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Watch Episode 170 Thinking Differently Pain research has long followed a familiar route: from molecule Why This Approach Matters In pain research, bottom-up approaches often fail to translate. It asks researchers to consider the entire ecosystem: from patient to molecule , not just the other way Alex Serafini makes the case for building pain research from the clinic down, not the bench up. _____ ___ Keyword Cloud: GPCR podcast , pain modeling , GPCR online course , translational research , neuroimmune

That perspective changed the moment he entered GPCR research . Instead, he acts as an advisor, helping research teams decide where modeling can accelerate progress—and The GPCR Challenge What makes collaboration non-negotiable in GPCR research is the biology itself. Whether in academia or biotech, the future belongs to research groups that can orchestrate ecosystems GPCR Models Don’t Discover Drugs—People Do In GPCR research, the biggest breakthroughs won’t come from

How Fluorescence Polarization Assays Work: Principles and Applications in GPCR Research FP assays work Ligands Looking ahead, fluorescence polarization technology is expected to expand its role in GPCR research

chemistry, and drug discovery —rethinking how simulations, docking, and machine learning can transform GPCR research Translational Impact for Drug Discovery While the Carlsson lab is rooted in academia, its impact extends But success depends on researchers who can manage expectations, build trust, and integrate across disciplines With rigor, transparency, and cross-disciplinary collaboration, they’re pushing GPCR science toward a ligand design, and experimental collaboration. 🧠 Learn from the field’s top innovators. 📈 Sharpen your translational

Why Purpose Matters in Science For some researchers, science is a job. For others, it’s a calling. , Catherine reflects on how her identity as a scientist took shape, why she’s committed to academic research That alignment between curiosity and urgency set her on the path toward doctoral research. What’s Next in Her Opioid Research Catherine’s current experiments focus on outcomes such as respiratory Catherine’s story shows that when purpose drives research, science becomes more than a job—it becomes

Drug pipelines live and die by your ability to make fast, accurate calls. One wrong assumption about how your molecule behaves in a living system can sink months of work and millions in development costs. The real challenge? GPCR signaling almost never follows a straight path. Reflex arcs, compensatory pathways, and receptor trafficking can turn your expected outcome on its head, sometimes after you’ve already committed to a clinical strategy. This session gives you the tools to anticipate those twists before they hit your program. This article is about one big idea: GPCRs don’t act in isolation—they respond to the system they’re in, often through opposing processes that you must model to get reproducible results. In this session, you’ll gain: ✅ A mental model you can trust  for predicting how GPCR ligands behave in real physiology—not just in a dish. ✅ A pattern-recognition toolkit  to spot red flags early and make course corrections before trials derail. ✅ Practical strategies  for using receptor trafficking data and system set-points to design cleaner, more predictive experiments. Why Pipeline Efficiency Starts with Physiology Drug discovery doesn’t happen in a vacuum. Every ligand you design enters a system that is already balancing opposing forces—vasoconstriction vs. vasodilation, sympathetic vs. parasympathetic tone, signal activation vs. receptor downregulation. Ignore these forces, and your “selective” agonist may deliver surprises the first time it meets a patient. This lecture challenges the habit of treating in vitro data as destiny. Instead, you’ll walk through cardiovascular reflexes, surface signaling vs. internalization, and constitutive receptor activity to show how the body bends your molecule’s effect. If your job is to move molecules confidently toward the clinic, this is a blueprint for building a more reliable evidence base—one that accounts for biology’s counterpunch. When In Vitro Lies: The Patient vs. Volunteer Gap Many programs die in Phase II, not because the molecule is “bad,” but because its profile in patients was never truly understood. A renin inhibitor that lowers blood pressure in healthy volunteers might not drop blood pressure at all in heart failure patients, because increased cardiac output cancels the expected effect. You’ll understand why this is good news, not bad data, and how it can actually prevent harmful reflex tachycardia. The bigger lesson? Context matters. This section outlines the logic required to match preclinical models to patient physiology and avoid being misled by early screens. Once you see how patient physiology flips expected outcomes, the next step is to ask, could these reflexes work in your favor? Reflexes as Drug Design Partners Not all reflexes are enemies. Some can make a mediocre drug shine. Dobutamine’s dual action on beta and alpha receptors, for example, invites reflex bradycardia that blunts its heart rate liability—making it a better inotrope than isoproterenol in heart failure. Learn how to view reflexes not just as confounders but as potential allies. The teaser question How could you design your next lead to recruit the body’s own feedback loops in your favor? Surface vs. Internalized Signaling: Same Receptor, Different Story A GPCR response isn’t always over when the receptor leaves the membrane. In this module, you’ll explore how some receptor–agonist complexes continue signaling from endosomes, creating “protected” signaling that extracellular antagonists can’t block. This insight has huge implications for how you select and rank agonists in discovery campaigns. You’ll come away asking Which of my ligands might be producing hidden signaling from inside the cell—and how can I measure it before it surprises me downstream? System-Dependent Activity and Opposing Processes Partial agonists don’t wear single labels. The same compound can look like an activator in one system and a blocker in another—depending on basal tone. Terry illustrates this with classic β-receptor partial agonists, showing how heart rate set-points under different anesthetics can flip observed pharmacology. The takeaway? When you evaluate partial agonists, enzyme inhibitors, or antagonists, you must recreate the “working system” they’ll face in vivo—otherwise you risk throwing out molecules that would have worked. Constitutive Activity: When Doing Nothing Still Does Something Some GPCRs simply refuse to stay quiet. Ghrelin receptors, for example, signal spontaneously, meaning a neutral antagonist won’t suppress appetite; it just blocks added stimulation. Get a sense of why inverse agonists may be necessary to truly shift the physiological balance. This section raises a critical design question for teams Are you sure your “antagonist” is enough—or do you need an inverse agonist to get the clinical outcome you want? Your molecule isn’t failing—your model might be too simple. Terry’s Corner exists to fix that blind spot. Subscribe today and get direct access to decades of pharmacology experience that turn complex systems into better decisions. Why Terry’s Corner Most pharmacology training freezes at equilibrium snapshots. But drug discovery isn’t static — it’s a moving target. Ligands come and go, feedback loops kick in, and what you see in vitro rarely tells the whole story. Go inside the real-world playbook. Here’s what you’ll get: Weekly expert sessions  that turn messy data into clear decisions On-demand access  to a growing library of system-level case studies Unfiltered Q&A recordings  where challenging problems get solved live Direct input opportunities  so future sessions answer your  questions Battle-tested insight  from four decades of drug discovery experience If you’re serious about derisking your pipeline, this is where you sharpen the tools that actually move molecules forward. See beyond the equilibrium. Make decisions with confidence. 🟢 40 years of expertise at your fingertips: Explore the complete library ➤ ✳️ Want to know what’s inside? Read the latest articles ➤ Stay sharp between lectures. Subscribe to The Kenakin Brief today ➤

