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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 This success was not mere luck. It’s a subtle yet powerful innovation. These were not mere vendor-supplier relationships.

27, 2024 | 1st Virtual GPCR Forum Conference November 26 - 28, 2024 | GPCRs-Targeted Drug Discovery Summit Precursor Cells Derived from Patients Diagnosed with Schizophrenia Sphingosine 1-phosphate receptor subtype

27, 2024 | 1st Virtual GPCR Forum Conference November 26 - 28, 2024 | GPCRs-Targeted Drug Discovery Summit

This is the silent advantage of many successful drugs: they bind tightly or covalently , making target But it also means new liability surfaces : persistent effects can’t be simply “washed out” when things Subscribe to The Kenakin Brief  today ➤

You can already explore the platform and subscribe to The Kenakin Brief—our new newsletter packed with MOR-positive allosteric modulator (BMS-986122) selectively enhances opioid signaling  through specific Gα subtypes

the mindset that helped shape products used across biotech and academia—and why play, failure, and surprise This mindset, he argues, suffocates innovation. He knows the cost firsthand. For Early-Career Scientists: Don’t confuse “final product” with overnight success.

If you want your molecules to survive first contact with biology, enzyme inhibition must be part of your Breakthroughs this week:  Potentiation of GPCR signaling by ATP and sugar monophosphates; Pharmacology Whether you’re designing a ligand, optimizing ADME, or predicting PK, enzyme inhibition defines what survives Whether you’re building assays or a scientific career, this is a must-read on why risk, surprise, and Read the Feature ➤ Summer Days: Appetite, Suntans, and GPCR Micro-Domains Two recent papers connect ciliary

Enzymes decide who survives. to clinical success. Their broad substrate tolerance shields us from xenobiotics. isn’t a checkbox; it’s a survival test. Subscribe to The Kenakin Brief  today ➤

unlocks a simple lever that separates signal from storytelling, moving programs forward with fewer surprises discovery Flexible , on-demand lessons for busy scientists Influence   the curriculum with your topic suggestions 🗞️ Weekly research, careers & event intelligence 🤝 Members-only networking, AMAs & matchmaking 💡 Support

Built to Fail, Built to Win: The IP One Gamble After the success of their cAMP assay, Trinquet’s team on the front lines of GPCR science, it’s a new lens to see what’s always been there—just below the surface

For drug hunters working at the GPCR interface, the difference between a successful lead and a dead-end Better Predictions For drug discovery scientists, time and predictive accuracy are the currency of success pipeline translates directly into better prioritization, cleaner data packages, and fewer late-stage surprises Unlock Assay Volume Control Only in Terry’s Corner 🎬 Watch Course Trailers Not sure yet? Subscribe to The Kenakin Brief  today ➤

Breakthroughs this week: New work clarifies how active-state GPCR conformations can support coupling GPCR internalization and soluble proteins; core meetings from GPCR Forum to Biophysics; plus targeted summits That subtle distinction opened the door to a brand-new assay format. For GPCRs, fluorescent ligands have quietly become one of the most versatile technologies—supporting Subtype specificity:  selectively track receptor subtypes in complex brain tissue.

This makes it an ideal candidate for GPCR research, where accuracy in detecting subtle signaling changes

blood-brain-barrier (BBB) and the complexity of the central nervous system (CNS) pose a challenge for developing successful central role in neuronal signaling and have been used to treat these diseases with varying degrees of success One of the biggest hurdles is the understanding and correct targeting of the different receptor subtypes promotes nucleotide release from, and activation of, the G protein α-subunit. Greater specificity : allows for selective tracking of receptor subtypes in complex brain tissues.

