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Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding
10:13

Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding

Published on: June 9, 2017

Solution NMR spectroscopy of the human vasopressin V2 receptor, a G protein-coupled receptor

Changlin Tian1, Richard M Breyer, Hak Jun Kim

  • 1Center for Structural Biology and Department of Biochemistry, Vanderbilt University School of Medicine, Nashville, Tennessee 37232-8725, USA.

Journal of the American Chemical Society
|June 2, 2005
PubMed

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G-protein Coupled Receptors

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G Protein-coupled Receptors

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Activation and Inactivation of G Proteins

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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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Transducer Mechanism: Enzyme-Linked Receptors

Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
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