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Watch Episode 174 You never forget the day your data surprises you—in a positive way. For Dr. Eric Trinquet, that moment arrived when his team successfully tracked GPCR internalization in native beta cells. They achieved this without complex imaging or radioactive materials. It was simply a clean, scalable assay—and a wave of new possibilities. This success was not mere luck. It was the result of chemistry, collaboration, and relentless effort until the signal finally confirmed: “We’re in.” From Bench to Breakthrough: Why pHSense Matters Decades of GPCR research have relied heavily on engineered systems. These include overexpression, tags, and fluorescent imaging. While they produce impressive data, they also impose artificial constraints. What if you could directly measure receptor internalization in physiologically relevant cells without disrupting their native state? That’s the promise of pHSense, a groundbreaking reagent developed by Eric Trinquet and his team at Revvity. This innovation emerged from years of foundational work in photophysics and GPCR pharmacology. Instead of creating another black-box assay, they designed pHSense around rare-earth europium probes. These probes shift brightness and fluorescence lifetime as pH changes. It’s a subtle yet powerful innovation. These probes become brighter and have a longer lifespan as internalized receptors enter acidic endosomes—translating biology into signal, instantly and accurately. Why does this matter? Until now, visualizing GPCR trafficking required imaging or forced overexpression. pHSense offers a high-throughput, no-wash, plate-reader-compatible assay with real-world relevance. The Chemistry That Almost Didn’t Work Designing pH-sensitive rare-earth complexes was not an obvious choice. The chemistry involved is notoriously complex. Solubility poses significant challenges. Even minor adjustments can compromise photophysical properties. However, Trinquet’s team, in collaboration with Professor David Parker from Durham University, cracked the code. They learned how to fine-tune both brightness and fluorescence lifetime. This led to the creation of a two-dimensional pH response curve capable of detecting subtle endosomal acidification. “You’re not changing the spectrum. You’re just changing how bright it is—and how long it glows,” said Dr. Eric Trinquet. Once they identified a lead compound, it became evident: this was not just another probe. This was the foundation of a new set of assay tools. The Day It Worked — Without Overexpression Trinquet describes this as a cornerstone moment. After months of adjustments, a scientist on his team presented a data set that transformed everything: a clean, dose-dependent response of GLP-1 receptor internalization in native beta cells. No imaging. No genetic modification. Just a plate reader, an agonist, and an endogenous GPCR. This achievement was not only technically impressive; it was conceptually transformative. For the first time, a team demonstrated high-throughput internalization data in physiologically relevant cells. Behind Every Probe Is a Partnership While the final product may arrive neatly packaged, the journey behind pHSense was anything but straightforward. The chemistry originated from Parker’s lab. The biological validation came from Jean-Philippe Pin’s group at the Genomic Functional Institute in Montpellier. The Revvity team acted as the glue. They constructed the platform, tested every variable—pKa, brightness, lifetime—and made decisions that few would even consider measuring. These were not mere vendor-supplier relationships. They were collaborative scientific ventures, years in the making. The outcome is not just a probe; it’s a tool scientists can trust. Mini Timeline: pHSense Development Early 2020s: Rare-earth probe synthesis begins Collaborative screening of scaffold families Key milestone: Clean signal in endogenous beta cells Revvity commercial launch Building a Scalable Platform — Not a One-Off Assay The brilliance of pHSense lies not only in the chemistry but also in its modularity. The assay is compatible with SNAP-tags, FLAG-tags, HA-tags, and even antibody fragments for native GPCRs. Whether in industry or academia, whether overexpressing or not, you can adapt the assay to your system. Since it operates on plate readers without wash steps, it is suitable for full-scale compound screening. “Don’t chase the shiny imaging tool if it doesn’t scale. Build or adopt assays that can evolve with your questions—like pHSense.” What’s Next? Follow the Feedback For Trinquet, commercialization is not the end; it’s a new beginning. User feedback will guide the development of future tags and variants. Teams are already investigating temperature effects, biased signaling, and endogenous dynamics. There is excitement about combining pHSense with other HTRF assays for multi-pathway mapping—G protein, arrestin, internalization—on the same cell line. What started as a chemistry problem has evolved into a discovery platform. “It’s like a funnel,” Trinquet explains. “You start wide with chemistry, you narrow with biology, and at the end—if you did it right—you open new doors.” To hear the full story of how pHSense came to life—and why the GLP-1 data changed everything— 🎧 Listen to the full podcast episode here ⸻ More about Revvity pHSense Reagents GPCR Reagents Revvity on Dr. GPCR   Dr. GPCR X Revvity Collaboration ⸻ Want more like this? 👉 Join the Dr. GPCR Premium Ecosystem for behind-the-scenes access to GPCR innovators, exclusive deep-dives, and practical tools to accelerate your research or career. 👥 Build connections. 🧪 Get insights. 🎧 Stay ahead.

