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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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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
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
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
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
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
Reversible Photocontrol of Dopaminergic Transmission in Wild-Type Animals
October 2022 "Understanding the dopaminergic system is a priority in neurobiology and neuropharmacology. Dopamine receptors are involved...

GPCR News
Sep 30, 20221 min read
Nanobodies as Probes and Modulators of Cardiovascular G Protein-Coupled Receptors
October 2022 "Understanding the activation of G protein-coupled receptors (GPCRs) is of paramount importance to the field of...

GPCR News
Sep 30, 20221 min read
Structural basis of adhesion GPCR GPR110 activation by stalk peptide and G-proteins coupling
October 2022 "Adhesion G protein-coupled receptors (aGPCRs) are keys of many physiological events and attractive targets for various...

GPCR News
Sep 30, 20221 min read
Endosomal parathyroid hormone receptor signaling
October 2022 "The canonical model for G protein-coupled receptors (GPCRs) activation assumes that stimulation of heterotrimeric G protein...

GPCR News
Sep 30, 20221 min read
Targeting CXCR1 and CXCR2 receptors in cardiovascular diseases
October 2022 "CXCR1 and CXCR2 chemokine receptors, mainly activated by interleukin 8 (IL-8 or CXCL8), are expressed in a variety of cells...

GPCR News
Sep 30, 20221 min read
Structural perspectives on the mechanism of signal activation, ligand selectivity and allosteric...
October 2022 Structural perspectives on the mechanism of signal activation, ligand selectivity and allosteric modulation in angiotensin...

GPCR News
Sep 30, 20221 min read
GPCR Agonist-to-Antagonist Conversion: Enabling the Design of Nucleoside Functional Switches for...
October 2022 GPCR Agonist-to-Antagonist Conversion: Enabling the Design of Nucleoside Functional Switches for the A2A Adenosine Receptor...

GPCR News
Sep 30, 20221 min read
Endogenous ligand recognition and structural transition of a human PTH receptor
October 2022 "Endogenous parathyroid hormone (PTH) and PTH-related peptide (PTHrP) bind to the parathyroid hormone receptor 1 (PTH1R) and...

GPCR News
Sep 30, 20221 min read
Coincident Regulation of PLCβ Signaling by Gq-Coupled and μOpioid Receptors Opposes Opioid- Mediated
October 2022 Coincident Regulation of PLCβ Signaling by Gq-Coupled and μOpioid Receptors Opposes Opioid- Mediated Antinociception "Pain...

GPCR News
Sep 30, 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
Sep 30, 20221 min read
Adenosine receptor signalling in Alzheimer's disease
October 2022 "Alzheimer's disease (AD) is the most common dementia in the elderly and its increasing prevalence presents treatment...

GPCR News
Sep 30, 20221 min read
Glucagon receptor-mediated regulation of gluconeogenic gene transcription is endocytosis-dependent..
October 2022 Glucagon receptor-mediated regulation of gluconeogenic gene transcription is endocytosis-dependent in primary hepatocytes "A...

GPCR News
Sep 30, 20221 min read
Keratinocyte-derived defensins activate neutrophil-specific receptors Mrgpra2a/b to prevent skin...
October 2022 Keratinocyte-derived defensins activate neutrophil-specific receptors Mrgpra2a/b to prevent skin dysbiosis and bacterial...

GPCR News
Sep 30, 20221 min read
Mechanistic Understanding of the Palmitoylation of Go Protein in the Allosteric Regulation of...
October 2022 Mechanistic Understanding of the Palmitoylation of Go Protein in the Allosteric Regulation of Adhesion Receptor GPR97...

GPCR News
Sep 30, 20221 min read
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