<< Back to podcast list Strategic Partner(s) Yao Lu (Jackie) About Yao Lu (Jackie) "Jackie is a Ph.D. student, at Monash University, Australia, investigating the role of functional selectivity in a novel class of potential antipsychotics for the treatment of schizophrenia. Her work involves the pharmacological and structural characterisation of novel putative antipsychotic small molecules. Her research aims to provide a molecular explanation of small molecules for their pre-clinical efficacy and to support the design of novel therapeutics. " Yao Lu (Jackie) on the web Monash University Georgina Sweet Fellowship Authorea Dr. GPCR Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

Explore how GPCR signaling shapes mosquito feeding and mating behaviors with Dr. Laura Duvall. Insights for GPCR researchers and functional assay innovators. << Back to podcast list Strategic Partner(s) Why Mosquitoes Hunt You: GPCR Control of Blood Feeding and Mating This episode features Dr. Laura Duvall, whose research tracks the molecular mechanisms that govern mosquito behavior, focusing on the intersection of neuropeptide signaling and GPCR function. Dr. Duvall discusses her lab’s work dissecting how GPCRs—especially neuropeptide Y (NPY) receptors—regulate innate behaviors such as blood feeding and mating in Aedes aegypti . She shares approaches that combine genetic manipulation (CRISPR-Cas9) and functional behavioral assays, including high-throughput and video-based methods, to reveal these receptors’ roles. The conversation explores translational implications, such as leveraging conserved GPCR pathways to inhibit pathogen transmission, highlighting unexpected links between mosquito and human gut-brain signaling. Dr. Duvall emphasizes the value of model systems and cross-species discoveries in GPCR biology. Listeners interested in GPCR drug discovery, functional assay development, or fluorescence-based assays in behavioral research are encouraged to explore more episodes of the Dr. GPCR Podcast and consider the expanded content on Dr. GPCR University . Why This Matters? How GPCR-mediated neuropeptide signaling dictates mosquito attraction to humans, directly impacting disease transmission. Why the study of conserved receptor pathways enables the development of broadly effective, species-independent vector control strategies. What functional and behavioral assays in mosquitoes reveal about the underlying diversity of GPCR signaling across taxa. How dissecting receptor function in non-neuronal tissues uncovers new parallels to human gut-brain communication. Who Should Listen? This episode is essential for anyone advancing GPCR-targeted research in physiological or behavioral contexts. If you often translate receptor mechanism findings from model organisms to human systems. If you want to expand high-throughput or fluorescence-based assay strategies to non-traditional models. If you are interested in how behavioral outcomes emerge from cell-type-specific GPCR expression and signaling dynamics. If you are considering novel ways to connect molecular pharmacology with organismal phenotype, especially in vector biology or neurobiology. About Laura Duvall Laura Duvall trained in biochemistry and behavioral biology at the University of Pennsylvania. During her PhD with Paul Taghert at Washington University in St. Louis, she investigated neuropeptide control of circadian behaviors in Drosophila , with a specific focus on how GPCR family members orchestrate brain clock cell function. As a postdoctoral researcher in Leslie Vosshall’s laboratory at Rockefeller University, Dr. Duvall pivoted to the Aedes aegypti mosquito, focusing on the molecular regulation of feeding and reproductive behaviors via neuropeptidergic GPCR signaling. In 2019, Dr. Duvall established her laboratory at Columbia University, where she is part of the Department of Biological Sciences and the Zuckerman Institute. Recognized with the Beckman Young Investigator Award, the Klingenstein-Simons Fellowship in Neuroscience, and a Pew Scholarship, she continues to drive efforts to decode how evolutionarily conserved GPCR pathways modulate complex behavioral outcomes. Her research is consistently motivated by uncovering new biological connections that can bridge basic and translational science. Guest on The Web LinkedI n Google Scholar Lab Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Strategic Partner(s) Dr. Sai Prasad Pydi About Dr. Sai Prasad Pydi Dr. Sai Prasad Pydi obtained his Ph.D. from the University of Manitoba – Canada, where he was introduced to G protein-coupled receptors (GPCRs) by Prof. Prashen Chelikani . His doctoral research focused on the structural and functional characterization of bitter taste receptors (T2Rs). In 2014, Dr. Pydi joined Dr. Jurgen Wess’s lab at the National Institute of Diabetes, Digestive and Kidney Diseases (NIDDK) - NIH, USA as a postdoctoral fellow and trained on understanding the physiological role of GPCR signaling and beta-arrestins in diabetes and obesity. In February 2021, Dr. Pydi joined BSBE department at IIT-Kanpur. The main target of Dr. Pydi's laboratory is to develop GPCR-based drugs for the treatment of obesity and Type 2 Diabetes (T2D) by exploring metabolically important signaling pathways in immune cells and insulin-sensitive tissues (liver, pancreas, skeletal muscle, adipose tissue, and brain). His laboratory uses knock-out and transgenic mouse models, along with different cell culture systems, to understand the role of immune cell GPCRs and their cross-talk with other insulin-sensitive tissues regulating glucose and lipid metabolism. Dr. Sai Prasad Pydi on the web Molecular Metabolism & Cell Signaling Laboratory Website Twitter.com Research Gate PubMed Google Scholar Dr. GPCR Ecosystem Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Strategic Partner(s) 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 Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

< Back Introduction to GLP-1 pharmacology October 8, 2026 10 AM - 11:30 AM EST 🔒 Watch Recordings - Join Premium Access the full library of recorded Masterclass sessions. Get Live Updates Be notified when new live Masterclasses are scheduled. Introduction Glucagon-like peptide-1 (GLP-1) is an incretin hormone that plays a central role in the regulation of glucose metabolism and energy balance. Its discovery and characterization have led to the development of GLP-1 receptor agonists, a therapeutic class widely used in the treatment of type 2 diabetes and obesity. This session provides a foundational overview of GLP-1 physiology and receptor pharmacology. The discussion will examine how GLP-1 regulates insulin secretion, suppresses glucagon release, slows gastric emptying, and influences central appetite pathways. The session also reviews currently approved GLP-1 receptor agonists, highlighting pharmacokinetic strategies used to extend activity and comparing short- and long-acting agents in clinical practice. Instructor Marsha Pierce earned her PhD at Creighton University, where she studied the role of microRNAs in inner ear development and function. She later completed postdoctoral training at Creighton University in the Department of Pharmacology and Neuroscience, focusing on neuroactive natural products. Dr. Pierce is currently an Associate Professor at Midwestern University. Her laboratory investigates marine-derived natural products with neuroactive properties, with particular emphasis on identifying compounds that modulate neural signaling pathways and may serve as leads for therapeutic development. In this Masterclass, she introduces the physiological and pharmacological foundations of GLP-1 receptor signaling in metabolic disease. Upcoming Live Sessions

