vivo. To this end, we combine behavioral, biochemical, immunohistochemical and functional readouts, with the overarching ambition to expand our knowledge on the mechanistic details underlying aGPCR activation in mechanosensation." Authors & Affiliations "Brodmerkel Lara-Sophie 1, Bormann Anne 1, Seufert Florian 2, Hildebrand Peter 2,3 ´, Ljaschenko Dmitrij 1´, Scholz Nicole 1´ 1Rudolf Schönheimer Institute of Biochemistry, Division of General Biochemistry, Medical Faculty, Leipzig University, Leipzig, Germany 2Institute for Medical Physics and Biophysics, Medical Faculty, Leipzig University, Leipzig, Germany 3Institute of Medical Physics and Biophysics, Charité – Universitätsmedizin Berlin, Berlin, Germany ´ correspondence: scholzlab@gmail.com , Dmitrij.Ljaschenko@medizin.uni-leipzig.de , peter.hildebrand@medizin.uni-leipzig.de *contributed equally" About Lara-Sophie Brodmerkel "I am a medical student and I´m currently working on my MD thesis in the lab of Dr. Nicole Scholz. We are investigating the relevance of GAIN domain dynamics for aGPCR signaling in Drosophila melanogaster." Lara-Sophie Brodmerkel on the web University of Leipzig Novel isoforms of adhesion GPCR B1 (ADGRB1/BAI1) generated from an alternative promoter in intron 17 Rashed Rezwan Parag Abstract "Brain-specific angiogenesis inhibitor 1 (BAI1) belongs to the adhesion G-protein-coupled receptors, which exhibit large multi-domain extracellular N-termini that mediate cell-cell and cell-matrix interactions. To explore the existence of BAI1 isoforms, we queried genomic datasets for markers of active chromatin and new transcript variants in the ADGRB1 (adhesion G protein-coupled receptor B1) gene. Two major types of mRNAs were identified in human/mouse brain, those with a start codon in exon 2 encoding a full-length protein of a predicted size of 173.5/173.3 kDa and shorter transcripts starting from alternative exons at the intron 17/exon 18 boundary with new or exon 19 start codons, predicting shorter isoforms of 76.9/76.4 and 70.8/70.5 kDa, respectively. Immunoblots on wild-type and Adgrb1 exon 2-deleted mice, reverse transcription PCR and promoter-luciferase reporters confirmed that the shorter isoforms originate from an alternative promoter in intron 17. The shorter BAI1 isoforms lack most of the N-terminus and are very close in structure to the truncated BAI1 isoform generated through GPS processing from the full-length receptor. The cleaved BAI1 isoform has a 19 amino acid extracellular stalk that can serve as a receptor agonist, while the alternative transcripts generate BAI1 isoforms with extracellular N-termini of 5 or 60 amino acids. Further studies are warranted to compare the functions of these isoforms and examine the distinct roles they play in different tissues and cell types." About Rashed Rezwan Parag "Rashed is from Bangladesh. He has received his BSc and MS degree from the Department of Biochemistry and Molecular Biology, University of Chittagong, Bangladesh. Before joining UAB as a graduate student, he worked in the EuGEF Research Group to identify novel prognostic biomarkers and therapeutic options for Metastatic Breast Cancer (BC) and Head and Neck Squamous Cell Carcinoma (HNSCC). Currently, he is working to elucidate the role of ADGRB1 and ADGRB3 in medulloblastoma (pediatric brain tumor)." Rashed Rezwan Parag on the web Google Scholar Identification of Differentially Expressed Gpr116 (Adgrf5) Transcript Variants in Mouse Kidney Hailey Steichen Abstract "Adhesion G protein-coupled receptors (aGPCRs) are important and understudied modulators of physiological processes. Previous work suggests that aGPCRs, and Adgrf5 in particular, undergo significant tissue-specific mRNA processing that results in holoreceptors with unique and variable N-terminal structures (Knierim et al. 2019). Recently, it was shown that transcripts of the postsynaptic aGPCR Latrophilin-3 (Lphn3/Adgrl3) undergo physiologically relevant alternative splicing, which determined heterotrimeric signaling through