Get ready for an expedition, GPCR explorers! Embark on another exciting exploration of the unknown realms of GPCR research. Welcome back to your weekly GPCR quest! This Week’s Highlights: Congrats to: John Teye Azietaku , our great contributor, for his article Class B1 GPCR Dimerization: Unveiling Its Role in Receptor Function and Signaling Sonja Peter , Brian Bender , Chris De Graaf for their excellent work on Comparative Study of Allosteric GPCR Binding Sites and Their Ligandability Potential Today, we started the Principles of Pharmacology II course! Thank you to all participants in Dr. Terry Kenakin's educational initiative this fall! Your dedication has greatly enriched the learning experience. Let’s keep fostering a collaborative environment for sharing ideas and expanding knowledge! Classified GPCR News  Let’s dive into the   Classified GPCR News from October 21st to 27th, 2024 Industry News Call for GPCR Papers Deadline: Nov 1, 2024. Emerging Voices in GPCR Biology in Special Issue of Molecular Pharmacology GPCR Events, Meetings, and Webinars November 5 - 7, 2024 | 16th Annual PEGS Europe   November 25 - 27, 2024 | 1st Virtual GPCR Forum Conference November 26 - 28, 2024 | GPCRs-Targeted Drug Discovery Summit Europe July 12 - 17, 2026 | 20th World Congress of Basic and Clinical Pharmacology GPCR Jobs Scientist I Cell Biology - Tectonic Therapeutic Senior Scientist, GPCR Pharmacology Research Associate - Professor Graeme Milligan Postdoc in Molecular Pharmacology - The Hauser Group Postdoctoral Scholar – iPSC in cardiac and endothelial cell function Protein Biochemist/Structural Biologist Senior Scientist/Staff Scientist, Computational Chemistry Postdoc in GPCR mechanosensing   GPCR Activation and Signaling A gain of function variant in RGS18 candidate for a familial mild bleeding syndrome Fusarium graminearum Ste2 and Ste3 Receptors Undergo Peroxidase-Induced Heterodimerization when Expressed Heterologously in Saccharomyces cerevisiae The beta 2 adrenergic receptor cross-linked interactome identifies 14-3-3 proteins as regulating the availability of signaling-competent receptors GPCRs in Neuroscience Astrocyte Gi-GPCR signaling corrects compulsive-like grooming and anxiety-related behaviors in Sapap3 knockout mice Orphan GPCRs in Neurodegenerative Disorders: Integrating Structural Biology and Drug Discovery Approaches Altered PLCβ/IP3/Ca2+ Signaling Pathway Activated by GPRCs in Olfactory Neuronal Precursor Cells Derived from Patients Diagnosed with Schizophrenia Sphingosine 1-phosphate receptor subtype 1 (S1P1) activity in the course of Alzheimer's disease GPCRs in Oncology and Immunology Characterization, expressional and evolutionary analysis of five fish-specific CCRs (CCR4La, CCR4Lc, CCR12a1, CCR12a2, and CCR12b) in largemouth bass (Micropterus salmoides) The pyruvate-GPR31 axis promotes transepithelial dendrite formation in human intestinal dendritic cells Methods & Updates in GPCR Research Generation of CRISPR/Cas9 modified human iPSC line with correction of heterozygous mutation in exon 6 of the CaSR gene Reviews, GPCRs, and more Insight into structural properties of viral G protein-coupled receptors and their role in the viral infection: IUPHAR Review 41 Structural and Molecular Insights into GPCR Function Comparative Study of Allosteric GPCR Binding Sites and Their Ligandability Potential Molecular Dynamics (MD) Simulations Provide Insights into the Activation Mechanisms of 5-HT2A Receptors Investigating the Effect of GLU283 Protonation State on the Conformational Heterogeneity of CCR5 by Molecular Dynamics Simulations Become a Premium Member! Get your 5-day free trial TODAY!