GPCRs drive cancer more often than the textbooks say. Dr. Silvio Gutkind on G protein hotspot mutations, why the canonical GαQ pathway fails in uveal melanoma, and how CXCR3 may gate immunotherapy response. << Back to podcast list Strategic Partner(s) Silvio Gutkind: When GPCRs Drive Cancer GPCRs are the most drugged protein family in medicine, but until recently their role in cancer was treated as marginal — a few curiosities around mas and muscarinic receptors, overshadowed by kinases and Ras. The emergence of cancer genomics has dismantled that framing. Roughly 20% of tumors now show mutations in GPCRs or their coupled G proteins, and specific cancers — uveal melanoma above all — are understood to be driven almost entirely by single hotspot mutations in GαQ. For Dr. J. Silvio Gutkind, who has spent more than three decades pushing GPCRs as oncogenic signaling systems, the shift has concrete stakes: uveal melanoma patients who metastasize to the liver live six to twelve months, and every pathway his lab has opened — from TRIO and Rho to YAP and FAK — has been an attempt to give those patients something the canonical PLC pathway could not. In this conversation, Dr. Gutkind traces how GPCRs moved from a side project nobody believed in to a recognized driver class in oncology, and explains why chemokine receptors like CXCR3 may be the next frontier for understanding immunotherapy response. About the Guest Dr. J. Silvio Gutkind is Professor of Pharmacology and Associate Director of Basic Science at the UC San Diego Moores Cancer Center. His training began at the University of Buenos Aires on alpha-2 adrenergic receptors, continued at the NIH across neurobiology and oncogenes, and grew into a multi-decade program on GPCR signaling in cancer — first as NIH branch chief at NIDCR, then as head of a team that moved cross-country with him to UCSD in 2015. His lab combines classical pharmacology with cancer genomics, bioinformatics, and synthetic lethality approaches to identify druggable nodes downstream of G protein mutations. Current focuses include GαQ-driven uveal melanoma, GαS mutations across pancreatic, colon, and appendix cancers, and chemokine receptor biology in cancer immunotherapy. Scientific Themes of the Conversation GPCRs as oncogenes without mutations — aberrant expression and "oncocrine" autocrine/paracrine signaling The cancer genomics revolution and the rise of G protein hotspot mutations (GαQ Q209, GαS, Gα13) GαQ-driven uveal melanoma and the limits of the canonical PLC pathway Non-canonical GαQ signaling through TRIO, Rho, YAP, and the druggable FAK node CXCR3 and the chemokine axis that gates immunotherapy response Structural biology, machine learning, and team science in GPCR pharmacology Key Insights from the Conversation 1. GPCRs don't need mutations to drive cancer. Aberrant expression — a receptor in the wrong place at the wrong time, paired with autocrine or paracrine ligand — is sufficient to transform cells. Early focus-formation assays using muscarinic receptors and carbachol produced transforming efficiencies comparable to Ras, and the community largely looked away because the biology didn't fit the prevailing mutation-centric frame. 2. Cancer genomics rewrote the role of G proteins. Roughly 20% of tumors carry mutations in GPCRs or G proteins, with striking hotspots in GαQ, GαS, and Gα13. Most large cancer sequencing panels now include these genes — though most oncologists are still unsure what the results mean clinically, leaving a gap between the genomic data and how it's acted upon. 3. The uveal melanoma driver is almost monogenic. Nearly 93% of uveal melanomas carry a single GαQ Q209 activating mutation that blocks GTPase activity. Beyond this driver, the tumor has only a handful of additional mutations — more like a pediatric cancer than an adult one. The canonical assumption that targeting PLC would be therapeutic has failed in the clinic, and patients with liver metastases still have six to twelve months to live. 4. Non-canonical signaling opened a new drug target. A synthetic lethality analysis performed entirely in silico revealed that GαQ tumors depend not only on PLC but on a TRIO → Rho → YAP axis, with FAK emerging as a druggable downstream node. That insight is now powering focal adhesion kinase–directed clinical trials, including one Dr. Gutkind's team is launching. 5. CXCR3 may be the hidden gatekeeper of immunotherapy response. CXCL9, CXCL10, and CXCL11 are among the most robust predictive signatures for checkpoint inhibitor response — and all three are ligands for CXCR3. In knockout mice, loss of CXCR3 abolishes response to both anti-PD-1 and anti-CTLA-4, reframing the receptor as something to activate, not block. 6. "What the heck" moments define real discoveries. Two of Dr. Gutkind's most cited papers came from results that directly contradicted the textbook: βγ subunits (not α) activating ERK through Gi-coupled receptors, and Rho GTPases (not Ras) driving JNK activation. Both required trusting the data when the conceptual framework was telling the team they must be wrong. Both landed in Nature and Cell respectively. 7. Team science is structural, not decorative. The 2020 Cell paper on G protein coupling specificity came from a Gordon Conference hallway conversation, combining bioinformatics from Europe, high-throughput screens from Japan, and biology from UCSD. And the 12 people who moved cross-country from NIH to UCSD did so because of relationships built over years — a retention outcome Dr. Gutkind attributes to the team, not the weather. Selected Quotes "The very simple concept is that GPCRs do not need to be mutated to be oncogenic." "There are cancers that are driven by G proteins. That changed the landscape in terms of understanding and appreciation." "What the heck — this doesn't make sense. And that was our first Cell paper. Still our most cited paper." "Don't be afraid to send emails." Episode Timeline 00:00 Introduction 02:09 From Buenos Aires to NIH: a career that followed the science, not the field 06:19 Operation Exodus — the team that moved cross-country 07:35 The muscarinic focus assay and a side project no one believed in 10:52 The cancer genomics result that reframed GPCRs as drivers 16:45 Why CXCR3 may decide who responds to checkpoint inhibitors 20:28 GαQ, uveal melanoma, and the failure of the textbook pathway 41:27 Structural biology, machine learning, and the coupling problem 45:31 Two "what the heck" moments that became Nature and Cell papers 50:48 Advice for young scientists — read, think, question the dogma 56:33 Why small conferences produce the best collaborations Timestamps were generated using AI for readability. 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 Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Strategic Partner(s) Dr. Mark Connor About Dr. Mark Connor Undergraduate BSc with Honours in Pharmacology from University of Sydney (1987, snake neurotoxins), Ph.D. from Department of Pharmacology, University of Washington (1992, mentor Charley Chavkin , sigma receptors). Postdoc with Graeme Henderson (Bristol, opioids and Ca signaling) and Mac Christie (Sydney, opioids in neurons, novel spider toxins). Grant-funded independent research positions from 2001 at University of Sydney (opioids and sensory neurons), Vollum Institute Portland (visiting scientist with Ed McCleskey, sensory neuron properties); Pain Management Research Institute (more opioids, cannabinoids and T-type Ca channels) and Brain and Mind Research Institute (Sydney). 2009, appointed Professor of Pharmacology at Macquarie University. Focus on study of drugs and toxins on GPCR (opioid, cannabinoid receptor) and ion channel (K, Ca, TRP channel) function; mostly electrophysiology and fluorescence-based reporters, but can grind and bind. Currently pursuing molecular pharmacology of phytocannabinoids and novel synthetic cannabinoids, with a focus on efficacy and novel targets. Interested in orthosteric and allosteric interactions, and still looking for some bias ... anywhere ... these days human only. Dr. Mark Connor on the web Researchers Twitter Google Scholar Dr. GPCR Ecosystem Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

< Back The spatiotemporal organization of GPCR signalling September 10, 2026 10 AM - 11:30 AM EST 🔒 Watch Recordings - Join Premium Access the full library of recorded Masterclass sessions. Get Live Updates Be notified when new live Masterclasses are scheduled. Introduction GPCR signaling is organized in space and time. Where a receptor signals, how long it remains engaged, and which membrane it occupies all shape the downstream response, yet these events are averaged away by conventional population assays. This Masterclass examines the spatiotemporal organization of GPCR signaling and the optical methods that resolve it in living cells, down to individual molecules. Coverage spans the mechanisms of receptor signaling and trafficking, labeling strategies and quantitative imaging by FRET, BRET, and single-molecule microscopy, and signaling on internal membranes including endosomes and the Golgi. Intended for GPCR scientists, cell biologists, and drug discovery professionals working on receptor signaling dynamics, trafficking, and quantitative microscopy. Instructor Bio Davide Calebiro's work has reshaped how the field understands where and when GPCRs signal. Using single-molecule microscopy, FRET, and BRET to observe signaling directly in living cells, one molecule at a time, his team resolves how receptors and transducers interact in space and time, and how GPCRs signal from internal membranes such as endosomes and the Golgi, work with direct bearing on therapeutic directions such as biased agonists for metabolic disease. He is Chair of Molecular Endocrinology and a Wellcome Trust Senior Research Fellow at the University of Birmingham, where he heads the Department of Metabolism and Systems Science and co-directs the Centre of Membrane Proteins and Receptors (COMPARE). His Masterclass brings this single-molecule, imaging-driven view of receptor signaling directly to Dr. GPCR University. Upcoming Live Sessions

Live webinar with Dr. Terry Kenakin on detecting, quantifying, and applying receptor signaling bias in GPCR drug discovery. May 28, 2026. Free. < Back to Webinars 📅 Thursday, May 28, 2026 at 11:00:00 AM EDT 🤝 Webinar in collaboration with: Eurofins DiscoverX Receptor Signaling Bias: A Valuable and Accessible Property of New Drug Candidates Turning functional selectivity into a practical decision-making tool in GPCR drug discovery Beyond Potency: What Ligand-Dependent Signaling Reveals About Drug Candidates G protein-coupled receptors can signal through multiple intracellular pathways, and ligands do not necessarily engage those pathways to the same extent. This phenomenon, receptor signaling bias or functional selectivity, is now recognized as a meaningful property of many drug candidates and a potential route to improved efficacy, better tolerability, and new opportunities in challenging targets. Bias is not an anomaly. It is a consequence of ligand-dependent receptor conformations and allosteric probe dependence, and it can be revealed with the right combination of functional assays. This webinar explains the biological basis of signaling bias, shows how to detect and quantify it using reliable functional assays, and discusses how these data can guide lead selection and optimization. Practical assay strategies, interpretation pitfalls, and the value of comparing pathway outputs quantitatively, rather than relying on potency alone, sit at the center of the session. The Biology Behind Bias Ligands produce differential pathway engagement at a single receptor because they stabilize distinct receptor conformations. These conformations determine which downstream pathways are favored and which are muted. Due to this potential inherent bias, it is best practice to evaluate multiple pathways using different GPCR assays to obtain a better understanding of the ligand effects on the GPCR system. Speaker Dr. Terry Kenakin Professor of Pharmacology & Pharmacology Course Coordinator Department of Pharmacology, University of North Carolina School of Medicine, Chapel Hill. Dr. Kenakin trained in chemistry and pharmacology at the University of Alberta and completed postdoctoral work at University College London in the laboratory of Sir James Black. He spent 25 years in drug discovery at Glaxo (now GlaxoSmithKline) before joining UNC Chapel Hill, where he teaches and leads research in receptor pharmacology. His work is central to the quantitative framework used today to describe receptor signaling bias, allosteric function, and agonism. He proposed one of the first mechanistic explanations of biased signaling and co-authored the widely-applied simple method for quantifying functional selectivity. He is the author of A Pharmacology Primer, Editor-in-Chief of the Journal of Receptors and Signal Transduction, and a Fellow of the British Pharmacological Society, recognized with the Goodman and Gilman Award from ASPET and the Gaddum Memorial Award. Within the Dr. GPCR ecosystem, Terry hosts Terry's Corner, a live room where GPCR scientists get direct access to him. It's where the mechanistic questions that usually sit beneath the data get asked out loud, and where receptor theory, biased signaling, and the pharmacology of real drug discovery decisions are worked through together. Organizers Eurofins DiscoverX Eurofins DiscoverX is a one-stop-shop for GPCR drug discovery and development, with 25+ years of expertise and validated cell-based assays spanning basic research through therapeutic discovery, optimization, and regulatory submission. Their assays are industry-standard, accepted for regulatory potency testing, and backed by thousands of peer-reviewed publications and partnerships with leading pharma and biotech companies. 1,500 human GPCR products covering ~90% of the GPCR-ome, including orphan receptors and ortholog variants Multiple mechanisms of action: cAMP accumulation, β-arrestin recruitment, receptor internalization, ligand binding, calcium flux, and pharmaco-chaperone discovery Flexible formats: cell line assay kits, ready-to-use eXpress kits, qualified bioassays, membrane preps, detection kits, and custom products Applications across target identification, HTS, lead optimization, ligand bias and allostery evaluation, safety assessment, and regulatory potency testing Dedicated portfolio for obesity and diabetes GPCR targets (GLP-1R, GIPR, GCGR, MC4R, AMY receptors, and more) Dr. GPCR Dr. GPCR is a membership-based nonprofit ecosystem dedicated to advancing GPCR-targeted drug discovery. It provides curated industry intelligence, expert-led masterclasses, and structured engagement opportunities for scientists and biotech leaders working across pharmacology, translational research, and therapeutic development. Curated intelligence on GPCR drug discovery trends and developments Expert-led webinars and masterclasses with leading researchers Structured networking for scientists and biotech professionals Nonprofit model, community-first, member-driven Free membership tier available Previous Webinar Next Webinar Don’t Miss the Next Live Session Dr. GPCR membership gives you access to all upcoming live, interactive webinars. Free. Takes less than a minute to join. Cancel anytime. Sign Up for Free

