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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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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
Oct 1, 20221 min read
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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
Oct 1, 20221 min read
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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
Oct 1, 20221 min read
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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
Oct 1, 20221 min read
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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
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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
Oct 1, 20221 min read
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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
Oct 1, 20221 min read
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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
Oct 1, 20221 min read
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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
Oct 1, 20221 min read
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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
Oct 1, 20222 min read
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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
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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
Oct 1, 20222 min read
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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
Oct 1, 20221 min read
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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
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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
Oct 1, 20221 min read
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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
Oct 1, 20221 min read
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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
Oct 1, 20221 min read
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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
Oct 1, 20221 min read
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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
Oct 1, 20221 min read
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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
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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
Oct 1, 20221 min read
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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
Oct 1, 20221 min read
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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
Oct 1, 20221 min read
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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
Oct 1, 20221 min read
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