That’s not a story about nostalgia — it’s a snapshot of how GPCR research was built, on technique at These painstaking manual workflows laid the foundation for what would become the evolution of GPCR research Every step felt like it could make or break the result, The pace and precision of GPCR research today What Changed After This : High-throughput capabilities meant researchers could map GPCR signaling more The Mindset Shift: From Technique to Strategy Michelle reflects on how early-career researchers once

activity biosensors Marta Lopez-Balastegui, Antonella Di Pizio, Jiafei Mao, Jana Selent, et al. for their research Bouvier, et al. for their study on the Role of the V2R-βarrestin-Gβγ complex in promoting G protein translocation Join fellow scientists and researchers in person to stay updated with adhesion GPCR biology. and Six Herbal Compounds as Potential Drugs for Chronic Myeloid Leukemia Methods & Updates in GPCR Research - 17, 2026 | 20th World Congress of Basic and Clinical Pharmacology 2026 GPCR Jobs NEW Postdoctoral Research

Who should listen Researchers navigating complex datasets, balancing innovation with assay rigor, or conversation is part of a three episode series produced in collaboration with our partners at Celtarys Research How GPCR Collaboration Built an Innovation Engine From Pipettes to Platforms: The Evolution of GPCR Research GPCR scientists, translational pharmacologists, biotech discovery teams, and decision-makers who need

Every R&D team is under the same pressure: deliver validated targets, clean pharmacology, and translatable Months of wasted resources, failed translation, and opportunity loss. Allosteric sites operate differently: ligands bind elsewhere, transmit energy changes, and shift the Translational Relevance: From Bench to Clinic Misjudging orthosteric vs allosteric behavior can derail your ligand interacts with the receptor lets you predict safety margins, dose–response behavior, and translational

Drum rolls, we’ve got 15 GPCR research papers, updates, industry news events, and GPCR ads curated just in downstream pathway activation Chiara D Mancinelli, Joshua Levitz, David Eliezer, et al. for their research It is an opportunity to connect with like-minded scientists and researchers and gain valuable insights signaling reveals unexpected differences in downstream pathway activation Methods & Updates in GPCR Research NEW Senior Scientist, Cryo-Electron Microscopy Postdoctoral Research Associate Senior Scientist - Discovery

This makes it an ideal candidate for GPCR research, where accuracy in detecting subtle signaling changes Enhancing HTRF Assay Performance in GPCR Research Using Fluorescent Ligands GPCRs are involved in numerous By using donor-acceptor pairs with different emission spectra that don’t overlap, researchers can design technologies by providing high-performance fluorescent ligands designed specifically for pharmacological research

Eric Trinquet, Director of Research and Development at Revvity.   A GPCR Internalization Tool Designed for Real Research Needs Built on more than two decade A GPCR Internalization Tool Designed for Real Research Needs s of GPCR assay innovation , pHSense™  was developed to overcome GPCR  is a global nonprofit platform advancing GPCR research  through education, community, and platform Its GPCR research tools  support discovery teams and academic labs with precision reagents and validated