Gαs- or Gα12/13- mediated pathways (Südhof et al. 2024). These results demonstrate that identifying precise, tissue-specific transcript variants is critical to understanding the physiological relevance of aGPCRs. Moreover, these studies highlight the possibility that tissue expression of single aGPCRs is likely comprised of multiple transcript variants. We previously demonstrated that kidney-specific Adgrf5/Gpr116 knockout causes luminal membrane accumulation of V-ATPase in acid-secreting A-type intercalated cells (AICs) in the collecting ducts and a significant reduction in urine pH (Zaidman et al. 2020). Renal Adgrf5 is restricted to two distinct populations of cells: AICs and endothelial cells (ECs). We hypothesized that cell-specific Adgrf5 transcript variants are expressed in renal AICs and ECs, and therefore are activated by distinct mechanisms unique to the cellular microenvironment. We detected and aligned three Adgrf5 exons that undergo differential expression in the kidney: exons 2, 12, and 22. Adgrf5 transcripts in FACS-sorted GFP+ ICs do not contain the exon 2 variable region, or the alternative exons 12 and 22, while ECs contain all three. However, EC markers were detected in GFP+ ICs, demonstrating some EC contamination in the sorted ICs. Detection of transcripts that do, and do not, contain multiple variable regions suggests expression of multiple mRNAs in specific cells. These data demonstrate that Adgrf5 transcript variants are cell-specific in the kidney. Moreover, the complete repertoire of aGPCRs expressed in the kidney is undefined. We performed single-nucleus RNA sequencing on male and female kidneys. snRNAseq revealed abundant, cell-specific expression of six aGPCRs (Adgrl4, Adgre5, Adgrf1, Adgrf5, Adgrg1, and Adgrg3). Detection of these, as well as 18 other aGPCRs, was confirmed by PCR screening for GAIN/GPS domains on cDNA from whole-kidney lysates. These results reveal the complete set of aGPCRs expressed in the murine kidney. Future studies will focus on determining the physiological roles and tissue-specific variants of these receptors." Authors & Affiliations "Department of Biochemistry & Molecular Biology, University of New Mexico Health Sciences Center Xue, Jianxiang; Yan, Teagan; Eaton, Krystin, and Zaidman, Nathan" About Hailey Steichen "I currently work in Dr. Nathan Zaidman’s lab at the University of New Mexico Health Sciences Center. I am researching the physiological relevance of Adgrf5 (Gpr116) transcript variants in specific cell types in the kidney. I have also worked in the laboratory of Dr. James Bridges at National Jewish Health in Denver, CO researching molecular mechanisms of lung injury and repair mediated by Adgrf5. I received my MS in Applied Toxicology from the University of Washington, and my BA in Biology from Vassar College." Hailey Steichen on the web Zaidman Physiology Lab Elucidating The Role Of GPR97/ADGRG3 In Neutrophil Biology Tyler Bernadyn Abstract Only available for AGPCR 24 Workshop Attendees Authors & Affiliations "Gandhi, Riya; Chandan, Nancy; Kwarcinski, Frank; Smrcka, Alan; and Tall, Gregory G." About Tyler Bernadyn "4th year Pharmacology Ph.D. Student in Greg Tall's Lab." Tyler Bernadyn on the web LinkedIn Next Generation MBD2 inhibitors for Brain Cancer Therapy Jesse Stillwell Abstract "Medulloblastoma (MB) is one of the most lethal pediatric brain tumors. Standard of care for MB includes tumor resection, chemotherapy, and cranio-spinal radiation. This regimen has long lasting side-effects, including neuroendocrine and cognitive problems, and ~ 30% of patients still do not survive 5 years past diagnosis. Clearly, a new, less toxic therapeutic is needed. Our lab has previously shown that expression of adhesion GPCR BAI1 (ADGRB1) is lost by epigenetic silencing in MB. Restoration of ADGRB1 expression slowed tumor growth and improved survival in mice bearing MB xenografts. The ADGRB1 promoter is methylated in MB, and this allows for Methyl CpG Binding Domain protein 2 (MBD2) to silence