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Updated: Jul 7, 2025

Characterization of G Protein-coupled Receptors by a Fluorescence-based Calcium Mobilization Assay
11:49

Characterization of G Protein-coupled Receptors by a Fluorescence-based Calcium Mobilization Assay

Published on: July 28, 2014

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GPR39:一个孤儿受体乞求配体

Urszula Doboszewska1, Wolfgang Maret2, Piotr Wlaź3

  • 1Department of Pharmacobiology, Jagiellonian University Medical College, Medyczna 9, PL 30-688 Kraków, Poland.

Drug discovery today
|December 20, 2023
PubMed
概括

对G蛋白结合受体39 (GPR39) 的药理学数据不一致,阻碍了进展. 本综述批判性地评估了连接体识别,合成激素特异性和GPR39信号传导的治疗策略.

关键词:
14,15-EET 的时间.15-HETE 的意思是G-蛋白结合受体的受体.癌症 癌症 癌症 癌症 癌症心脏代谢疾病心脏代谢疾病甲化除甲化

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Brain Membrane Fractionation: An Ex Vivo Approach to Assess Subsynaptic Protein Localization09:49

Brain Membrane Fractionation: An Ex Vivo Approach to Assess Subsynaptic Protein Localization

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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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Heterotrimeric G proteins are guanine nucleotide-binding proteins. As the name suggests, heterotrimeric G proteins are composed of three subunits: alpha, beta, and gamma. They remain GDP-bound or GTP-bound inside the cells and switch between inactive/active states. The Gα subunit possesses the nucleotide-binding pocket that binds guanine nucleotides and switches between GDP or GTP-bound states. In contrast, the Gꞵ and Gγ subunits are always bound together with high...
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