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...
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GPCR News
- Nov 1, 2022
- 1 min
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...
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GPCR News
- Oct 1, 2022
- 1 min
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...
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GPCR News
- Oct 1, 2022
- 1 min
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...
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GPCR News
- Oct 1, 2022
- 1 min
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...
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GPCR News
- Oct 1, 2022
- 1 min
Network pharmacological investigation into the mechanism of Kaixinsan powder for the treatment of...
October 2022 Network pharmacological investigation into the mechanism of Kaixinsan powder for the treatment of depression "Kaixinsan...
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GPCR News
- Aug 1, 2022
- 1 min
In vitro assays for the functional characterization of (psychedelic) substances at the serotonin...
August 2022 In vitro assays for the functional characterization of (psychedelic) substances at the serotonin receptor 5-HT2A R...
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GPCR News
- Aug 1, 2022
- 1 min
Therapeutic validation of an orphan G protein-coupled receptor: The case of GPR84
August 2022 "Despite the importance of members of the GPCR superfamily as targets of a broad range of effective medicines many GPCRs...
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GPCR News
- Aug 1, 2022
- 1 min
Exploring pharmacological inhibition of G q/11 as an analgesic strategy
August 2022 "Background and purpose: Misuse of opioids has greatly affected our society. One potential solution is to develop analgesics...
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GPCR News
- Aug 1, 2022
- 1 min
Fluorescent Ligands Targeting Intracellular Allosteric Binding Site of the Chemokine Receptor CCR2
August 2022 "Fluorescently labeled ligands are versatile molecular tools to study G protein-coupled receptors (GPCRs) and can be used for...
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GPCR News
- Aug 1, 2022
- 1 min
Synthesis and characterization of an orally bioavailable small molecule agonist of the apelin recept
August 2022 "The apelin receptor (APJ) is a target for cardiovascular indications. Previously, we had identified a novel pyrazole-based...
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GPCR News
- Aug 1, 2022
- 1 min
Pharmacophore-guided Virtual Screening to Identify New β 3 -adrenergic Receptor Agonists
August 2022 "Abstract The β3 -adrenergic receptor (β3 -AR) is found in several tissues such as adipose tissue and urinary bladder. It is...
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GPCR News
- Aug 1, 2022
- 1 min
Effects of Small Molecule Ligands on ACKR3 Receptors
August 2022 "Abstract Chemokines such as stromal derived factor 1 and their G protein coupled receptors are well-known regulators of the...
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GPCR News
- Aug 1, 2022
- 1 min
A new Kunitz-type snake toxin family associated with an original mode of interaction with the...
August 2022 A new Kunitz-type snake toxin family associated with an original mode of interaction with the vasopressin 2 receptor...
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GPCR News
- Aug 1, 2022
- 1 min
Discovery of 3(2-aminoethyl)-thiazolidine-2,4-diones as a novel chemotype of sigma-1 receptor ligand
August 2022 "Abstract Sigma receptor is a transmembrane non-GPCR protein expressed mainly in the endoplasmic reticulum membrane...
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GPCR News
- Aug 1, 2022
- 1 min
Actions of Parathyroid Hormone Ligand Analogues in Humanized PTH1R Knockin Mice
August 2022 "Abstract Rodent models are commonly used to evaluate parathyroid hormone (PTH) and PTH-related protein (PTHrP) ligands and...
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GPCR News
- Dec 23, 2021
- 1 min
Precise druggability of the PTH type 1 receptor
Class B G protein-coupled receptors (GPCRs) are notoriously difficult to target by small molecules because their large orthosteric...
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GPCR News
- Dec 22, 2021
- 1 min
A Chemical Biology Toolbox Targeting the Intracellular Binding Site of CCR9: Fluorescent Ligands ...
A conserved intracellular allosteric binding site (IABS) has recently been identified at several G protein-coupled receptors (GPCRs)....
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GPCR News
- Dec 17, 2021
- 1 min
Applications of Cryo-EM in small molecule and biologics drug design
Electron cryo-microscopy (cryo-EM) is a powerful technique for the structural characterization of biological macromolecules, enabling...
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GPCR News
- Dec 12, 2021
- 1 min
Opioid Receptors and Protonation-Coupled Binding of Opioid Drugs
Opioid receptors are G-protein-coupled receptors (GPCRs) part of cell signaling paths of direct interest to treat pain. Pain may...
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