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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 274 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 203 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 203 min read


GPCR Allostery: Unlock Hidden Mechanisms and Make Smarter Drug Decisions
Allostery isn’t just an advanced concept—it’s essential to understanding efficacy, ligand bias, and receptor behavior in real-world systems.

Dr. GPCR News
Jul 313 min read


Pharmacologic Models
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.

Terry's Desk
Jul 81 min read


Accelerating GPCR Drug Discovery
Why I Started GPCR Consulting You've got great data. You've got brilliant scientists. But your GPCR program still isn't moving at the...

Yamina's Corner
Jun 302 min read
Dual loss of regulator of G protein signaling 2 and 5 exacerbates ventricular myocyte arrhythmias...
October 2022 Dual loss of regulator of G protein signaling 2 and 5 exacerbates ventricular myocyte arrhythmias and disrupts the...

GPCR News
Oct 1, 20221 min read
Structural view of G protein-coupled receptor signaling in the retinal rod outer segment
October 2022 "Visual phototransduction is the most extensively studied G protein-coupled receptor (GPCR) signaling pathway because of its...

GPCR News
Oct 1, 20221 min read
Intermolecular Interactions in G Protein-Coupled Receptor Allosteric Sites at the Membrane Interface
October 2022 Intermolecular Interactions in G Protein-Coupled Receptor Allosteric Sites at the Membrane Interface from Molecular Dynamics...

GPCR News
Oct 1, 20221 min read
Activation of GPR183 by 7 α,25-Dihydroxycholesterol Induces Behavioral Hypersensitivity through...
October 2022 Activation of GPR183 by 7 α,25-Dihydroxycholesterol Induces Behavioral Hypersensitivity through Mitogen-Activated Protein...

GPCR News
Oct 1, 20222 min read
Use of CRISPR/Cas9-edited HEK293 cells reveals that both conventional and novel protein kinase C...
October 2022 Use of CRISPR/Cas9-edited HEK293 cells reveals that both conventional and novel protein kinase C isozymes are involved in...

GPCR News
Oct 1, 20221 min read
Function and structure of bradykinin receptor 2 for drug discovery
October 2022 "Type 2 bradykinin receptor (B2R) is an essential G protein-coupled receptor (GPCR) that regulates the cardiovascular system...

GPCR News
Oct 1, 20221 min read
Differences across sexes on head-twitch behavior and 5-HT2A receptor signaling in C57BL/6J mice
October 2022 "Psychedelics, also known as classical hallucinogens, affect processes related to perception, cognition and sensory...

GPCR News
Oct 1, 20221 min read
Structure-Based Discovery of Negative Allosteric Modulators of the Metabotropic Glutamate Receptor 5
October 2022 "Recently determined structures of class C G protein-coupled receptors (GPCRs) revealed the location of allosteric binding...

GPCR News
Oct 1, 20221 min read
Single-molecule counting applied to the study of GPCR oligomerization
October 2022 "Single-molecule counting techniques enable a precise determination of the intracellular abundance and stoichiometry of...

GPCR News
Oct 1, 20221 min read
A cryptic mode of GPCR regulation revealed
October 2022 "Over three decades of research have provided thorough insights into G protein-coupled receptor (GPCR) regulation. In a...

GPCR News
Oct 1, 20221 min read
Microbial Metabolites Orchestrate a Distinct Multi-Tiered Regulatory Network in the Intestinal Epith
September 2022 Microbial Metabolites Orchestrate a Distinct Multi-Tiered Regulatory Network in the Intestinal Epithelium That Directs...

GPCR News
Sep 1, 20221 min read
Isoforms of GPR35 have distinct extracellular N-termini that allosterically modify...
September 2022 Isoforms of GPR35 have distinct extracellular N-termini that allosterically modify receptor-transducer coupling and...

GPCR News
Sep 1, 20221 min read
Opposite Effects of Src Family Kinases on YAP and ERK Activation in Pancreatic Cancer Cells...
September 2022 Opposite Effects of Src Family Kinases on YAP and ERK Activation in Pancreatic Cancer Cells: Implications for Targeted...

GPCR News
Sep 1, 20221 min read
Self-docking and cross-docking simulations of G protein-coupled receptor-ligand complexes
Self-docking and cross-docking simulations of G protein-coupled receptor-ligand complexes: Impact of ligand type and receptor activation...

GPCR News
Dec 28, 20212 min read
GPCRs Are Optimal Regulators of Complex Biological Systems and Orchestrate the Interface between ...
GPCRs Are Optimal Regulators of Complex Biological Systems and Orchestrate the Interface between Health and Disease GPCRs arguably...

GPCR News
Dec 13, 20211 min read
G protein-coupled receptor interactions and modification of signalling involving the ghrelin ...
G protein-coupled receptor interactions and modification of signalling involving the ghrelin receptor, GHSR1a The growth hormone...

GPCR News
Dec 9, 20211 min read
Integration and Spatial Organization of Signaling by G Protein-Coupled Receptor Homo- and ...
Integration and Spatial Organization of Signaling by G Protein-Coupled Receptor Homo- and Heterodimer Information flow from a source to a...

GPCR News
Dec 3, 20211 min read
Genome-wide identification of 216 G protein-coupled receptor (GPCR) genes from the marine water ...
Genome-wide identification of 216 G protein-coupled receptor (GPCR) genes from the marine water flea Diaphanosoma celebensis G...

GPCR News
Nov 2, 20211 min read
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