Insights That Move the GPCR Field 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...

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...

1. Introduction 1.1 The Endocannabinoid System The Endocannabinoid System (ECS) is composed of the Cannabinoid Receptors 1 and 2...

Hello GPCR Minds, This week, you'll learn all about Terry’s Pharmacology Corner, your new learning space focused on GPCR pharmacology. Whether you’re early in your career or pushing the edge of MoA design, weekly lesson help you apply key concepts like binding, signaling, and kinetics in practical, decision-shaping ways. The Corner comes will live monthly AMA sessions with Dr. Kenakin. Get curated content at your own pace. Subscribe to The Kenakin Brief below to stay in t

Understanding receptor-ligand interaction is key in drug discovery and biomedical research. Radioligands have been used to study GPCRs...

Hello GPCR Trailblazers, This week, we’re spotlighting Celtarys Research, our newest partner, featured in a blog and podcast with CSO Dr. Maria Majellaro, highlighting their fluorescent ligand tools for live-cell GPCR assays. After 40+ years and 250 publications, Dr. Terry Kenakin is launching a new learning space with video courses, AMAs, and practical insights . Get a sneak peek and sign up for The Kenakin Brief—his free weekly newslette r. On the industry side, Novo N

Celtarys Research Joins Dr. GPCR – Precision Tools for GPCR Assays Dr. GPCR and Celtarys Research have teamed up. This partnership aims to bring advanced chemical probe strategies to the forefront. The goal is to accelerate receptor-targeted discovery. They will showcase innovative conjugation methods. These methods will provide scientists with direct access to emerging tools and insights. Explore the partnership Multiplexing GPCR Discovery - Sakmar Lab’s Toolkit Goes Publi

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

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

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 "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...

October 2022 "Arrestins interact with G protein-coupled receptors (GPCRs) to stop G protein activation and to initiate key signaling...

October 2022 Dual loss of regulator of G protein signaling 2 and 5 exacerbates ventricular myocyte arrhythmias and disrupts the...

October 2022 "G protein-coupled receptors (GPCRs) are important drug targets characterized by a canonical seven transmembrane (TM) helix...

October 2022 Dimerization of β2-adrenergic receptor is responsible for the constitutive activity subjected to inverse agonism...

October 2022 "Visual phototransduction is the most extensively studied G protein-coupled receptor (GPCR) signaling pathway because of its...

October 2022 Discovery and In Vivo Evaluation of ACT-660602: A Potent and Selective Antagonist of the Chemokine Receptor CXCR3 for...

October 2022 "Understanding the dopaminergic system is a priority in neurobiology and neuropharmacology. Dopamine receptors are involved...

October 2022 "Understanding the activation of G protein-coupled receptors (GPCRs) is of paramount importance to the field of...

October 2022 "Adhesion G protein-coupled receptors (aGPCRs) are keys of many physiological events and attractive targets for various...

October 2022 "The canonical model for G protein-coupled receptors (GPCRs) activation assumes that stimulation of heterotrimeric G protein...

October 2022 "CXCR1 and CXCR2 chemokine receptors, mainly activated by interleukin 8 (IL-8 or CXCL8), are expressed in a variety of cells...