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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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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
Sep 30, 20222 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
Sep 30, 20221 min read
Adrenal G Protein-Coupled Receptors and the Failing Heart: A Long-distance, Yet Intimate Affair
October 2022 "Systolic heart failure (HF) is a chronic clinical syndrome characterized by the reduction in cardiac function and still...

GPCR News
Sep 30, 20222 min read
GB83, an Agonist of PAR2 with a Unique Mechanism of Action Distinct from Trypsin and PAR2-AP
October 2022 "Protease-activated receptor 2 (PAR2) is a G-protein-coupled receptor (GPCR) activated by proteolytic cleavage of its...

GPCR News
Sep 30, 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
Sep 30, 20221 min read
Comparative studies of AlphaFold, RoseTTAFold and Modeller: a case study involving the use of...
October 2022 Comparative studies of AlphaFold, RoseTTAFold and Modeller: a case study involving the use of G-protein-coupled receptors...

GPCR News
Sep 30, 20221 min read
Mechanism of enhanced sensitivity of mutated β-adrenergic-like octopamine receptor to amitraz in...
October 2022 Mechanism of enhanced sensitivity of mutated β-adrenergic-like octopamine receptor to amitraz in honeybee Apis mellifera: An...

GPCR News
Sep 30, 20221 min read
Enhanced membrane binding of oncogenic G protein αqQ209L confers resistance to inhibitor YM-254890
October 2022 "Heterotrimeric G proteins couple activated G protein-coupled receptors (GPCR) to intracellular signaling pathways. They can...

GPCR News
Sep 30, 20221 min read
N-terminal alterations turn the gut hormone GLP-2 into an antagonist with gradual loss of GLP-2 ...
October 2022 N-terminal alterations turn the gut hormone GLP-2 into an antagonist with gradual loss of GLP-2 receptor selectivity towards...

GPCR News
Sep 30, 20221 min read
PH-Binding Motif in PAR4 Oncogene: From Molecular Mechanism to Drug Design
October 2022 "While the role of G-protein-coupled receptors (GPCR) in cancer is acknowledged, their underlying signaling pathways are...

GPCR News
Sep 30, 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
Sep 30, 20221 min read
Membrane Lipids Are an Integral Part of Transmembrane Allosteric Sites in GPCRs: A Case Study of...
October 2022 Membrane Lipids Are an Integral Part of Transmembrane Allosteric Sites in GPCRs: A Case Study of Cannabinoid CB1 Receptor...

GPCR News
Sep 30, 20221 min read
Advancements in G protein-coupled receptor biosensors to study GPCR-G protein coupling
October 2022 "Enzymatic and cellular signalling biosensors are used to decipher the activities of complex biological systems. Biosensors...

GPCR News
Sep 30, 20221 min read
Diversification of PAR signaling through receptor crosstalk
October 2022 "Protease activated receptors (PARs) are among the first receptors shown to transactivate other receptors: noticeably, these...

GPCR News
Sep 30, 20221 min read
Comparative study of neuropeptide signaling systems in Hemiptera
October 2022 "Numerous physiological processes in insects are tightly regulated by neuropeptides and their receptors. Although they form...

GPCR News
Sep 30, 20221 min read
Lysosomal GPCR-like protein LYCHOS signals cholesterol sufficiency to mTORC1
October 2022 "Lysosomes coordinate cellular metabolism and growth upon sensing of essential nutrients, including cholesterol. Through...

GPCR News
Sep 30, 20221 min read
Genome-scale CRISPR screening reveals that C3aR signaling is critical for rapid capture of fungi...
October 2022 Genome-scale CRISPR screening reveals that C3aR signaling is critical for rapid capture of fungi by macrophages "The fungal...

GPCR News
Sep 30, 20222 min read
Successful prednisolone or calcimimetic treatment of acquired hypocalciuric hypercalcemia caused...
October 2022 Successful prednisolone or calcimimetic treatment of acquired hypocalciuric hypercalcemia caused by biased allosteric CaSR...

GPCR News
Sep 30, 20221 min read
Developing the Cannabinoid Receptor 2 (CB2) pharmacopoeia: past, present, and future
October 2022 "Cannabinoid Receptor 2 (CB2) is a G protein-coupled receptor (GPCR) with considerable, though as yet unrealised,...

GPCR News
Sep 30, 20221 min read
The microglial endocannabinoid system similarly regulated by lipopolysaccharide and interferon gamma
October 2022 "Perturbation of the endocannabinoid system can have profound effects on immune function and synaptic plasticity. Microglia...

GPCR News
Sep 30, 20221 min read
Label-free LC-MS based assay to characterize small molecule compound binding to cells
October 2022 "Study of small molecule binding to live cells provides important information on the characterization of ligands...

GPCR News
Sep 30, 20221 min read
Pepducin-mediated G Protein-Coupled Receptor Signaling in the Cardiovascular System
October 2022 "Pepducins are small-lipidated peptides designed from the intracellular loops of G protein-coupled receptors (GPCRs) that...

GPCR News
Sep 30, 20221 min read
The regulation of PKA signaling in obesity and in the maintenance of metabolic health
October 2022 "The cAMP-dependent protein kinase (PKA) system represents a primary cell-signaling pathway throughout systems and across...

GPCR News
Sep 30, 20221 min read
G protein-biased GPR3 signaling ameliorates amyloid pathology in a preclinical Alzheimer's disease..
October 2022 "Biased G protein-coupled receptor (GPCR) ligands, which preferentially activate G protein or β-arrestin signaling pathways,...

GPCR News
Sep 30, 20221 min read
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