the gene through recruitment of the NuRD silencing complex. KCC-07 is an inhibitor that prevents MBD2 from binding to DNA, allowing re-expression of BAI1. To further optimize the chemical scaffold, we synthesized KCC07 analogs that we’re testing for their ability to reactivate BAI1 expression. The current methods for testing KCC-07’s ability to reactivate ADGRB1 expression involve western blotting and RT-qPCR, both of which are semi-quantitative methods that require large numbers of cells and high volumes of analogs, creating a bottleneck in screening. These methods are time consuming, and their inherent variability makes precise quantification difficult. This research focuses on the design of a new endogenous ADGRB1 activation reporter assay to test analogs faster and with more reproducibility." Authors & Affiliations "Erwin Van Meir, University of Alabama at Birmingham/Sadanandan Velu, University of Alabama at Birmingham/Takahiro Yamamoto, Kumamoto University" About Jesse Stillwell "Jesse Stillwell is a 3rd year graduate student with a research focus in drug development. His project is drug discovery focused, with particular interest in use of a novel epigenetic therapy to reactivate ADGRB1 expression." Jesse Stillwell on the web Van Meir Lab – Heersink School of Medicine < Previous Session Next Session >

Retreat 2023 About Program Registration Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule Pharmacological and Genetic Preclinical Models of Ghrelin Receptor Functional Selectivity to Investigate Metabolic Disease Pathophysiology Date & Time Friday, November 3rd / 9:45 AM Abstract Coming Soon Authors and Affiliations Gross JD -1 (lead author, presenter) Kohlenbach LM -2 Zhou Y -1 Marugan JJ -3 Barak LS -1 (senior author) 1-Department of Cell Biology, Duke University Medical Center, Durham, NC 27710. 2-Department of Biology, Duke Trinity College of Arts and Sciences, Durham, NC 27710. 3-National Center for Advancing Translational Sciences (NCATS), NIH Division of Preclinical Innovation, Rockville, MD 20892. About Joshua Gross "I am a neuropharmacologist interested in exploiting GPCR biased signaling to design/develop new pharmacotherapeutics to treat reward- and metabolism-based diseases, including obesity, eating disorders, and diabetes. I received my PhD in Cellular & Integrative Physiology from West Virginia University under the mentorship of Drs. David Siderovski and Vincent Setola (2014-2019). I am currently completing my postdoctoral research in the laboratory of the late Dr. Marc Caron (2019-2023) and subsequently, will begin my independent research career as a tenure-track Assistant Professor at Penn State University (University Park) in August 2023. My broad research interest is to better understand the underlying mechanisms of food reward and its downstream dysregulation of metabolic function, particularly in response to obesogenic 'Western' diets (aka, ultra-processed food). With my expertise in reward behavior, neurophysiology, GPCR signaling, and preclinical drug development, my lab will strive to develop novel GPCR pharmacotherapies that improve efficacy and minimize side effects for diet-induced metabolic diseases. " Josh Gross on the web 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

Home → Flash News → Disrupting VIPR2 dimerisation halts breast cancer spread—could TM3-4 peptides be the next breakthrough in targeted cancer therapy? Check out the latest GPCR news in the Ecosystem today! You’ll need to register but don’t worry, it’s Free! ➡️ https://www.ecosystem.drgpcr.com/gpcrs-in-oncology-and-immunology/dimerisation-of-the-vip-receptor-vipr2-is-essential-to-its-binding-vip-and-g%CE%B1i-proteins%2C-and-to-its-functions-in-breast-cancer-cells #gpcr#drgpcr Published on May 12, 2025 Category GPCR Weekly News Disrupting VIPR2 dimerisation halts breast cancer spread—could TM3-4 peptides be the next breakthrough in targeted cancer therapy? Check out the latest GPCR news in the Ecosystem today! You’ll need to register but don’t worry, it’s Free! ➡️ https://www.ecosystem.drgpcr.com/gpcrs-in-oncology-and-immunology/dimerisation-of-the-vip-receptor-vipr2-is-essential-to-its-binding-vip-and-g%CE%B1i-proteins%2C-and-to-its-functions-in-breast-cancer-cells #gpcr#drgpcr Previous Next Recent Articles