Transform your biotech idea or data into a clear, strategic roadmap with aligned biology, timelines, and CRO partnerships for faster results. Home About Services News Get in Touch Welcome Biotech Growth Wherever You Are in Discovery—Let’s Build a Plan That Moves You Forward Align your biology, timeline and CRO roadmap. Take your idea, platform, or early data and turn it into a strategic roadmap with clear decisions, timelines, and results fast. Start My Discovery Plan Too Much Uncertainty, Not Enough Progress You’re not alone. Biotech teams often tell me: “We have too many CROs and not enough clarity.” “We don’t know what matters most right now.” “We’re running experiments before aligning on strategy.” That's where I come in. How I Help Biotechs Accelerate GPCR Discovery with Clarity, Speed & Confidence Decisions, Not More Data We'll define what matters, when to decide, and how to act—based on your biology, not just what's easy to test. Prioritize assays based on project phase and decision points Map go/no-go logic that guides program momentum Focus resources where they’ll change outcomes No More Strategy Swirl I build structure that sticks—from CRO engagement to assay cascades—so your team isn't guessing what's next. Build experiment timelines aligned with strategy, not spreadsheets Set up clear deliverables across internal and CRO teams Keep cross-functional teams moving with shared structure Impress Your Board and Your Team Walk into every update with a confident story, backed by data, decisions, and momentum. Distill discovery progress into board-ready insights Craft milestone updates that tie data to strategy Present clear next steps that build investor confidence Trusted by Biotech Innovators Before working with Yamina, we were navigating challenging decisions around corporate and early discovery strategy. After bringing her in, we made confident progress on a key program and gained clarity around where to focus next. She helped bring teams together and created momentum across both science and execution. - Murat Tunabolyu, CEO Antiverse Frequently Asked Questions 01 What size companies do you work with? I work with early-stage biotechs—typically preclinical through IND-enabling—who need strategic clarity and hands-on discovery support. 02 How involved are you day-to-day? I adapt to your needs. Some teams want regular strategy sessions. Others bring me in to fix one key problem fast. 03 What's the typical outcome? You walk away with a decision-ready roadmap, improved CRO output, and faster movement through your discovery funnel. Let's turn complexity into clarity—before your next program milestone. Start My Discovery Plan Send me a message First name* Last name Company name* Email* How Can I Help?* Send Message or Book My Call Menu Home Services About Ready to collaborate? Let’s talk about how I support GPCR discovery, pharmacology strategy, and cross-functional execution across biotech, VC, and CRO teams. Get in touch Connect LinkedIn Podcast Dr. GPCR Calendly ©2023-2025 All rights reserved by FindYooour, LLC & Dr. GPCR Corp Proudly created with Wix.com

<< Back to podcast list Strategic Partner(s) Dr. Marta Filizola About Dr. Marta Filizola Dr. Marta Filizola is the Sharon & Frederick A. Klingenstein-Nathan G. Kase, MD Professor in the Departments of Pharmacological Sciences, Neuroscience, and Artificial Intelligence and Human Health, as well as the Dean of The Graduate School of Biomedical Sciences at the Icahn School of Medicine at Mount Sinai, in New York, USA. The overall goal of her research program is to obtain rigorous mechanistic insights into the structure, dynamics, and function of important classes of membrane proteins and prominent drug targets, including G protein-coupled receptors (GPCRs), transporters, channels, and 3 integrins. To this end, her lab uses several computational structural biology tools and rational drug design approaches, ranging from molecular modeling, bioinformatics, cheminformatics, molecular dynamics simulations, free-energy perturbations, machine learning, etc. A native of Italy, she received her Bachelor’s and Master’s degrees in Chemistry from the University Federico II in Naples. She pursued a Ph.D. in Computational Chemistry at the Second University of Naples and a postdoctorate in Computational Biophysics at the Molecular Research Institute in California, USA. Dr. Marta Filizola on the web Icahn School of Medicine at Mount Sinai Filizola Lab Wikipedia Twitter Linkedin ResearchGate Google Scholar Orcid PubMed Dr. GPCR Ecosystem Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

