Insights That Move the GPCR Field Forward

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.

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?

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.

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.

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.

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.

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.

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 week's Terry's Corner with Dr. Terry Kenakin delivers a game-changing framework for teams grappling with the gap between in vitro potency and in vivo performance.

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.

From cryptic binding sites to ligand‑specific signaling, uncover how GPCR dynamics redefine drug discovery strategies and decision‑making.

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.

Allostery isn’t just an advanced concept—it’s essential to understanding efficacy, ligand bias, and receptor behavior in real-world systems.

Explore how GPCRs function as dynamic allosteric machines in this expert-level breakdown from Dr. Terry Kenakin. Learn how probe dependence, cryptic binding sites, and conformational changes impact drug discovery and therapeutic design.

Discover how RGS proteins like RGS4 are reshaping our understanding of GPCRs and chronic pain. Dr. Alex Serafini explains the quiet power of GPCR regulation.

GPCRs pose a critical challenge in drug discovery: a vast therapeutic potential with many targets yet to be explored.  35% of...

Dr. Alex Serafini turned chronic pain into a research mission. Discover how personal experience shaped his work on GPCRs, RGS proteins, and new pain models.

Welcome GPCR Fans,   Every discovery-phase decision you make shapes your entire pipeline trajectory—and understanding when equilibrium...

Kenakin’s kinetic insights help you translate assay readouts into actionable knowledge that keeps your programs focused and moving efficiently toward clinical relevance.

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.

Sokhom Pin explains why staying in GPCR research during its “unpopular” phase helped him become a sought-after expert today.

Sokhom Pin shares how he built a thriving GPCR research team at Alkermes through trust, culture, and empowerment-driven leadership.