Home → Flash News → terrys corner no fluff pure insight Published on July 8, 2025 Category Terry's Corner The wait is over! Terry's Corner is LIVE! ✨ We've poured our passion for pharmacology into creating this essential resource, designed to meet you exactly where you are in your drug discovery journey. Dr. Terry Kenakin delivers razor-sharp insights, all on-demand. Ready to: Strengthen your pharmacology fundamentals? Bridge theory to practical drug development decisions? Push the boundaries with advanced concepts like allosteric modulation and residence time? Terry's Corner helps you make better decisions through better pharmacology. Enroll now: https://www.terrykenakin.com #pharmacology #GPCRscience #drugdiscovery #TerrysCorner #biotechtraining #ScienceEducation #Pharma #GPCR #DrGPCR Previous Next Recent Articles

Home → Flash News → terrys corner predict drug behavior Published on July 12, 2025 Category Terry's Corner Linear, linkage, or probability? Dive into the logic of drug modeling with Terry Kenakin. In his latest lesson, he breaks down the essential models shaping modern pharmacology. Learn to “extend your eyes” and predict complex drug behaviors. 🟢 Browse the full catalog (and expect a new course every week!) ✳️ https://www.terrykenakin.com #pharmacology #drugmechanism #kenakin #GPCR #DrGPCR Previous Next Recent Articles

Michelle Halls reminds us of something every scientist eventually learns: hard work is essential, but noticing the unexpected often defines your biggest breakthroughs. Home → Flash News → Scientific careers are not just built on brilliance Scientific careers aren’t just built on brilliance Published on November 14, 2025 Category Dr.GPCR Podcast Scientific careers aren’t just built on brilliance—they’re shaped by curiosity, timing, and paying close attention. In this conversation, Michelle Halls reminds us of something every scientist eventually learns: hard work is essential, but noticing the unexpected often defines your biggest breakthroughs. She also names a truth we rarely acknowledge out loud—luck and timing matter. Many talented scientists leave the field not because they lacked skill, but because the right opportunity didn’t land at the right time. And that’s why attention to detail, persistence, and a bit of serendipity can change the trajectory of a research career. 🎧 Watch this moment — then catch the full episode: https://www.ecosystem.drgpcr.com/dr-gpcr-podcast/leadership-luck-and-gpcr-signaling #GPCR #DrGPCR Previous Next Recent Articles Why Biotech Fundraising Fails Due to Intellectual Property Gaps 👉 Why has intellectual property become a first-order fundraising signal? Biotech fundraising has undergone a subtle yet significant shift. Capital still exists, but investors are making decisions earlier and filtering more carefully . As a result, intellectual property is no longer something that comes up late in the process. 👉 It has become an early signal of whether a biotech company is fundable at all. This shift does not mean founders need more patents or heavier legal Attila Foris 5 days ago The Hidden Operating Cadence That’s Actually Driving Your Biotech Founders love the idea that a new year, or a new quarter, will reset the company. But here’s the uncomfortable truth: 👉 Your biotech is already running on an operating cadence you didn’t consciously design. And that cadence is shaping everything: timelines, decisions, investor calls, BD traction, internal focus. Most CEOs think they’re steering the strategy. 