In this short resilience conversation, Dr. Graciela Pineyro shares what a forced lab shutdown taught her about prioritization, remote lab meetings, and running a research program across closed borders. << Back to podcast list Strategic Partner(s) Graciela Pineyro: Resilience, Lab Life, and the Zoom Effect Research doesn't pause neatly. In March 2020, Dr. Graciela Pineyro — a principal investigator at CHU Sainte-Justine in Montreal studying GPCR signaling — watched her lab close from one day to the next. This short resilience conversation, part of a Dr. GPCR Podcast series capturing the realities of scientific life, returns to Dr. Pineyro several months into the shutdown to hear what she learned. The discussion moves across three overlapping questions: how a forced pause reshapes scientific prioritization, how remote lab meetings alter who speaks up and why, and what it costs a scientist personally to keep a lab running across a closed international border. For Dr. Pineyro, whose husband remained in Uruguay for the duration of the shutdown, the scientific work and the human cost were never separate conversations. What emerges is a quiet argument that the structural shifts the pandemic forced — project planning in self-contained blocks, flatter meeting dynamics, planned reflection time — may deserve to survive the return to the bench. About the Guest Dr. Graciela Pineyro is a principal investigator at CHU Sainte-Justine in Montreal, where her research group works on GPCR signaling. She is a returning guest of the Dr. GPCR Podcast; her earlier episode covers her scientific profile in depth, including her research trajectory, laboratory focus, and contributions to the field. This resilience conversation captures her voice not as a researcher presenting results, but as a PI speaking candidly about how her program is navigating a moment no one planned for. Scientific Themes of the Conversation Forced pause as a prioritization tool — How closure reveals what a lab would otherwise never stop to question. The democratizing effect of remote meetings — Why some lab members speak more freely from home than they ever did in person. Experimental planning under uncertainty — Structuring projects into self-contained blocks so a lab can survive iterative shutdowns. The personal geography of modern science — What it costs a scientist when the research program and the family are in different countries. Civic responsibility in returning to the bench — Deconfining a research center slowly, with planning for possible return to closure. Key Insights from the Conversation The pause was never just a pause. Dr. Pineyro frames the shutdown not as lost time but as a rare moment of recul — the French word for a step back that allows for perspective. She talks about finally being able to ask which projects deserved to be finished first, second, third. The question was always there; the pause was what forced it to be answered. Zoom did not flatten the lab. It flattened the hierarchy of who gets heard. The most striking observation in the conversation: lab members who rarely spoke up during in-person meetings began contributing more on Zoom. Dr. Pineyro notes she isn't sure why — something about speaking from home, something about reduced interpersonal threat. But the finding is sharp enough to take seriously when in-person dynamics return. Planning in blocks is a form of resilience. The lab restructured projects into discrete, self-contained units — each one designed so that if the research center closed again, the team would still have something to analyze, something to write. This is operational wisdom that long outlives the pandemic. The personal cost doesn't stay outside the lab. Dr. Pineyro speaks openly about her husband being stuck in Uruguay since March, missing their planned reunion, hoping for Christmas. She does not separate this from the scientific conversation — and the listener shouldn't either. Running a lab during the pandemic was rarely just a scientific problem. Returning to the bench is a decision, not a default. The research center was deconfining at 20% capacity the week of the recording. Dr. Pineyro frames reopening as something her team is taking "civically with responsibility and a grain of salt" — acknowledging that back-and-forth closures may be the new baseline. That framing, made months before it became the standard narrative, is worth noticing. Some pandemic-era practices deserve to survive. The implicit argument threaded through the whole conversation: the structural shifts forced by the shutdown — planned reflection, remote meeting inclusion, block-based project design — may be worth keeping. Not because the pandemic was good for science, but because normal lab life had quietly suppressed some of the things the pause made visible. Episode Timeline Timestamps were generated using AI for readability. 00:00 Introduction and 2020 Summit announcement 01:45 Welcoming a returning guest 02:02 How COVID reshaped the lab and the personal cost 03:30 Using forced pause for prioritization 04:10 Planning experiments in self-contained blocks 04:47 The Zoom effect — quieter voices speaking up 05:49 Closing reflections 06:01 Outro Selected Quotes "One day we were doing experiments, and the next we had to close. We have to go back now and start from scratch." "Zoom democratizes the world. People that usually do not speak so much in the lab meetings were speaking a little bit more through Zoom." "We are sort of thinking in advancing our projects in sort of blocks, closing some questions very tightly. So if we are sent back home, at least we have something to work on." "We are all prepared to take this civically with responsibility and also with a grain of salt, knowing that we might have to be going back and forth for a while before everything goes back to normal." About this episode: Dr. Graciela Pineyro is a professor of pharmacology at the department of pharmacology and physiology of the University of Montreal. She has done extensive work on the molecular pharmacology of opioid receptors and is currently focusing on the pharmacology of cannabinoids in the context of pain. We chatted about how the current pandemic has affected her personally and professionally. Dr. Graciela Pineyro on the web Dr. Graciela Pineyro on LinkedIn Dr. Graciela Pineyro - University of Montreal Dr. Graciela Pineyro - CHU Ste-Justine Research Centre Pineyro Lab Publications on Google Scholar Pineyro Lab on Pubmed Dr. GPCR Ecosystem Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Strategic Partner(s) Developing new tools to uncover GPCR signaling patterns with Remi Janicot About Remi Janicot I was born in Paris (France) and grew up in Europe until I was 18. After graduating high school, I moved to America to pursue my passion for basketball while continuing high level studies. I played collegiate basketball and earned my bachelor’s at Ursinus College, a small school around Philadelphia where I graduated from in 2018. After that, I worked at Johns Hopkins in Baltimore as a research assistant investigating mechanisms and treatments for pediatric epilepsy. With my background in neuroscience, the lab of Dr. Mikel Garcia-Marcos seemed like a good fit as GPCRs are integral to the functioning of the nervous system (and much more). My particular projects revolve around developing new tools to study GPCR activity in ways that were not previously possible. This research has led to a first-author Cell article on the development of a new biosensor platform called ONE-GO biosensors. Overall, the lab works on diverse models and diseases, and has developed a wide array of tools to dissect GPCR/G protein signaling which I would be happy to discuss. Remi Janicot on the web Chobanian & Avedisian School of Medicine Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Strategic Partner(s) Dr. Françoise Bachelerie About Dr. Françoise Bachelerie " FB leads a team at Paris-Saclay University with expertise in immunology and virology related to Host/Virus interactions and GPCR function. The team’s projects are devoted to the activation/function of CXCR4-ACKR3 (CXCR7) receptors of the CXCL12 chemokine, key effectors of the immune system, including their role in immunological disorders (e.g. WHIM syndrome) and in the innate control of the life cycle of papillomavirus, which are commensal inhabiting the healthy human epithelium (virome) while presenting an oncogenic potential that remains a major health concern. FB is recognized for her expertise and pioneering works in the field of biological and pathological functions of chemokines and their receptors, for which she made important breakthroughs regarding the CXCL12/CXCR4/ACKR3 trio. In particular, FB contributed to the discovery that CXCL12 is the ligand for the CXCR4 receptor and can therefore prevent infection by the Human Immunodeficiency Virus (HIV). FB’ team has identified the orphan CXCR7/ACKR3 receptor as being the 2nd receptor for CXCL12, which behaves as a modulator of CXCL12/CXCR4 functions. FB is a member of various international committees in the field, including the one that reviewed the standard nomenclature for chemokine receptors that are categorized into a large subgroup of G protein–coupled (GPCR) leukocyte chemotactic receptors (including CXCR4), and a smaller subgroup of atypical chemokine receptors (including the CXCR7/ACKR3). " Dr. Françoise Bachelerie on the web INSERM ResearchGate SciSpace Loop LinkedIn Dr. GPCR Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Strategic Partner(s) Exploring Career Paths in GPCR Research with Dr. Jacek Mokrosiński About Dr. Jacek Mokrosiński "Jacek is a Senior Scientist at Novo Nordisk specializing in molecular pharmacology and cell-based screening technologies. He works in a multidisciplinary Chemical Biology team based at the recently established US R&D hub in Lexington, MA. Originally from Łódź, Poland, Jacek completed his Master's degree in Biology, specializing in Biochemistry at the University of Łódź. He then moved to Denmark, where he trained at the University of Copenhagen under supervision of Professor Thue W. Schwartz, and worked closely with Dr Birgitte Holst studying structural and mechanistic properties of ghrelin receptor and GPCRs involved in regulation of metabolism. After completing his Ph.D., he pursued research in genetics of metabolic regulation at the Institute of Metabolic Science - Metabolic Research Laboratories at the University of Cambridge in the team led by Professor I. Sadaf Farooqi. His research aimed at understanding molecular mechanism through which rare genetic variation may lead to or protecting from excessive body weight gain. As part of Farooqi's team, he characterized a series of novel human genetic variants identified in several GPCRs associated with obesity and other metabolic diseases, including GPR10, Melanocortin 4, Serotonin 2C and TRH receptors. Since 2021, Jacek has been working at Novo Nordisk at its research sites in the UK (Oxford) and the US (Indianapolis, Indiana and most recently Lexington, Massachusetts). He is passionate about cell-based in vitro technologies to study mechanistic properties of GPCRs and understanding the dynamics of receptor signalling. He is an avid proponent of close collaboration between industry and academia." Dr. Jacek Mokrosiński on the web ORCID ResearchGate LinkedIn Twitter Dr. GPCR AI Summary AI-generated content may be inaccurate or misleading. Always check for accuracy. Quick Recap Yamina and Jacek discussed their experiences with name mispronunciations, cultural differences, and the importance of a multidisciplinary approach in drug development. They also shared their career journeys, emphasizing the value of being open-minded, proactive, and embracing new opportunities. Lastly, they discussed their research interests, particularly in the field of GPCR, and the importance of method development, integrity, and honesty in scientific research. Next Steps Jacek will collaborate with Alex Romeo on a podcast about transitioning to the industry. In future talks and interviews, Jacek will share his stories and advice about GPCRs. Yamina will schedule a future talk with Jacek about GPCRs as therapeutic modalities. Summary Embracing Cultural Differences and Collaboration Yamina and Jacek shared their experiences with name mispronunciations and variations and discussed the importance of embracing cultural differences. They also discussed their professional backgrounds, highlighting the benefits of a multidisciplinary approach in drug development and the importance of collaboration between academia and industry. They talked about their shared passion for advancing science and improving patient outcomes, and their early interests in science and chemistry. They also shared their appreciation for documentaries showcasing manufacturing processes and the value of true experimentation in scientific research. Jacek's Career Journey and Advice Jacek and Yamina discussed Jacek's career journey, focusing on his experiences, challenges, and lessons learned. Jacek highlighted the importance of being open-minded and proactive, emphasizing that he learned by doing rather than taking specific courses. He also underscored the role of the people around him, expressing gratitude for their guidance and support. His advice was to be ready for changes and to embrace opportunities as they arise. Jacek's career path, which led him from Poland to Denmark and then to the US, exemplified his advice in action. Passion for Science and Career Journeys Yamina and Jacek discussed their passion for science and how it led them to their current careers. Jacek shared his experience of working with Piketa and how he found a job in Seda's lab at Cambridge, where he could immediately contribute due to his technical skills. Yamina agreed with Jacek's sentiments and spoke about her own journey, expressing her happiness in discussing science and reading papers. They emphasized the importance of finding a job that aligns with one's interests and strengths and being open to opportunities. They also highlighted the need for a work-life balance and the joy of a well-done job. Embracing Networking for Professional Growth Jacek and Yamina discussed the importance of building a network and being open to new opportunities. Jacek realized that being introverted doesn't mean he can't benefit from networking and interaction with others. He also highlighted the benefits of attending conferences and engaging with colleagues, sharing examples of how such interactions led to collaborations and new opportunities. Yamina agreed, emphasizing the importance of mental preparation and embracing different social situations, both virtual and in-person. They underscored the value of these interactions for professional growth and encouraged others to adopt a proactive approach to networking. Building Professional Connections Strategies Yamina and Jacek discussed the importance of building professional connections and strategies for introducing oneself to potential contacts. They emphasized the need to be mindful of the other person's time, provide clear explanations for the purpose of the connection, and offer something of value in return. They also highlighted the advantages of using LinkedIn as a tool for networking and the significance of personalizing messages to make a lasting impression. GPCR Research Interests and Collaborations Yamina and Jacek had a deep and engaging discussion about their research interests and achievements, particularly in the field of GPCR. Jacek shared his fascination with the growth hormone secretion receptor and the melanocortin 4 receptor, and their roles in regulating body weight and growth. Yamina, in turn, talked about her work on melanocortin receptors and an upcoming collaboration with a postdoc scientist. They also highlighted the importance of method development, integrity, and honesty in scientific research. The discussion revealed their interest in GPCRs as therapeutic modalities and possible future collaborations. Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