Greetings, Pioneers of GPCR Science! Embark on this week’s thrilling updates in GPCR research, learning opportunities, and industry developments. Don’t just stay informed—immerse yourself, expand your knowledge, and become a trailblazer in the field! This Week’s Highlights: Celebrating Excellence: Wessel A. C. Burger , Arthur Christopoulos , David M. Thal , et al., for their groundbreaking work on Positive allosteric modulation of a GPCR ternary complex Unlock Your Learning: Limited Spots Available! There are only 5 spots left for our upcoming courses, so seize the chance to learn from the best in the field. 🚨 Hurry to reserve your spot for the Principles of Pharmacology I & II BUNDLE before the Early Bird Deadline on September 27 . With just one week left, becoming a premium member is all it takes to benefit from this discount! Not a premium member yet?  No worries – you can sign up for a 5-day FREE trial! Gain access to over 500 minutes of recorded classes in our  GPCR courses   taught by Drs. Terry Kenakin  and Sam Hoare ! Every Thursday at 10 AM EST: Principles of Pharmacology I Dates: October 3, 10, 17, 24 (four sessions) Topics: Pharmacologic activity measurement, mechanisms of action, and GPCR discovery strategies. Registration deadline: September 27, 2024 Principles of Pharmacology II Dates: October 31, November 7, 14, 21, December 5 (five sessions) (we skipped Thanksgiving, of course!) Topics: New cellular assays, real-time kinetics, and unique GPCR behaviors. Registration deadline: October 25, 2024 🔥 Why You Should Enroll Now: Cost-effective & Distinctive Educational Experience Affordable courses that maintain high-quality standards. Adaptable Learning Access recorded sessions at your convenience to enhance your understanding. Our Students Highly Recommend Us! Previous students praise the course content and our exceptional service. Join us for an exciting discussion with Dr. Terry Kenakin to gain insights and prepare for upcoming courses. Don't miss this valuable opportunity! Exclusive Deal for Scientists Residing and Working in Developing Nations If you live and work  in a developing country, please complete this form to enjoy complimentary access to Dr. Kenakin's upcoming courses. Our goal is to ensure that education is within reach for everyone! Secure your spot today and dive into the evolving world of GPCRs! GPCR Event Spotlight Discovery on Target’s 19th Annual GPCR-Based Drug Discovery Targeting G Protein-Coupled Receptors for New Therapeutic Options 📍  Boston, MA 📅 October 2 -3, 2024 Join leading scientists to investigate the most recent advancements in GPCR-targeted drug development, incorporating machine learning, innovative biophysical methods, and medicinal chemistry. Register today for the GPCR Drug Discovery Conference and save $200 with discount code “ DRGPCR24 ”. 11th Adhesion GPCR Workshop    📍  Mexico City 📅 October 23-25, 2024 Engage with your peers and delve into the latest developments in adhesion GPCR biology. The full agenda is now available; check it here ! If you want to enhance your brand, email Hello@DrGPCR.com  for sponsorship opportunities. Classified GPCR News  Let’s dive into the   Classified GPCR News from September 9th to 15th, 2024 Industry News MBX aims for $136M IPO to take potential rival to Ascendis' Yorvipath into phase 3 Certa Therapeutics Announces International Non-Proprietary Name for its First-in-class GPR68 Inhibitor Asengeprast (FT011) AlphaProteo generates novel proteins for biology and health research Innovate UK announced the winners of its Transforming Cancer Therapeutics grant, which focuses on developing life-changing cancer treatments. 