Related Experiment Video

Updated: Aug 30, 2026

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

Identification of surrogate ligands for orphan G protein-coupled receptors

Shigeki Takeda1, Atsushi Yamamoto, Tomoaki Okada

  • 1Institute for Biomolecular Science, Gakushuin University, 1-5-1 Mejiro, Tokyo 171-8588, Toshima-ku, Japan. tasuya.haga@gakushuin.ac.jp

Life Sciences
|November 11, 2003
PubMed

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G Protein-coupled Receptors

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G Protein-coupled Receptors

G-protein-coupled receptors are ligand-binding receptors that indirectly affect changes in the cell. The actual receptor is a single polypeptide that traverses the cell membrane seven times, creating intracellular and extracellular loops. The extracellular loops create a ligand-specific pocket which binds to neurotransmitters or hormones. The intracellular loops hold onto the G-protein.The G-protein, or guanine nucleotide-binding protein, is a large heterotrimeric complex. Its three subunits...
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Transducer Mechanism: G Protein–Coupled Receptors

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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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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