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Dr. Antonella Di Pizio on building computational models for GPCRs with almost no crystal structures and almost no ligands — bitter taste receptors, odorant receptors, and the trace amine-associated receptors that may one day treat depression. << Back to podcast list Strategic Partner(s) Antonella Di Pizio: Computational Pharmacology of Taste and Olfactory Receptors Chemosensory receptors — bitter taste receptors (TAS2Rs), odorant receptors, and trace amine-associated receptors (TAARs) — sit among the most structurally underserved families of class A GPCRs. No crystal structures exist for most of them, sequence identity within the TAS2R family hovers between 15% and 19%, and several members are effectively orphans with only a handful of known ligands. Yet these receptors appear to govern far more than flavor and smell. Bitter taste receptors have been identified in the heart and intestine, olfactory receptors in the brain, and the TAARs sit at the interface between neurotransmission and chemoreception — with clinical interest emerging in schizophrenia, neurodegeneration, depression, and anxiety. In this conversation, Dr. Antonella Di Pizio — who leads the computational pharmacology group at the Leibniz Institute for Food Systems Biology at the Technical University of Munich — describes how she uses homology modeling, docking, molecular dynamics, and iterative mutagenesis to probe these systems. For her, the work isn't abstract: she spent five months staring at empty protein crystals during her PhD, and learned that the distance between giving up and seeing a ligand inside a binding pocket can be measured in weeks. About the Guest Dr. Antonella Di Pizio is an independent research group leader in computational pharmacology at the Leibniz Institute for Food Systems Biology at the Technical University of Munich, where she was the first group leader appointed to the institute's newly-formed in-silico department. Trained as a medicinal chemist at the University of Chieti in Italy, she completed her PhD in computational medicinal chemistry before spending a formative period in Gerhard Klebe's structural biology lab in Marburg. Her postdoctoral training in Masha Niv's lab in Israel marked her first work on GPCRs, specifically the bitter taste receptors (TAS2Rs). Her group now studies taste receptors, odorant receptors, and trace amine-associated receptors using a combination of homology modeling, docking, molecular dynamics, and virtual screening — tightly integrated with experimental mutagenesis and functional assays through collaborations. Scientific Themes of the Conversation Chemosensory receptors as a frontier for GPCR drug discovery Trace amine-associated receptors (TAARs) and their neurological relevance Promiscuity and selectivity within the bitter taste receptor family Iterative integration of computational modeling with experimental mutagenesis Ectopic expression of taste and odorant receptors beyond their namesake tissues Persistence, career building, and what it means to lead a first-generation computational group Key Insights from the Conversation The first in-silico group inside a food biology institute. When Dr. Di Pizio arrived in October 2018, she founded the first computational group in an institute whose original identity had been food chemistry. Her job description — computational pharmacology — was itself an attempt to name a new interface between food chemistry and receptor pharmacology. TAARs look more classical than most chemosensory GPCRs — and that matters for modeling. Unlike bitter taste receptors, which share only 5–10% sequence identity with available structural templates, the TAARs share roughly 30% identity with the β2-adrenergic receptor. That proximity transforms what's computationally tractable, making homology modeling genuinely predictive rather than speculative. TAAR5 is effectively orphan — and may be a new kind of antidepressant target. With only about five known agonists, TAAR5 sits in a pharmacological twilight. Yet knockout mice show anti-anxiety, anti-depressant phenotypes, and expression of the receptor in the brain alters serotonin levels. An antagonist of TAAR5 could, in principle, seed a new class of psychiatric therapy. Bitter is not only about taste. TAS2Rs have been identified in the heart and intestine; olfactory receptors in the brain. What they do there remains largely unknown. But evidence is accumulating that bitter taste receptors participate in innate immunity, recognizing bacterial secretions that happen to register as bitter on the tongue. A bitter receptor is already in phase 2 clinical trials. Isohumulones — the hop-derived bitter compounds that give beer its characteristic flavor — have shown anti-diabetic activity in clinical development. The receptor responsible, TAS2R1, is expressed in the intestine. The drug candidate was never designed as a bitter receptor ligand; the receptor was identified post-hoc. Computational pharmacology is not a downstream silo. Dr. Di Pizio's workflow is deliberately iterative: build the model, predict binding-site residues, send them out for mutagenesis, fold the experimental results back into the model, rebuild. Collaborators are not recipients of finished predictions — they are partners embedded in the modeling loop itself. Five months of empty crystals, then a ligand. During her PhD, Dr. Di Pizio spent five months crystallizing carbonic anhydrase 2 with small molecules and seeing only empty proteins at the synchrotron. Two weeks before her internship ended, after changing every parameter she could think of, she finally saw her ligand inside the binding pocket. She describes it as the happiest moment of her scientific life — and, for a computational chemist, a lasting lesson in what sits behind every coordinate file. Episode Timeline Timestamps were generated using AI for readability. 00:00 Introduction 01:46 Computational pharmacology inside a food systems institute 03:13 From medicinal chemistry to bitter taste receptors 05:44 Trace amine-associated receptors on the edge of neuroscience 12:34 Anosmia and viruses of the olfactory system 19:03 Inside a computational workflow for orphan receptors 29:14 Bitter receptors in the heart and gut 30:43 A bitter receptor in phase 2 clinical trials 43:40 Five months of empty crystals 55:56 Rebuilding a research group during lockdown Selected Quotes "We don't have any crystal structures. So the research is more food-oriented and food-chemistry-oriented — this is why we have knowledge about compounds, but we don't have a lot of knowledge about quantitative structure-activity relations based on the structure of the receptor." "For five months, my protein was always empty at the X-ray. And two weeks before I had to leave, I finally saw my ligand inside the pocket. For me, I think that was my happiest moment in my life." "You share your research goal with your collaborators. They are more partners than collaborators." "Think of being an investor of yourself. Read, study, do the most as you can to learn as much as you can — not only scientifically, but also networking. Be passionate on exactly the field that you work on, because this will be extremely useful later." 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 Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

Expert support, trusted CROs, and ready-to-use tools to accelerate GPCR drug discovery, reduce risk, and advance your discovery-stage projects. Dr. GPCR Foundry: Accelerate GPCR Drug Discovery Move from idea to insight—faster, smarter, and with confidence. Partner with our nonprofit team for expert guidance, trusted CRO collaborations, and field-tested tools that de-risk your GPCR programs and keep momentum strong. 👉 Book a Free 30-min Strategy Call Select your Challenge... ↑ Pick your challenge to see tailored solutions. Yamina's Corner Expert strategic and scientific consultancy for GPCR-focused biotechs, VCs, and CROs. From pipeline acceleration and investment de-risking to CRO differentiation — turning GPCR complexity into clear, actionable direction. Book Your Free Strategy Call GPCR University Team Membership Dr. GPCR University for your whole organization. Unified access to the full course library, live masterclasses, and community — so your team builds from the same expert-led foundation and compounds knowledge. Get Team Access Terry's Pharmacology Corner Team Membership The team tier of Terry's Corner. Give every scientist on your team access to Dr. Kenakin's weekly insights and AMAs — building shared language around GPCR data and pharmacological decisions. Get Team Access GPCR University Expert-led courses spanning GPCR drug discovery — from receptor biology to translational pharmacology. Includes live masterclasses, a full course library, and community access. Built for working scientists. Explore the University Terry's Pharmacology Corner Weekly expert content and live AMAs led by Dr. Terry Kenakin. Translates complex GPCR pharmacology into practical understanding you can apply to data interpretation, lead optimization, and candidate selection. Explore Terry's Corner Timeline Strategy Strategic workshops that replace trial-and-error with proven frameworks for biotech growth. Real-world case studies and data-driven models for pipeline prioritization, resource allocation, and milestone planning. Explore Timeline Strategy Strategic Media Partnership A premium, limited partnership (12 spots/year) that positions your company as a leader within the Dr. GPCR ecosystem. Gated content, launch campaigns, and strategic co-creation — a mission-aligned collaboration, not a media buy. Apply for a Partnership Spot CRO Bank A curated directory of GPCR-specialized CROs and technology partners. Find the right service provider for your assay, screening, or discovery needs — without wading through generic directories. Explore CRO Bank For enterprise teams and custom engagements. Find the right collaboration model for your program. Book a Strategy Call → Our Core Support Areas Discovery Consulting & Strategy Expert guidance to de-risk projects, refine strategy, and drive scientific progress. Visibility for Solution Providers Strategic media partnerships that connect your company with biotech innovators and showcase your expertise Training & Upskilling Specialized, insight-packed courses designed for discovery-phase GPCR teams. Tools & Resources Ready-to-use frameworks and resources tailored to the realities of discovery-stage GPCR work Our Partners Join these innovative organizations already benefiting from the DrGPCR Foundry. Book Plan Your Next Move in GPCR Discovery Meet directly with Dr. Yamina Berchiche for a focused strategy conversation to align your goals, uncover opportunities, and map your next steps. Let's move your GPCR discovery program forward. Wherever you are in your discovery journey, the Foundry helps GPCR biotech companies move faster and reduce risk. Let's discuss your next step.

