Insights That Move the GPCR Field Forward

Every drug you design will meet an enzyme before it meets its receptor. If you want your molecules to survive first contact with biology—and with the FDA—enzyme inhibition must be part of your core playbook. This week’s feature breaks down exactly how to think about inhibitors with rigor and speed, so you can make better decisions earlier in the pipeline. Breakthroughs this week: Potentiation of GPCR signaling by ATP and sugar monophosphates; Pharmacology 2025; Nxera Pharma

The difference between orthosteric vs. allosteric mechanisms isn’t just academic — an orthosteric antagonist can hijack receptor physiology, while an allosteric modulator works with the system. That choice determines whether you risk over- or under-dosing, miss safety windows, or miss therapeutic breakthroughs.

GPCRs don’t play fair. Learn how opposing processes, receptor trafficking, and constitutive activity shape drug response—and how to design for them.

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.

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!

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.

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.

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.

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?

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.

From Venice to Munich, follow the story of Alessandro Nicoli, a PhD student whose path into science was anything but linear. In this episode, he shares how a love of chemistry, the guidance of key mentors, and a leap into computational modeling led him to tackle one of biology’s greatest puzzles: olfactory GPCRs. Discover how AlphaFold, molecular dynamics, and curiosity-driven research are reshaping the way we study G protein-coupled receptors.

This fundamental disconnect between the lab and the boardroom is precisely where programs get stuck—not because of bad science, but because companies find themselves throwing more money and people at problems that could be solved with better systems. This reactive approach, driven by a "go fast" mindset, burns through precious capital and time, leaving both scientific teams and investors frustrated.

Should we start research with the model, not the molecule? Dr. Alex Serafini explains how building backwards may be the future of GPCR-driven pain therapy.

That’s why this week at Dr. GPCR, we’re focusing on the hidden risks that undermine progress and how the right frameworks can keep your pipeline moving forward.

Is Your GPCR Program Slowing Down—Even With Good Data? You’re not alone. Most teams don’t stall because the science is weak. They stall...

In Terry Kenakin’s latest foundational lesson from Terry’s Corner, he unpacks the art and science of pharmacologic modeling. This isn’t just theory—it's the essential framework used to interpret experimental data, anticipate system-wide drug effects, and design smarter trials.

The latest Terry’s Corner unlocks clinical forecasting tools few scientists truly master.

1.       Introduction Dopamine receptors are G-protein-coupled receptors (GPCRs), which have 5 subtypes -D1-5. The dysfunction of these...

Hello Dr.GPCR readers! This is Lucía from the Celtarys Research chemistry team.  For our very first post in this ecosystem, we wanted to...

July 2022 "Orion Biotechnology and Peptilogics are pursuing AI-driven drug discovery to explore new functional chemical space and...

June 2022 "Ottawa, Canada, May 10, 2022 — Orion Biotechnology Canada Ltd, a drug discovery and development company unlocking the...

June 2022 "G protein-coupled receptors (GPCRs) represent a major therapeutic target class as they play a key role in many (patho-)...

May 2022 Sosei Heptares and Kallyope Enter Collaboration to Identify and Validate Novel Gastrointestinal GPCR Targets for Drug Discovery...