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Insights That Move the GPCR Field Forward
Read the latest analyses, interviews, and discoveries shaping the GPCR ecosystem — from research breakthroughs to biotech strategy.
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GPCR Articles


Optimizing HTRF Assays with Fluorescent Ligands: Time-Resolved Fluorescence in GPCR Research
What is Homogeneous Time-Resolved Fluorescence (HTRF)? HTRF is a hybrid detection technology that combines Förster Resonance Energy...

Lucía from Celtarys Research
Sep 17, 20254 min read


The Five Traps of Ignoring Kinetics
Learn how ligand binding kinetics reveal hidden drug effects, improve GPCR assay design, and prevent costly errors in drug discovery pipelines.

Terry's Desk
Sep 16, 20254 min read


Mechanism vs. Assumption: A Model-First Path to Getting GPCR MoA Right
Early signals can mislead. This week’s Dr. GPCR Weekly shows how to call Mechanism of Action with model-first rigor—distinguishing orthosteric vs. allosteric, designing assays that reveal mechanism, and unlocking SAR. Plus: Novo’s \$550M obesity/diabetes push, Rhythm’s sNDA, key events, and confocal imaging that respects function. Upgrade to Premium for the full digest.

Dr. GPCR News
Sep 11, 20254 min read


Integrating Fluorescent Ligands into Flow Cytometry: Enhancing GPCR Analysis Beyond Traditional Antibody Staining
Flow cytometry, a laser-based method, is used to examine single cells suspended in a fluid. By measuring the way these cells scatter...

Lucía from Celtarys Research
Sep 9, 20253 min read


From Snapshots to Predictions: Why Mechanism of Action Matters
Turn assay snapshots into predictions. Models separate orthosteric vs allosteric mechanisms and guide experiments for faster decisions in Terry’s Corner.

Terry's Desk
Sep 9, 20255 min read


How a Failed Med School Dream Sparked a GPCR Biotech Revolution
Ajay Yekkirala’s journey from rejected med student to GPCR biotech founder shows how failure, mentorship, and curiosity can drive real innovation in drug discovery.

Dr. GPCR Podcast
Sep 4, 20254 min read


How to Use Statistical Methods to Strengthen Every GPCR Drug Discovery Decision
Curve shifts can mislead, but statistics won’t. This week in Terry’s Corner: power analysis, t-tests, ANOVA, and F-tests to move from “I think” to “I know.” Plus, Ajay Yekkirala on AI-driven GPCR therapeutics and an invitation to Boston’s GPCR Happy Hour. Premium Members get full access to curated jobs, events, and must-read publications—your edge to stay ahead in fast-moving GPCR science.

Dr. GPCR News
Sep 4, 20253 min read


Applications of Fluorescent Probes in Confocal Imaging of GPCRs: From Live to Fixed Cells
Applications of Fluorescent Probes in Confocal Imaging of GPCRs: From Live to Fixed Cells GPCRs are present across cell membranes...

Lucía from Celtarys Research
Sep 3, 20253 min read


Curve Shifts Don’t Lie, But Your Eyes Might
Stop guessing at curve shifts. Learn how t-tests, ANOVA & F-tests bring confidence, not noise, to drug discovery decisions.

Terry's Desk
Sep 2, 20254 min read


Purpose-Driven Opioid Research: Catherine Demery’s Academic Path
Purpose-driven science works because it creates resilience. Careers built on prestige, titles, or external pressure can burn out quickly. But careers built on urgency, alignment, and meaning are the ones that last.

Dr. GPCR Podcast
Aug 28, 20253 min read


Allosteric Binding Demystified: Smarter GPCR Drug Discovery
This week’s Dr. GPCR Weekly News delivers urgent insights every GPCR scientist and drug discovery leader needs. From Terry’s Corner on the hidden traps of allosteric binding, to Yamina’s Corner on the hidden costs of fragmented systems, and a preview of Discovery on Target 2025, this edition highlights the frameworks shaping the next decade of therapies. Plus: industry breakthroughs on metabolic GPCRs, key September events, curated career opportunities, and must-read publicat

Dr. GPCR News
Aug 27, 20253 min read


GPCR Drug Discovery at Discovery on Target: Why This Track Is About More Than Receptors
Join us at the Discovery on Target meeting in Boston for the GPCR Drug Discovery track! I’m honored to chair a session featuring Terry Kenakin, a leader in functional selectivity. We’ll explore GPCR targets like GLP-1R, CXCR4, and dopamine receptors across oncology, metabolic, CNS, and immunology. As Dr. GPCR, we connect scientists and accelerate innovation — see you in Boston!

Dr. GPCR News
Aug 27, 20254 min read


Fluorescence Polarization in GPCR Research
The ability to identify compounds that interact with molecular targets involved in disease pathways is where the development of new...