<< Back to podcast list Strategic Partner(s) Dr. Ralf Jockers About Dr. Ralf Jockers Ralf Jockers studied in Cologne and received a Ph.D. in biotechnology and biochemistry from the University of Braunschweig, Germany. For postdoctoral training, he joined the laboratory of Dr. Strosberg AD in France, where he worked on the regulation of ß-adrenergic receptors. He is the Research director at INSERM with a specific interest in G protein-coupled receptors by developing original BRET and TR-FRET assays. His laboratory is currently located at the Institute Cochin – Inserm (Paris, France). His laboratory was among the first to demonstrate the oligomerization of GPCRs. He showed the formation of melatonin receptor heteromers in vitro and in vivo and their importance in retinal physiology. He established the concept of ligand-independent functions of orphan receptors in heterodimers with other GPCRs. He discovered multiple rare and loss-of-function variants of the MT2 melatonin receptors that are associated with type 2 diabetes (TD2) development. Many MT2 variants are biased and their defects are signaling pathway-specific opening new perspectives for T2D treatment and precision medicine. His lab was among the first to discover mitochondrial functions of GPCRs. He was the director of the French network of GPCRs (GDR-3545), currently directs the International Research Network (IRN) i-GPCRnet of the CNRS, is chair of IUPHAR « Melatonin receptor » sub-committee, Editor-in-Chief of « Frontiers in Cellular Endocrinology » and AE of « J Pineal Research”. He is a highly cited researcher – 2019 and 2020 identified by Clarivate Web of Science ™. Dr. Ralf Jockers on the web Jockers Lab WGDR-3545 Pubmed Dr. GPCR Ecosystem Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Strategic Partner(s) Dr. Prasenjit Saha About Dr. Prasenjit Saha I conducted my doctoral research at the Indian Institute of Science, Bangalore, India, to investigate the mechanisms behind rare mitochondrial diseases, which can lead to heart failure, muscle fatigue, and neurodegenerative disorders. I am now working at the Cleveland Clinic in Ohio, USA, studying the gut microbiome and its impact on cardiovascular disease (CVD). Specifically, I am interested in understanding dysregulated G-protein coupled receptor (GPCR) signaling linked to atherosclerosis and diabetes. My research goal is to identify novel cellular target receptors of human gut microbe-derived metabolites that are pathologically linked to CVD. Discovering these receptors would be a significant breakthrough in cardiovascular biology as they could be targeted for therapeutic purposes. During my post-doctoral research, I was part of a study that identified the receptors of a novel human gut microbe-derived metabolite called phenylacetylglutamine (PAG), which is linked to cardiovascular disease. This study demonstrated that PAG is a potential diagnostic marker for CVD as it causes serious fatal conditions such as thrombus formation, which can block blood vessels. In this study, I discovered adrenergic receptors (α2A, α2B, and β2-adrenergic receptors) that serve as the gut microbial metabolite (PAG) receptor and characterized the receptor-metabolite interaction. More recently, I have shifted my focus to identifying allosteric modulators of host G-protein-coupled receptors (GPCRs) that contribute to cardio-metabolic disorders. Traditional drug discovery efforts have focused on agonists and antagonists that bind to the orthosteric site of the receptor. However, the pursuit of allosteric modulators has gained attention as they have the potential to fine-tune cellular responses with greater selectivity among the subtypes of GPCRs. My long-term plan is to conduct research in the field of receptor biology, with a focus on GPCRs. They are the largest, most versatile, and most ubiquitous class of plasma membrane receptors and serve as targets for more than one-third of all prescribed drugs currently used in the treatment of human diseases all over the world. Dr. Prasenjit Saha on the web Google Scholar Pubmed LinkedIn Dr. GPCR Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Strategic Partner(s) Nicole Perry-Hauser About Nicole (Nicki) Perry-Hauser I am a postdoctoral research fellow endeavoring to build a productive, independent scientific research career in adhesion G protein-coupled receptor (aGPCR) biology. My long-term research interests involve resolving signaling pathways downstream of aGPCRs and establishing how/if these receptors’ adhesive properties influence signaling events, and in turn, whether signaling impacts synapse formation and neuronal wiring. Mutations in aGPCRs have been linked to various neuropsychiatric phenotypes, and my work will provide a basis for understanding aGPCR biology in the nervous system. Nicole (Nicki) Perry-Hauser on the web LinkedIn Research Gate Pubmed Dr. GPCR Ecosystem Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Strategic Partner(s) You never know where your GPCR takes you with Dr. Brian Hudson About Brian Hudson Brian is a lecturer in the School of Molecular Biosciences at the University of Glasgow. He has more than 20 years of experience in GPCR, primarily focused on drug discovery and developing new tools to study this receptor family. He leads a research group that is focused on understanding the pharmacology and function of a group a GPCRs that are activated by metabolic intermediates. Brian Hudson on the web University of Glasgow Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

Cheloha builds nanobody-GPCR ligand conjugates that rescue weak peptides, engineer receptor selectivity, and probe endosomal signaling at NIH. << Back to podcast list Strategic Partner(s) Ross Cheloha: Nanobody-GPCR Conjugates and the Engineering of Receptor Selectivity The parathyroid hormone receptor sits at the intersection of calcium homeostasis, bone metabolism, and a set of pharmacological questions that have resisted clean resolution for decades. How does receptor conformation shape the duration of downstream signaling? Why do some ligands continue activating from the endosome while others don't? And can selectivity for one receptor subtype be engineered without redesigning the ligand from scratch? Ross Cheloha approaches these questions from a chemical biology perspective - using synthetic peptide analogs, camelid single-domain antibodies (nanobodies), and bifunctional conjugates that split the binding event into two independently tunable pieces. In this conversation, he describes how attaching a moderately active peptide to a receptor-targeted nanobody can boost potency by up to 10,000-fold, and how the selectivity of the nanobody - not the ligand - is what engineers receptor subtype specificity. For Cheloha, the motivation traces back to a habit he carried from childhood: writing reports on exotic diseases and what scientists were doing to treat them. The experiment that mattered most was not a drug candidate or a clinical advance - it was a designed conjugate that worked when there was no clear reason it had to, every control behaving exactly as expected. About the Guest Ross Cheloha is a tenure-track investigator at the National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK) at the National Institutes of Health. His research combines peptide chemistry, chemical biology, and nanobody engineering to build mechanistic tools for studying GPCR signaling, with a particular focus on the parathyroid hormone receptor and its downstream consequences for calcium homeostasis and bone biology. Trained in the Gelman lab at the University of Wisconsin-Madison and later in the Ploegh lab at Harvard Medical School and Boston Children's Hospital, he developed methods for covalently functionalizing camelid single-domain antibodies with synthetic ligands to probe receptor conformation, endosomal activity, and the duration of signaling responses. His work has demonstrated that nanobody-ligand conjugates can rescue pharmacologically weak peptides, engineer receptor subtype selectivity, and open mechanistic questions that conventional ligand design cannot easily address. Scientific Themes of the Conversation Peptide analog engineering and the stabilization of GPCR ligands using non-natural amino acids Receptor conformation selectivity: G-protein coupled versus uncoupled states and their downstream consequences Camelid single-domain antibodies (nanobodies) as a platform for GPCR chemical biology Nanobody-ligand conjugates as bifunctional tools for potency rescue, selectivity engineering, and mechanistic dissection Duration of signaling and endosomal GPCR activity: what wash-and-measure paradigms have been missing Tissue-specific receptor targeting and the pharmacological logic of reducing GPCR side effect profiles Key Insights from the Conversation 1. Conformation selectivity changes the duration of the signal PTH receptor exists in G-protein coupled and uncoupled states, and peptide analogs incorporating non-natural amino acids show differential affinity for each conformation. The analogs that preferentially bind the uncoupled state produce markedly prolonged signaling responses - in cells and in animal experiments - compared to ligands that do not. The biology may have been using this distinction all along: two natural ligands for the same receptor already show subtly different conformation preferences and different physiological profiles in vivo. 2. One nanobody, four orders of magnitude Connecting a short, weakly active PTH fragment (11 amino acids, approximately 100 nanomolar potency) to a receptor-targeted nanobody produced sub-nanomolar potency in cell-based assays - an improvement of up to 10,000-fold from a single engineering step. The working model is that the nanobody anchors the conjugate at the receptor surface, positioning the ligand for activation that would otherwise be too transient to drive a strong response. The selectivity comes from the nanobody's binding specificity, not from chemical modification of the peptide itself. 3. Selectivity without redesigning the drug PTH 1-34 activates both PTHR1 and PTHR2 with high potency, and engineering subtype selectivity through chemical modification of the peptide is technically demanding. Attaching a short PTH fragment to a PTHR1-selective nanobody produces a ligand selective for that subtype; the same fragment attached to a PTHR2-selective nanobody redirects it entirely. The implication generalizes: wherever a selective nanobody exists for a GPCR target, it can be used to introduce specificity into an otherwise promiscuous ligand without restructuring the pharmacophore. 4. Endosomal signaling is being missed Conventional GPCR assay design - stimulate, wash, measure endpoint - systematically misses signaling that continues after receptor internalization into the endosome. Cheloha's position is that the standard assumption linking tighter binding to longer signaling is incomplete. Endosomal activity is a distinct mechanistic process, and the tools to dissect it - bifunctional conjugates with independently tunable affinity components - are not available with conventional single-piece ligands. This is the central mechanistic priority he is bringing to his NIH lab. 5. Tissue-specific targeting as a strategy for reframing side effects The primary dose-limiting side effect of PTH-based therapies is hypercalcemia, driven in part by receptor activity in kidney tissue rather than bone. Connecting a ligand to a tissue-targeted nanobody could restrict receptor activation to bone and reduce unwanted calcium release. The pharmacological logic is sound, and the engineering framework to test it exists. Whether it holds in vivo remains to be demonstrated - Cheloha is careful to say so - but it represents a genuinely new angle on a long-standing problem in PTH pharmacology. 6. The experiment that had no reason to work - and did Among three scientific aha moments Cheloha described, the one with the clearest forward momentum was the first successful nanobody-PTH conjugate - designed not because a clear rationale existed, but because he wondered whether it was possible. No hypothesis guaranteed the result. Every positive and negative control performed exactly as designed. The conjugate worked. That single experiment, Cheloha said, opened more mechanistic doors than anything he had produced before - and it came directly from experience-built intuition rather than hypothesis-first design. Episode Timeline Timestamps are AI-generated from the transcript and are approximate. Verify against the final edited video before publishing. 00:00 Introduction 01:58 From pharmacy school to chemical biology: how the research path took shape 08:12 Academia versus industry - why freedom to ask non-translatable questions matters 09:43 The academic job search: 65 applications, six interview trips, and landing NIH 14:20 How a peptide chemist found the PTH receptor - and a collaborator who changed everything 17:20 Non-natural amino acids, protease stability, and receptor conformation selectivity 21:40 PTH receptor pharmacology: calcium spikes, bone biology, and why long-acting isn't always better 23:22 A detour into immunology and the discovery of camelid nanobodies 25:45 The first nanobody-GPCR ligand conjugate and an unexpected 10,000-fold potency gain 30:32 Engineering receptor subtype selectivity without redesigning the pharmacophore 36:10 Mechanistic priorities at NIH: endosomal signaling and duration of signaling 40:25 Are GPCRs still a good drug target? Biased agonism, endosomal signaling, and what remains 47:13 Three aha moments: first data, an email from Gardella, and the conjugate that worked Selected Quotes "I just thought of something - hey, I wonder if this would work. There was not necessarily an underlying scientific rationale for trying this. I wasn't thinking this is going to be a new drug. I just thought of something and said, I wonder." "I was convinced that I designed something that worked where it was not at all obvious that it was going to work. And that just opened up so many doors." "I don't think tight binding equals longer signaling is necessarily the whole story. I think in large part it's been missed." "Anything you can contribute to that end is hopefully going to provide a step forward in understanding disease and treating disease. The freedom and creativity - that's what I was really attracted to." About this episode Dr. Ross Cheloha is an Investigator at the National Institutes of Health in the Laboratory of Bioorganic Chemistry in Bethesda, MD, where he started in October 2020. He completed his postdoctoral training at MIT and Harvard Med School in the lab of Hidde Ploegh , where he developed new applications of single-domain antibodies (nanobodies). He earned his Ph.D. in Chemistry at the University of Wisconsin-Madison in the lab of Sam Gellman on the study of analogs of the GPCR peptide ligand parathyroid hormone. Work in his independent laboratory is focused on developing new pharmacological tools via chemistry and protein engineering to interrogate GPCR signaling. Ross and I chatted about his work and transition to an independent investigator; join me to learn more about class B GPCRs and Dr. Cheloha’s work. Dr. Ross Cheloha on the web NIDDK Cheloha Lab Google Scholar LinkedIn Twitter ResearchGate Dr. GPCR Ecosystem Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