👉 In reality, their operating cadence is steering them. And until you see it, you can’t change it. Operating cadence Attila Foris Dec 24, 2025 GPCR Binding Affinity Experiments: Interpreting Data With Confidence as We Head Into 2026 As scientists, we know curves don’t equal clarity. As 2025 comes to a close, this final edition of Weekly News focuses on how GPCR binding affinity experiments are interpreted—and how those interpretations quietly shape SAR, lead selection, and development timelines long before anyone notices. The goal isn’t more data. It’s cleaner interpretation. And that’s exactly what carries strong discovery programs into 2026. Dr. GPCR News Dec 18, 2025 Scientific Isolation: The Real Reason Early Biotechs Lose Traction The Quiet Drift You Don’t Feel Until It’s Too Late 👉 Every early-stage biotech reaches a moment where the science finally starts clicking… and the company quietly stops doing anything else. BD conversations stay warm but motionless. Investor updates become thinner. Internal meetings slowly morph into scientific colloquia instead of decision-making forums. 👉 The uncomfortable truth: your company is doing a lot of science and very little building. No drama. No blow-ups.Just Attila Foris Dec 17, 2025 Orthosteric Binding Experiments: How to Avoid the Most Common Data Pitfalls Binding affinity appears straightforward: add ligand, measure signal, fit a curve. Yet discovery teams routinely lose time and misallocate resources because the underlying biology behaves nothing like the idealized systems we learned in textbooks. GPCRs couple, decouple, isomerize, deplete tracers, and shift apparent affinity depending on stoichiometry and time. The result is a recurring pattern across programs—clean data that is not actually telling the truth. Orthosteric bi Terry's Desk Dec 16, 2025

How Michelle Halls turned an unexpected summer project into a GPCR research career redefining spatial signaling and drug discovery. Home → Flash News → How GPCR Spatial Signaling Sparked a Scientific Journey How GPCR Spatial Signaling Sparked a Scientific Journey Published on November 12, 2025 Category Dr. GPCR Podcast When boredom met obsession. It started as a summer project.A reluctant student pipetting through the day, expecting nothing more than routine lab work. But for Michelle Halls, that first experiment flipped everything. One spark led to a PhD at Monash University, a fellowship at University of Cambridge, and eventually a leadership role at the forefront of GPCR spatial signaling — a field reshaping how we understand receptor biology and drug discovery. Michelle’s story isn’t just about science.It’s about what happens when curiosity takes over. From reluctant intern to scientific leader From local signaling to spatial pharmacology From spark to strategy Read the full story here🔗 https://www.ecosystem.drgpcr.com/post/how-gpcr-spatial-signaling-sparked-a-scientific-journey 🔓 Want deeper GPCR insights? Join Dr. GPCR Premium for exclusive content, expert access, and community. #GPCR #DrGPCR #SpatialSignaling #Pharmacology #DrugDiscovery #ScientificLeadership #Biotech Previous Next Recent Articles Why Biotech Fundraising Fails Due to Intellectual Property Gaps 👉 Why has intellectual property become a first-order fundraising signal? Biotech fundraising has undergone a subtle yet significant shift. Capital still exists, but investors are making decisions earlier and filtering more carefully . As a result, intellectual property is no longer something that comes up late in the process. 👉 It has become an early signal of whether a biotech company is fundable at all. This shift does not mean founders need more patents or heavier legal Attila Foris 5 days ago The Hidden Operating Cadence That’s Actually Driving Your Biotech Founders love the idea that a new year, or a new quarter, will reset the company. But here’s the uncomfortable truth: 👉 Your biotech is already running on an operating cadence you didn’t consciously design. And that cadence is shaping everything: timelines, decisions, investor calls, BD traction, internal focus. Most CEOs think they’re steering the strategy. 