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AAT Bioquest

What are the applications of GPCRs?

Posted September 27, 2023


Answer

One application of G protein coupled receptors (GPCRs) is their use in drug testing. They can affect insulin activity and secretion, and elongation of B cells. Thus, GPCRs are used as targets for treating diabetes. For example, the GPR40 fatty receptor may strengthen the function of islet B cells and induce insulin secretion. It may additionally improve the body’s ability to uptake insulin via activating GPCRs. The FDA has approved over 520 drugs which target GPCRs. Serotonin, dopamine, opioids, histamine and adrenergic receptors are the most commonly targeted GPCRs. GPCRs are also involved in neuroscience as they are commonly targeted in producing novel therapeutics for CNS disorders. This is important as studies show GPCRs are involved in the pathogenesis of neurodegenerative disorders including Alzheimer's, Parkinson’s disease, and Huntington’s disease, all of which still do not have a cure. By understanding and gathering more information about GPCR signaling pathways in these diseases, researchers are better able to work towards finding treatments.

Additional resources

Novel targets for potential therapeutic use in Diabetes mellitus

G-Protein-Coupled Receptors (GPCR)

Cell Meter™ Beta-Arrestin Translocation GPCR Signaling Kit