Get one year of free Dr. GPCR Premium access for your entire academic lab. Teach a course at Dr. GPCR University and unlock expert resources, training, and tools. Academic Team Access Program One Year of Dr. GPCR Premium — Free for Your Entire Lab Empowering academic discoveries with industry-grade GPCR resources. Why We Created This Program? Your research group plays a critical role in advancing GPCR science. We want to support academic labs with the same high-quality tools, courses, and insights used by leading biotech teams—without financial barriers. The Dr. GPCR Academic Team Access Program gives your entire lab one year of Premium membership at no cost, in exchange for contributing to the community’s shared knowledge base through teaching . How does it work? No Cost, No Hidden Requirements The program is 100% free for academic labs who contribute as instructors. No recurring charges. No credit card required. Your Whole Lab Gets One Year of Premium Access Once approved, every member of your team receives free Premium access for 12 months, including: Full access to Dr. GPCR Masterclasses & University Vault Weekly News extended editions Exclusive event recordings, slides, and community decks Premium research insights and ecosystem reports Priority access to certain events and AMAs A Member of Your Lab Teaches at Dr. GPCR University Contribute your expertise by teaching a topic, workshop, or course within the Dr. GPCR University. Format is flexible — we work with your availability. Become part of the Dr. GPCR University Instructor community Learn More & Join the Program To keep things simple, we created a single guide that covers: Eligibility guidelines Teaching formats & examples Instructor expectations Course creation support Application steps Timeline & onboarding What your team receives Renewal options 👉 Everything is explained here *This link takes you to a dedicated page with all the details. Book Ready to Unlock Premium for Your Entire Lab—At No Cost? 👉 Learn More & Get Started Meet directly with Dr. Yamina Berchiche for a focused strategy conversation to align your goals, uncover opportunities, and map your next steps.

Explore Martin Marro’s impact on GPCR drug discovery, assay innovation, and translational pharmacology bridging academia, pharma, and biotech. << Back to podcast list Strategic Partner(s) GPCR Assay Strategy, Bias, and Translational Drug Discovery This episode features Dr. Martin Marro, currently Executive Director and Head of Cell Pharmacology at Eli Lilly’s Obesity Research Group. Dr. Marro’s career spans big pharma and biotech, encompassing functional assay development, GPCR internalization research, and both small molecule and biologic drug discovery. He discusses his formative scientific experiences, critical decision points moving from academia into industry, and his role leading and shaping multidisciplinary teams for screening and innovative therapeutics targeting metabolic and cardiovascular diseases. The conversation explores the realities of using fluorescence-based assays, the challenge of translating in vitro pharmacology to in vivo models, lessons on bias agonism, and novel approaches in antibody discovery for GPCR targets. Dr. Marro’s path highlights the strategic and methodological pivots essential for driving projects into the clinic. For a deeper dive into modern GPCR research and tools, explore more episodes of the GPCR Podcast and discover Dr. GPCR Premium resources. Why This Matters? How advanced assay design is essential for translating cell-based GPCR signals to therapeutic outcomes. Why strategic flexibility in exploring non-canonical signaling pathways is critical for GPCR-targeted drug discovery. What learning from “failed” screens can reveal about receptor pharmacology and species selectivity. The moment when bias agonism and receptor trafficking concepts shifted industry standards for functional assays. How integrating antibody-based modalities has expanded options for hard-to-drug GPCR targets. Why persistent scientific questioning and collaborative networks accelerate GPCR innovation across disease areas. Who Should Listen? This episode is relevant to anyone navigating the complex landscape of GPCR research and translational pharmacology. Those facing disconnects between in vitro functional data and in vivo efficacy in GPCR programs. Researchers refining strategies for high-throughput screening or exploring biased signaling. Teams expanding into antibody or biologic modalities for challenging GPCR targets. Scientists seeking practical advice on career pivots between academia, pharma, and biotech. About Martin Marro Dr. Martin Marro leads the Cell Pharmacology group in the Diabetes, Obesity and Complications Therapeutic Area at Lilly's Seaport Innovation Center in Boston. His scientific training included a PhD at the International Center for Genetic Engineering and Biotechnology, followed by an industrial postdoctoral fellowship at GSK, where he entered the GPCR field and became proficient in aptamer selection and cell signaling assays. Dr. Marro’s career advanced through roles at Novartis and Tectonic Therapeutic, contributing to projects across key therapeutic areas—spanning metabolic, cardiovascular, and gastrointestinal diseases. With over two decades in drug discovery, he has established expertise in early phase functional assay development, small molecule and biologics research, and team leadership through high-profile programs. Awarded patents and a proven record in both target and pathway identification, his drive centers on integrating rigorous pharmacology with translational impact while cultivating innovation and scientific growth within his teams. Guest on The Web LinkedIn Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Strategic Partner(s) Robert Laprairie About Dr. Robert Laprairie Dr. Robert Laprairie is an Associate Professor and the Saskatchewan Research Chair in Drug Discovery and Development in the College of Pharmacy and Nutrition at the University of Saskatchewan. The focus of his research is the molecular pharmacology of cannabinoids and cannabinoid receptors. He was the 2018 and 2021 recipient of the Young Investigator of the Year Awards from the British Pharmacological Society and International Cannabinoid Research Society (ICRS), respectively. In 2019 he became the Director of Education for the Canadian Consortium for the Investigation of Cannabinoids (CCIC) and now also serves as the organization’s President. Dr. Robert Laprairie on the web University of Saskatchewan Twitter Instagram ResearchGate Google Scholar Dr. GPCR Ecosystem Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Strategic Partner(s) Dr. Stephen Ferguson About Dr. Stephen Ferguson Dr. Stephen Ferguson is a Professor in the Department of Cellular and Molecular Medicine at the University of Ottawa. He did B.Sc. in biology at McGill University and received his Ph.D. under the mentorship of Dr. Brian Collier in the Department of Pharmacology and Therapeutics at McGill University (1994). He did his postdoctoral training with Dr. Marc G. Caron at Duke University (1994-1997), where he and his colleagues investigated the role of G protein-coupled receptor kinases and beta-arrestin in regulating G protein-coupled receptor endocytosis, trafficking, and signaling. He has held four Canada Research Chairs since 2001 and was previously a Heart and Stroke Foundation of Canada MacDonald Scholar (1998-2003) and Heart and Stroke Foundation of Ontario Career Investigator (2003-2016). He was a recipient of Canada's Top 40 under 40 award in 2004 and received Queen Elizabeth II, Diamond Jubilee Medal, in 2012. He has also received both Junior (2001) and Senior (2005) investigator awards from the Pharmacological Society of Canada. Most recently, in 2021, he was elected as a Fellow of the Canadian Academy of Health Science (FCAHS). His research career has focused on the investigation of the regulation of G protein-coupled receptors signaling mechanisms in health and disease. He currently holds multiple research grants from the Canadian Institutes of Health Research (CIHR) for his research investigating the role of metabotropic glutamate receptor signaling in Huntington’s and Alzheimer’s disease. Dr. Stephen Ferguson on the web Carlton University Canada Research Chairs Twitter ResearchGate LinkedIn Dr. GPCR Ecosystem Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