𝗦𝘂𝗺𝗺𝗮𝗿𝘆 𝗼𝗳 𝘁𝗵𝗲 𝗿𝗲𝘀𝘂𝗹𝘁𝘀 𝗼𝗳 𝗔𝗘𝗙𝟬𝟭𝟭𝟳 𝗣𝗵𝗮𝘀𝗲 𝟮𝗯 𝗶𝗻 𝗖𝗨𝗗 Nxera Pharma’s Partner Centessa Announces Positive Interim Phase 1 Clinical Data with its Novel Orexin Receptor 2 (OX2R) Agonist, ORX750, in Acutely Sleep-Deprived Healthy Volunteers Cumulus raising $50M, spinning GPR68 small molecules into GIO New treatments being developed for schizophrenia Crinetics Pharmaceuticals Announces September 2024 Inducement Grants Under Nasdaq Listing Rule 5635(c)(4) Call for GPCR Papers Deadline: Nov 1, 2024. Emerging Voices in GPCR Biology in Special Issue of Molecular Pharmacology GPCR Events, Meetings, and Webinars September 5 - 6, 2024 | 4th Transatlantic ECI GPCR Symposium September 18, 2024 | FREE Webinar - The value of GPCR cell-based assays in drug discovery September 22, 2024 | Biomolecular Horizons 2024 September 30 - October 3, 2024 | 22nd Discovery on Target October 2024 | Biologics US 2024   October 2 - 4, 2024 | 9th GPCRs in Medicinal Chemistry October 17, 2024 | Unprecedented fragment-based screening using Spectral Shift for GPCRs October 23 - 25, 2024 | 11th Adhesion GPCR Workshop November 5 - 7, 2024 | 16th Annual PEGS Europe   NEW November 25 - 27, 2024 | 1st Virtual GPCR Forum Conference November 26 - 28, 2024 | GPCRs-Targeted Drug Discovery Summit Europe July 12 - 17, 2026 | 20th World Congress of Basic and Clinical Pharmacology GPCR Jobs HIGHLIGHT Research Associate - Professor Graeme Milligan HIGHLIGHT Postdoc in Molecular Pharmacology - The Hauser Group NEW Postdoctoral Scholar – iPSC in cardiac and endothelial cell function NEW Protein Biochemist/Structural Biologist Senior Scientist/Staff Scientist, Computational Chemistry Postdoc in GPCR mechanosensing   Postdoctoral Position Postdoctoral research position Adhesion GPCRs Loss of cardiomyocyte-specific Adhesion G Protein Coupled Receptor G1 (ADGRG1/GPR56) promotes pressure overload-induced heart failure GPCR Activation and Signaling Positive allosteric modulation of a GPCR ternary complex GPCR Binders, Drugs, and more Progress on the development of Class A GPCR-biased ligands GPCRs in Cardiology, Endocrinology, and Taste CRTC1 in Mc4r-expressing cells is required for peripheral metabolism and systemic energy homeostasis Eiken syndrome with parathyroid hormone resistance due to a novel parathyroid hormone receptor type 1 mutation: clinical features and functional analysis GPCRs in Neuroscience Gain control of sensory input across polysynaptic circuitries in mouse visual cortex by a single G protein-coupled receptor type (5-HT2A) GPCRs in Oncology and Immunology The power of many: Multilevel targeting of representative chemokine and metabolite GPCRs in personalized cancer therapy GPR97 depletion aggravates imiquimod-induced psoriasis pathogenesis via amplifying IL-23/IL-17 axis signal pathway Structural and Molecular Insights into GPCR Function Exploring the constitutive activation mechanism of the class A orphan GPR20 Become a Premium Member! 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Stay at the Forefront of GPCR Drug Discovery! Learn from pioneers shaping biased signaling, assay design, and pharmacology—skills you won't find it anywhere else. Stay at the Forefront of GPCR Drug Discovery Gain insider methods from the pioneers shaping biased signaling, assay design, and pharmacology—skills you won't find in any textbook or paper. ⧖ Hours of Expert Training ↓ Downloadable Resources ◕ New Courses added Quarterly Get Access to GPCR Courses Explore the Masterclasses Full classes require Premium. 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Whether you’re a scientist, student, or just curious, you’ll hear about discoveries, career stories, and the latest GPCR news. Jump in and get inspired! Strategic Partners Latest Podcast Episodes 2025-10-22 2025-08-19 2025-07-08 2025-09-22 2025-08-05 2025-06-11 2025-09-02 2025-07-22 2025-05-27 1 2 3 4 5 1 ... 1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16 17 18 19 20 ... 20 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 Listen and subscribe where you get your podcasts