His work spans deep academic research, startup life, and the application of machine learning and pharmacology There, Ajay expanded his understanding of neurobiology and translational research models, further refining He emphasizes that building a startup is not simply a continuation of research — it requires a mindset Advice for Young Scientists For early-career researchers, Ajay’s journey offers a powerful blueprint. addiction, or another unmet need, keeping the real-world impact in focus can clarify career decisions and research

Some Nbs that have been use for GPCR research are: Nb80: This nanobody stabilized an active-state conformation

Embark on another exciting exploration of the unknown realms of GPCR research. Pharmacology GPCR Jobs Scientist I Cell Biology - Tectonic Therapeutic Senior Scientist, GPCR Pharmacology Research transepithelial dendrite formation in human intestinal dendritic cells Methods & Updates in GPCR Research

receptor activity-modifying proteins Nicholas Kapolka , Geoffrey Taghon , and Daniel Isom  for their research protein-coupled receptor-mediated signaling of immunomodulation in tumor progression Methods & Updates in GPCR Research Clinical Pharmacology GPCR Jobs NEW Postdoc in GPCR mechanosensing   Postdoctoral Position Postdoctoral research position Senior or Lead Researcher   Senior Scientist, Cryo-Electron Microscopy   Postdoctoral Research

ahead without noise or delays: Industry insights:  Structure-Based Drug Design Summit; AI-Powered GPCR Research research. Redefine your playbook:  Why Serafini believes that pain research needs to start from clinical phenotype s Corner  digital pharmacology courses Priority access to insights from major conferences, emerging research GPCR scientists, translational pharmacologists, biotech drug discovery teams, and decision-makers who

GPCR, the global knowledge hub for G protein-coupled receptor (GPCR) research and education, is proud to welcome Celtarys Research to its partner ecosystem. Celtarys Research develops high-quality, fluorescently labeled ligands and innovative chemical biology , CEO of Celtarys Research. About Celtarys Research Celtarys Research is a biotech company based in Spain that specializes in the

In a recent study on TAAR1, a GPCR linked to central nervous system disorders, researchers compared the

Our scientific team can guide you choose or design the right fluorescent ligand for your research.  

After all, a good tool makes a good assay, and a good assay improves research capacity. Chemistry Tools session was more industry focused than those before, and Maria shared the floor with researchers

Despite their immense potential, utilizing FRET and BRET sensors in GPCR research comes with challenges Addressing these hurdles is essential for translating findings from cellular models to clinically relevant In conclusion, FRET and BRET-based sensors have transformed the landscape of GPCR research, offering

Embark on another exciting exploration of the unknown realms of GPCR research. The 11th Adhesion GPCR Workshop 2024 was a successful event that brought together experts, researchers Biology - Tectonic Therapeutic PhD fellowship in GPCR mechanosensing Senior Scientist, GPCR Pharmacology Research promotes transepithelial dendrite formation in human intestinal dendritic cells Methods & Updates in GPCR Research

Hello GPCR Trailblazers, This week, we’re spotlighting Celtarys Research, our newest partner, featured Maria Majellaro of Celtarys shares how her team translates medicinal chemistry into practical GPCR assay GPCR will help researchers move faster with custom fluorescent ligands, translational insight, and tool-enabled Introducing Celtarys - Probe Development via Conjugation Strategies   Celtarys Research's first article Explore this week’s research, tools, and biotech insights in one place. The insights are ready.

occurring Δ9-tetrahydrocannabinolderivatives to cannabinoid CB1 and CB2 receptors, Pharmacological Research

Summit 💲 Special Pricing on GPCR courses GPCR Forum Start a lively chat or request help with your research Scientist, Medicinal Chemistry PhD fellowship in GPCR mechanosensing Senior Scientist, GPCR Pharmacology Research ICAP-1 as novel regulators of LFA-1-mediated T cell polarity and migration Methods & Updates in GPCR Research

The GPCR ship is setting sail on a grand voyage across the vast ocean of research. Symposia 💲 Discounted GPCR courses GPCR Forum Start an engaging discussion or request help in your research Scientist, Medicinal Chemistry PhD fellowship in GPCR mechanosensing Senior Scientist, GPCR Pharmacology Research hepatocellular carcinoma cells via inhibition of the c-Jun N-terminal kinase Methods & Updates in GPCR Research

Thus, developing assays for commercially available probes such as CELT-419 would facilitate research For example, a Cy5-labelled fluorescent ligand with the same pharmacophore is available from Celtarys Research development of measurement methods can increase the quality and quantity of both fundamental receptor research

This is Lucía from the Celtarys Research chemistry team.  For our very first post in this ecosystem, we wanted to highlight a huge part of our work at Celtarys Research