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Insights That Move the GPCR Field Forward
Read the latest analyses, interviews, and discoveries shaping the GPCR ecosystem — from research breakthroughs to biotech strategy.
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Competitive vs Non-Competitive GPCR Antagonists: How to Interpret Pharmacology Data with Confidence
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.

Dr. GPCR News
Aug 145 min read


Why Kinetics Matter More Than Kd in GPCR Drug Discovery
Welcome GPCR Fans,  Every discovery-phase decision you make shapes your entire pipeline trajectory—and understanding when equilibrium...

Dr. GPCR News
Jul 244 min read


Your GPCR Program Decisions Depend on Good Data Interpretation
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.

Dr. GPCR News
Jul 174 min read
Targeting Intracellular Allosteric Sites in GPCRs
Exploring the intracellular allosteric site GPCRs represent one of the largest and most vital families of cell surface receptors, playing...

Inês Pinheiro
Nov 1, 20234 min read
Decoding β-Arrestins: from Structure to function
Fine-tuning GPCR signaling: conformational dynamics and intracellular responses GPCR signaling is a complex process modulated by protein...

Inês Pinheiro
Aug 21, 20235 min read
Structural landscape of the Chemokine Receptor system
Chemokine receptors (CKRs) belong to a subfamily of G-protein-coupled receptors (GPCRs) and play a crucial role in inflammation and...

Inês Pinheiro
Jun 28, 20237 min read
Artificial intelligence – faster, smarter, cheaper GPCR drug discovery
Artificial intelligence - Machine learning vs Deep Learning GPCRs have long been recognized as important drug targets, and numerous drugs...

Inês Pinheiro
May 16, 20235 min read
Emerging approaches for decoding neuropeptide transmission
November 2022 "Neuropeptides produce robust effects on behavior across species, and recent research has benefited from advances in...

GPCR News
Oct 31, 20221 min read
Location bias contributes to functionally selective responses of biased CXCR3 agonists
November 2022 "Some G protein-coupled receptor (GPCR) ligands act as "biased agonists" that preferentially activate specific signaling...

GPCR News
Oct 31, 20221 min read
Deciphering the signaling mechanisms of β-arrestin1 and β-arrestin2 in regulation of cancer cell...
November 2022 Deciphering the signaling mechanisms of β-arrestin1 and β-arrestin2 in regulation of cancer cell cycle and metastasis...

GPCR News
Oct 31, 20221 min read
Structure-Based Discovery of Negative Allosteric Modulators of the Metabotropic Glutamate Receptor 5
November 2022 "Recently determined structures of class C G protein-coupled receptors (GPCRs) revealed the location of allosteric binding...

GPCR News
Oct 31, 20221 min read
Structural insights into adhesion GPCR ADGRL3 activation and Gq, Gs, Gi, and G12 coupling
November 2022 "Adhesion G-protein-coupled receptors (aGPCRs) play key roles in a diversity of physiologies. A hallmark of aGPCR...

GPCR News
Oct 31, 20221 min read
Conservation of Allosteric Ligand Binding Sites in G-Protein Coupled Receptors
November 2022 "Despite the growing number of G protein-coupled receptor (GPCR) structures, only 39 structures have been cocrystallized...

GPCR News
Oct 31, 20221 min read
Dimerization of β2-adrenergic receptor is responsible for the constitutive activity subjected to inv
November 2022 "Dimerization of beta 2-adrenergic receptor (β2-AR) has been observed across various physiologies. However, the function of...

GPCR News
Oct 31, 20221 min read
High hedgehog signaling is transduced by a multikinase-dependent switch controlling the...
October 2022 High hedgehog signaling is transduced by a multikinase-dependent switch controlling the apico-basal distribution of the GPCR...

GPCR News
Sep 30, 20221 min read
Structure of the vasopressin hormone-V2 receptor-β-arrestin1 ternary complex
October 2022 "Arrestins interact with G protein-coupled receptors (GPCRs) to stop G protein activation and to initiate key signaling...

GPCR News
Sep 30, 20221 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
Sep 30, 20221 min read
Mechanistic basis of GPCR activation explored by ensemble refinement of crystallographic structures
October 2022 "G protein-coupled receptors (GPCRs) are important drug targets characterized by a canonical seven transmembrane (TM) helix...

GPCR News
Sep 30, 20221 min read
Increased Anxiety-like Behaviors in Adgra1-/- Male But Not Female Mice are Attributable to...
October 2022 Increased Anxiety-like Behaviors in Adgra1-/- Male But Not Female Mice are Attributable to Elevated Neuron Dendrite Density,...

GPCR News
Sep 30, 20221 min read
Dimerization of β2-adrenergic receptor is responsible for the constitutive activity subjected to...
October 2022 Dimerization of β2-adrenergic receptor is responsible for the constitutive activity subjected to inverse agonism...

GPCR News
Sep 30, 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
Sep 30, 20221 min read
Case Report of a Juvenile Patient with Autism Spectrum Disorder with a Novel Combination of Copy...
October 2022 Case Report of a Juvenile Patient with Autism Spectrum Disorder with a Novel Combination of Copy Number Variants in ADGRL3...

GPCR News
Sep 30, 20221 min read
Discovery and In Vivo Evaluation of ACT-660602: A Potent and Selective Antagonist of the Chemokine..
October 2022 Discovery and In Vivo Evaluation of ACT-660602: A Potent and Selective Antagonist of the Chemokine Receptor CXCR3 for...

GPCR News
Sep 30, 20221 min read
Recurrent hypoglycemia increases hepatic gluconeogenesis without affecting glycogen metabolism or sy
October 2022 Recurrent hypoglycemia increases hepatic gluconeogenesis without affecting glycogen metabolism or systemic lipolysis in rat...

GPCR News
Sep 30, 20221 min read
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