Lucía from Celtarys Research
Aug 27, 20253 min read


Fentanyl and Xylazine: Why Breathing Fails in Overdose
At its core, Catherine Demery’s research is about receptors and signaling pathways—how mu-opioid and alpha-2 adrenergic receptors interact to disrupt breathing. But it’s also about public health urgency.

Dr. GPCR Podcast
Aug 26, 20254 min read


Why “Displacement” Misleads You: Allosteric Binding Demystified
Think you understand ligand displacement? Think again. This week’s Terry’s Corner blog reveals how allosteric modulators reshape receptor identity—and why conventional binding logic fails in these systems.

Terry's Desk
Aug 26, 20253 min read


Understanding the Journey: Catherine Demery's Path to Addiction Science
Catherine Demery shares how walking away from pharmacy school led her to discover a passion for opioid pharmacology. From CRO experience to addiction-focused research, she now investigates fentanyl and xylazine’s effects on respiration using mouse models. Her story offers critical insight into how non-linear paths, personal loss, and public health urgency can shape impactful scientific careers in the GPCR research community.

Dr. GPCR Podcast
Aug 21, 20254 min read


The Hidden Driver of GPCR Drug Success: Why Target Residence Time Matters More Than You Think
This week's breakthroughs are crucial for staying ahead in the rapidly evolving landscape of GPCR research and drug discovery. Dr. Terry Kenakin's insights on target residence time can reshape how you evaluate and advance lead compounds, potentially saving your team from costly late-stage failures. That's exactly what Dr. GPCR delivers every week: practical tools and critical intelligence to elevate your science and sharpen your decisions.

Dr. GPCR News
Aug 21, 20254 min read


GPCR Happy Hour – Boston, Sept 2025
Every September, Boston welcomes the global biotech and drug discovery community. Scientists, investors, and CRO professionals fly in from around the world, while Boston’s own vibrant life sciences hub shows up in full force. GPCR Happy Hour is where these two worlds meet. It’s not just networking. It’s where partnerships spark, ideas collide, and the GPCR community grows stronger — together.

Dr. GPCR News
Aug 20, 20253 min read


The Imprecision Problem: Why Your GPCR Drug Discovery Program Is Off-Track Before It Even Starts
A GPCR program can have brilliant science and talented people and still get stuck. The issue isn't a lack of effort; it's a lack of precision. The granular, often overlooked details are where programs falter, leading to unforeseen costs and delays. So, why do promising programs stall despite significant investment and a skilled team?

Yamina's Corner
Aug 20, 20253 min read


Target Residence Time: The Hidden Driver of In Vivo Efficacy
Most drug discovery teams chase potency, but miss the variable that often determines real-world success: target residence time. In this expert lecture, Dr. Terry Kenakin explores how restricted diffusion, rebinding, and kinetic dissociation transform in vivo pharmacology, especially when PK and PD diverge. If your leads fail in translation, this may be the insight your pipeline needs.

Terry's Desk
Aug 19, 20253 min read


From Student to Mentor: What Alessandro Nicoli Learned About Leading in Science
What does it mean to lead in science as a PhD student? In this episode, Alessandro Nicoli reflects on being the first PhD in a new lab, the challenges of delegating, and the rewards of mentoring students. His story reveals how leadership is learned through shared growth, patience, and shaping the next generation of GPCR researchers. A must-read for scientists balancing research with mentoring responsibilities.

Dr. GPCR Podcast
Aug 14, 20252 min read


Competitive vs Non-Competitive GPCR Antagonists: How to Interpret Pharmacology Data with Confidence
In pharmacology, the wrong interpretation of antagonist behavior can derail your conclusions, your experiments, and even your program’s credibility. That’s why mastering competitive vs non-competitive antagonism isn’t optional — it’s essential for accurate, defensible science.
This week’s Terry’s Corner takes you beyond curve shapes into the kinetic and mechanistic realities that separate surface-level analysis from true expertise.

Dr. GPCR News
Aug 14, 20255 min read


Misread the Curve, Misjudge the Drug: Rethinking Antagonism in GPCR Pharmacology
Don’t let curve shapes deceive you. In this blog, Dr. Terry Kenakin unpacks why dose-response shifts aren’t definitive proof of antagonist mechanism. Learn how binding kinetics—not just appearance—distinguish competitive from non-competitive antagonism, and why assumptions can mislead drug discovery decisions. If your team relies on DR curves to evaluate receptor blockade, this read will sharpen your approach and help you avoid common pitfalls in mechanism interpretation.

Terry's Desk
Aug 12, 20253 min read


Decoding Olfactory GPCRs: How AlphaFold and AI Are Changing the Game
How do you study receptors with no ligands and no structures? In this episode, PhD student Alessandro Nicoli explains how AlphaFold and molecular dynamics are revolutionizing the study of olfactory GPCRs. By turning predictions into starting points, Alessandro and his team are building models that not only match experimental accuracy but also open new doors in ligand discovery, drug design, and the future of computational biology.

Dr. GPCR Podcast
Aug 12, 20252 min read
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