How a bell-shaped FSH dose-response curve led to one of the earliest demonstrations of biased GPCR signaling - and a decade of pushback from the field. << Back to podcast list Strategic Partner(s) Brian Arey: Discovering Signaling Bias at the FSH Receptor Biased signaling - the idea that a single receptor can preferentially activate one downstream pathway over another depending on how it is engaged - is now a central concept in GPCR pharmacology and drug design. But for the researcher who first encountered it not as a theory but as an anomalous bell-shaped dose-response curve in an FSH receptor assay, it arrived as a problem that needed explaining. Brian Arey, Director of Mechanistic Pharmacology at Bristol-Myers Squibb, traces the origins of that discovery to a glycosylation difference between pituitary-purified and insect-cell-expressed FSH - a difference that turned out to encode physiologically distinct signaling outputs. The broader argument Arey has spent his career developing is that biased signaling is not a GPCR-specific phenomenon but an evolutionarily conserved principle present across all receptor classes. That argument eventually became a book, co-authored with Terry Kenakin, that Arey dedicated to his children - not because they are scientists, but because he wanted them to understand what he spent his life doing and why it mattered. ABOUT THE GUEST Brian Arey is Director of Mechanistic Pharmacology within the Discovery and Optimization organization at Bristol-Myers Squibb, where he leads research spanning GPCR pharmacology, enzymology, and protein homeostasis pathways. A physiologist by training, he completed his doctoral work on circadian regulation of prolactin secretion at Florida State University before postdoctoral research at Northwestern, and has spent over 25 years in pharmaceutical drug discovery across Wyeth and BMS. His early work at Wyeth's Women's Health Research Institute produced foundational observations on biased signaling at the FSH receptor, which were among the first experimental demonstrations that a GPCR could signal through parallel G protein pathways in a ligand-dependent manner. He is the author of a 2014 book on evolutionarily conserved receptor signaling, co-written with Terry Kenakin and published through Elsevier. SCIENTIFIC THEMES OF THE CONVERSATION Biased signaling at glycoprotein hormone receptors - the experimental origin Glycosylation isoforms as physiological regulators of differential receptor signaling Evolutionary conservation of biased receptor function across receptor classes The physiologist's approach to mechanistic drug discovery The erosion of pharmacology training in pharmaceutical research - and why it matters Career navigation across academia, industry, and the blurring boundary between them KEY INSIGHTS FROM THE CONVERSATION The bell-shaped curve was a hypothesis, not an artifact When insect-cell-expressed FSH produced a bell-shaped dose-response curve instead of a sigmoidal one, the obvious interpretation was contamination or a production problem. Arey treated it as a signal. The glycosylation difference between the recombinant material and pituitary-purified FSH had altered the receptor's downstream signaling profile - and the bell shape was the read-out. It took a pertussis toxin experiment, borrowed conceptually from Tom Burris's dopamine receptor work, to demonstrate that FSH receptor was signaling through both Gs and Gi simultaneously, and that the two glycoforms were biasing the system differently. Forty years of unresolved biology had a signaling answer The existence of multiple glycosylated isoforms of FSH, LH, and other glycoprotein hormones had been recognized for decades, but their physiological significance was not understood. Arey's data offered a functional explanation: different glycoforms stabilize different receptor conformations, which recruit different intracellular effectors with different affinities, driving different physiological outcomes in target cells. What had looked like biochemical noise in circulating hormone pools was, in this framework, a mechanism for fine-tuned signaling control. If the controls are right, the data has to be trusted When a substantial portion of the literature responded to Arey's published data by calling it wrong, he called his graduate advisor. The advice he received - that if all controls have been run appropriately and the result still holds, you have to have confidence in your data - has remained his operating principle for three decades. That conviction did not resolve the argument quickly. The field took nearly a decade to come around. But the data held. Biased signaling is not a GPCR specialty - it is a conserved principle The central argument of Arey's 2014 book is that the bimodal structure of receptor signaling - a ligand-binding pocket with one inherent affinity, and a cytoplasmic effector-binding pocket with its own independent affinity, both modulated by the conformational state the ligand stabilizes - is not unique to GPCRs. The same logic applies to cytokine receptors, nuclear hormone receptors, and receptor tyrosine kinases. Arey arrived at this hypothesis in the mid-1990s, before the structural and mechanistic data existed to support it, and spent years watching the field gradually produce that evidence. Techniques are tools in a toolbox - not endpoints One of the formative intellectual influences Arey credits from his graduate training is the principle that no technology is intrinsically interesting - it is only interesting insofar as it can answer a scientific question. That orientation shapes how he runs his team at BMS: a healthy skepticism toward established methods, including antibody-based assays that he views as 50-year-old technology capable of improvement, and a standing question of whether the current tool is actually capturing the biology being studied. Drug discovery needs modulators more than it needs hammers Arey's philosophy of drug discovery is grounded in a view of human physiology as inherently variable - shaped by evolution, divergent across populations, and rarely susceptible to single-target solutions. He argues for a therapeutic strategy built around modulators that can be combined, rather than single agents designed to dominate a pathway. That argument is not abstract: it is the conclusion of someone who has watched large programs fail to find silver bullets in multifactorial diseases for 25 years. EPISODE TIMELINE Timestamps are AI-generated from the transcript and may not perfectly reflect final edited audio. Verify against the published episode before using for navigation. 00:00 Introduction 01:48 Career overview - 25 years in drug discovery at Wyeth and BMS 06:03 Origin story - glassware, the first binding assay, and the decision not to become a physician 11:54 Graduate school - independently discovering a circadian rhythm regulating prolactin secretion still cited 30 years later 17:57 Leaving academia for Wyeth - a two-week decision, $18,000 a year, and the door that closed behind it 19:55 The FSH receptor anomaly - how a production shortcut produced the first experimental evidence of biased GPCR signaling 23:40 When the literature called the data wrong - holding the line for nearly a decade 30:41 The physiologist's lens - why Arey has never chased the trending field 35:00 Science, family, and the years he was a single father of two young children 40:35 Writing the book with Kenakin - the argument that biased signaling is evolutionarily conserved, and why he chose a book over a review 48:09 Dinner with Martin Rodbell - drawing the FSH data on a napkin and hearing "I'm not surprised" 53:07 Advice for scientists - follow the data, trust your controls, stay humble, give back 01:01:55 What pharmacologists bring to drug discovery that nobody else does SELECTED QUOTES "If you've done all the controls appropriately, and you've done the experiments to the best of your ability, and you've asked all the hard questions and you still get the same result, then you have to have confidence in your data." "What we study in pharmacology, whether it's a GPCR or whatever, what we're really studying is evolution at the base level. And when you think about it from that perspective, it's hard not to be awed by nature." "I'm not surprised." - Martin Rodbell, upon being shown Arey's FSH signaling data drawn on a dinner napkin, citing a 1972 paper in which Rodbell had proposed a similar mechanism. "Science is really a personal endeavor - it's creative and personal. I hate to say it because it's so overused, but it really is an art form and everybody approaches it differently." About this episode Brian Arey is Senior Director of Mechanistic Pharmacology within Leads Discovery and Optimization at Bristol-Myers Squibb Co . in Lawrenceville, NJ. He obtained both his MS and Ph.D. in Neuroendocrine Physiology at Florida State University before completing his postdoctoral training at Northwestern University. He then moved to work in the pharmaceutical industry where he has held positions of increasing responsibility. He currently leads a team that provides a mechanistic understanding of small molecule drug candidates across the entire portfolio of BMS. Brian has contributed to the discovery or development of 5 marketed drugs through his work spanning molecular, biochemical, cellular, and in vivo assessment of drug candidates in many different physiological systems. Dr. Arey’s laboratory discovered the first described synthetic agonists and antagonists of the FSHR and has been an early champion of signaling bias as a physiological mechanism of gonadotropin action. He continues to pioneer in drug discovery studying GPCRs and other target classes. His recently published book on signaling bias, Biased Signaling in Physiology, Pharmacology, and Therapeutics is available on Amazon . I sat down with Brian to chat about GPCRs, working in the industry, and being a leader. This is part 1 of our conversation. Dr. Brian Arey on the web LinkedIn ResearchGate Pubmed Dr. GPCR Ecosystem Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Strategic Partner(s) Dr. Adriano Marchese About Dr. Adriano Marchese Adriano Marchese is a Professor of Biochemistry at the Medical College of Wisconsin. Adriano received his Bachelor of Science degree in Pharmacology in 1991 from the University of Toronto. He continued his graduate studies at the University of Toronto where he earned his MSc (1994) and Ph.D. (1998) in Pharmacology. He then moved to Thomas Jefferson University in Philadelphia, PA, for his postdoctoral training in Jeff Benovic’s laboratory studying the regulation of G protein-coupled receptor trafficking and signaling. In 2004 Adriano joined the faculty of the Department of Pharmacology at Loyola University Chicago. In 2016 he decided to move his lab to the Medical College of Wisconsin in Milwaukee, WI. Adriano’s research has contributed to our understanding of the role that ubiquitin plays in GPCR signaling and trafficking. His laboratory is interested in understanding the mechanisms that govern spatial and temporal regulation of GPCR signaling by -arrestins and post-translational modifications (PTMs), such as phosphorylation, ubiquitination, and SUMOylation. His lab has shown a role for -arrestins and PTMs in GPCR trafficking and signaling and has leveraged this knowledge to reveal the spatial and temporal requirements for GPCR activation of signaling pathways related to cell survival, proliferation, and migration. The ultimate goal of Adriano’s research is to target novel aspects of GPCR signaling for therapeutic development. Dr. Adriano Marchese on the web Twitter LinkedIn Google Scholar Website Dr. GPCR Ecosystem Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Strategic Partner(s) Dr. Evi Kostenis About Dr. Evi Kostenis "Pharmacist by training - PhD in Pharmacology - Postdoc at the NIH with Dr. Juergen Wess - Postdoc and Group leader in Aventis, now Sanofi, Frankfurt, Germany - Head of in vitro Pharmacology at 7TM Pharma in Denmark; Full professor, department chair and director of the institute for pharmaceutical Biology at the University of Bonn. Research interests: Signaling mechanisms involving GPCRs and heterotrimeric G proteins" Dr. Evi Kostenis on the web University of Bonn ResearchGate LinkedIn Dr. GPCR Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>