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Updated: Jul 10, 2025

G Protein-selective GPCR Conformations Measured Using FRET Sensors in a Live Cell Suspension Fluorometer Assay
09:12

G Protein-selective GPCR Conformations Measured Using FRET Sensors in a Live Cell Suspension Fluorometer Assay

Published on: September 10, 2016

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2024年GproteinDb:新的G蛋白-GPCR合,AlphaFold2-多重模型和接口相互作用

Gáspár Pándy-Szekeres1,2, Luis P Taracena Herrera1, Jimmy Caroli1

  • 1Department of Drug Design and Pharmacology, University of Copenhagen, 2100 Copenhagen, Denmark.

Nucleic acids research
|November 24, 2023
PubMed
概括

G蛋白结合受体 (GPCRs) 对药物的作用至关重要. 现在GproteinDb提供了扩展的数据和先进的工具,包括AlphaFold2模型,用于分析GPCR-G蛋白相互作用和选择性.

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G Protein–Coupled Receptors (GPCRs) are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to various stimuli. GPCRs regulate critical physiological pathways and are excellent drug targets for treating diseases such as diabetes, cancer, obesity, depression, or Alzheimer's. Nearly 35% of approved drugs implement their therapeutic effects by selectively interacting with specific GPCRs.
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Multiprotein signaling complexes are formed in a dynamic process involving protein-protein interactions at the cytoplasmic domain of transmembrane receptors or enzymatic and non-enzymatic proteins associated with the receptor. These complexes ensure the activation and propagation of intracellular signals that regulate cell functions.
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Interaction domains recognize exposed features of their binding partners containing post-translationally modified sequences,...
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G protein-coupled receptor (GPCR) signaling plays a crucial role in cell functioning. GPCR desensitization is an equally essential process. It allows cells to respond to changing environments and regain sensitivity to new stimuli while preventing unnecessary stimulation when no longer needed. Prolonged exposure to stimuli leads to GPCR desensitization. It involves blocking the receptors from binding and activating additional G proteins. This inhibits activation of downstream effectors, thereby...
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