Insights That Move the GPCR Field Forward

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.

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.

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.

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.

In Terry Kenakin’s latest lecture from the Emerging Drug Hunter series, he invites you into a thought-provoking reevaluation of one of pharmacology’s most misleading concepts: the myth of high and low-affinity binding sites.

November 2022 "Neuropeptides produce robust effects on behavior across species, and recent research has benefited from advances in...

November 2022 "Some G protein-coupled receptor (GPCR) ligands act as "biased agonists" that preferentially activate specific signaling...

November 2022 Deciphering the signaling mechanisms of β-arrestin1 and β-arrestin2 in regulation of cancer cell cycle and metastasis...

November 2022 "Recently determined structures of class C G protein-coupled receptors (GPCRs) revealed the location of allosteric binding...

November 2022 "Adhesion G-protein-coupled receptors (aGPCRs) play key roles in a diversity of physiologies. A hallmark of aGPCR...

November 2022 "Despite the growing number of G protein-coupled receptor (GPCR) structures, only 39 structures have been cocrystallized...

November 2022 "Dimerization of beta 2-adrenergic receptor (β2-AR) has been observed across various physiologies. However, the function of...