👉 In reality, their operating cadence is steering them. And until you see it, you can’t change it. Operating cadence Attila Foris Dec 24, 2025 GPCR Binding Affinity Experiments: Interpreting Data With Confidence as We Head Into 2026 As scientists, we know curves don’t equal clarity. As 2025 comes to a close, this final edition of Weekly News focuses on how GPCR binding affinity experiments are interpreted—and how those interpretations quietly shape SAR, lead selection, and development timelines long before anyone notices. The goal isn’t more data. It’s cleaner interpretation. And that’s exactly what carries strong discovery programs into 2026. Dr. GPCR News Dec 18, 2025 Scientific Isolation: The Real Reason Early Biotechs Lose Traction The Quiet Drift You Don’t Feel Until It’s Too Late 👉 Every early-stage biotech reaches a moment where the science finally starts clicking… and the company quietly stops doing anything else. BD conversations stay warm but motionless. Investor updates become thinner. Internal meetings slowly morph into scientific colloquia instead of decision-making forums. 👉 The uncomfortable truth: your company is doing a lot of science and very little building. No drama. No blow-ups.Just Attila Foris Dec 17, 2025 Orthosteric Binding Experiments: How to Avoid the Most Common Data Pitfalls Binding affinity appears straightforward: add ligand, measure signal, fit a curve. Yet discovery teams routinely lose time and misallocate resources because the underlying biology behaves nothing like the idealized systems we learned in textbooks. GPCRs couple, decouple, isomerize, deplete tracers, and shift apparent affinity depending on stoichiometry and time. The result is a recurring pattern across programs—clean data that is not actually telling the truth. Orthosteric bi Terry's Desk Dec 16, 2025

Home → Flash News → How do GPCRs sense pH changes? New cryo-EM structures of GPR4 and GPR68 reveal how extracellular histidines act as proton sensors-trigger activation and biased G protein coupling! Did you know that we work hard to bring you the most recent GPCR News, weekly? Catch up today in the Ecosystem using your free site membership! ➡️https://www.ecosystem.drgpcr.com/structural-and-molecular-insights-into-gpcr-function/structural-basis-and-biased-signaling-of-proton-sensation-by-gpcrs-mediated-by-extracellular-histidine-rearrangement #gpcr#drgpcr Published on May 26, 2025 Category GPCR Weekly News How do GPCRs sense pH changes? New cryo-EM structures of GPR4 and GPR68 reveal how extracellular histidines act as proton sensors-trigger activation and biased G protein coupling! Did you know that we work hard to bring you the most recent GPCR News, weekly? Catch up today in the Ecosystem using your free site membership! ➡️ https://www.ecosystem.drgpcr.com/structural-and-molecular-insights-into-gpcr-function/structural-basis-and-biased-signaling-of-proton-sensation-by-gpcrs-mediated-by-extracellular-histidine-rearrangement #gpcr#drgpcr Previous Next Recent Articles

Home → Flash News → We’re proud to welcome Celtarys as our media partner! Known for their fluorescent ligand innovation, Celtarys is helping researchers make biology visible, faster, smarter, and with more precision. Their chemistry speaks the language of biology, and now, they’re speaking to the global GPCR community through this powerful collaboration. 🔗 Explore Celtarys on the Dr. GPCR Ecosystem: https://www.ecosystem.drgpcr.com/celtarys-research-dr-gpcr-ecosystem #DrGPCR #GPCRtools #FluorescentLigands #BiotechInnovation Published on June 4, 2025 Category Celtarys - Media Partner We’re proud to welcome Celtarys as our media partner! Known for their fluorescent ligand innovation, Celtarys is helping researchers make biology visible, faster, smarter, and with more precision. Their chemistry speaks the language of biology, and now, they’re speaking to the global GPCR community through this powerful collaboration. 🔗 Explore Celtarys on the Dr. GPCR Ecosystem: https://www.ecosystem.drgpcr.com/celtarys-research-dr-gpcr-ecosystem #DrGPCR #GPCRtools #FluorescentLigands #BiotechInnovation Previous Next Recent Articles