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Ignore these forces, and your “selective” agonist may deliver surprises the first time it meets a patient Surface vs. This section raises a critical design question for teams Are you sure your “antagonist” is enough—or Subscribe today and get direct access to decades of pharmacology experience that turn complex systems Subscribe to The Kenakin Brief today ➤

GPCR Reagent Portfolio pHSense™ is the latest addition to Revvity’s GPCR reagent portfolio , which supports Its GPCR research tools  support discovery teams and academic labs with precision reagents and validated

occupancy and complex activity, leverage hemi-equilibrium calcium assays, recognize fractal potency, and surface Corner members get to rewatch the recording Subscribe to the Kenakin Brief and Join the Live AMA ➤ Celtarys nanodiscs, peptidiscs, SMALPs, SPR, ITC—plus how construct design and solubilization choices shape success need to brief leadership, plan experiments, or time a move in the market or your career, Premium makes sure 🗞️ Weekly research, careers & event intelligence 🤝 Members-only networking, AMAs & matchmaking 💡 Support

Onset and offset rates (not just “final numbers”) decide which drugs succeed in patients and which ones Suddenly, at higher doses, you see an exaggerated ‘bang’ of effect. It’s like waiting for popcorn: at first, nothing happens, then suddenly the bag explodes with pops. them Exclusive access  to the next AMA session Direct engagement opportunities  through AMAs and topic suggestions Subscribe to The Kenakin Brief  today ➤

Upcoming events:  “Drug Discovery at Superluminal Speeds”; and Discovery on Target 2025—GPCR track you Engineer assays on purpose:  Set ranges, controls, and system sensitivity to surface mechanism—before Also super-valuable for those of us learning how to teach pharmacology." — DrGPCR University Attendee

Flow cytometry, a laser-based method, is used to examine single cells suspended in a fluid. Autofluorescence and multiplexing: Using far-red or near-infrared fluorophores can reduce background and support At Celtarys, we support this transition by offering optimized fluorescent ligands specifically designed CELT-240 in flow cytometry binding assays is suitable to measure the affinity of compounds for the D2

Suddenly, your snapshot becomes a forecast . The question was: could crude gp120 supernatant be used instead, without corrupting results? Chemists suddenly have meaningful levers to pull. The lesson: models don’t just need data. Subscriber-driven topics,  so the next lesson addresses your bottleneck. Subscribe to The Kenakin Brief today ➤

Superluminal Medicines: AI/ML Meets GPCR Pharmacology As Ajay continued to explore how GPCR signaling To address this, he co-founded Superluminal Medicines , a biotech company focused on integrating machine Superluminal is building systems that learn from receptor movement, conformational shifts, and complex In August 2025, Superluminal Medicines announced a collaboration with Eli Lilly and Company to advance Takeaway: Ajay Yekkirala’s story is not just about GPCR science or startup success.

insights for drug discovery Hi GPCR Friends, Every week, critical decisions in GPCR research hinge on subtle underpowered studies, this module hands you a practical framework to validate differences, confirm subtle Eliminate subjective calls:  From t-tests to ANOVA and F-tests, know which tool to apply when, so debates This is where the real conversations begin—made possible with the support of NIS, Proteos, and Axxam  

SNAP-tag has been successfully used while preserving activity. It can even study the GPCR distribution within endocytic vesicles and across subcellular compartments Cell-surface protein-protein interaction analysis with time-resolved FRET and snap-tag technologies:

Our Sponsors This event would not be possible without the generous support of our sponsors: NIS Proteos Axxam Axxam is a leading provider of integrated discovery services, supporting the entire drug discovery This comprehensive approach enables Axxam to support clients worldwide in identifying and optimizing

And when decisions ride on subtle shifts, “looks different” isn’t good enough. Subtle shifts vanish in noise. them Exclusive access to the next AMA session Direct engagement opportunities  through AMAs and topic suggestions Subscribe to The Kenakin Brief today ➤ #ttest #ANOVA #poweranalysis #curvecomparison #ftest #assayvalidation

There, she chose to write a review on genetic variation in susceptibility to alcoholism and opioid addiction—a I was staying up super late. I was excited to work on this, till 2 or 3 a.m.” Her current work examines how these substances, when used alone or together, impair breathing in mice This mindset can lead to a more fulfilling and successful career.

While writing a literature review on opioid and alcohol addiction susceptibility, something shifted. Lessons from Catherine’s Story Catherine’s career challenges the idea that success requires a straight Academic success is less about prestige than about impact. That urgency, more than titles, positions, or prestige, is what sustains a lasting career in science.

Blueprint for survival:  Continuous improvement and operational scaffolding—not more hires—are the real