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Rediocide A, an Insecticide, Induces G-protein-coupled Receptor Desensitization via Activation of Conventional Protein Kinase C. J. Nat. Prod., 2012, 75: 1058–1062.

来源: J. Nat. Prod.日期: 2015-01-29

Abstract:

In order to identify small-molecule antagonists of Methuselah (Mth), a Drosophila G-protein-coupled receptor (GPCR) involved in life-span control, a library of natural compounds was screened, and it was found that rediocide A (1), a daphnane ester from the roots of Trigonostemon reidioides and used currently for flea control, potently inhibited calcium mobilization mediated by this receptor. Compound 1 inhibited calcium mobilization in GPCRs other than Mth, indicating that the inhibitory effect was not due to receptor antagonism but rather to a more general mechanism. It was found that 1 can induce GPCR desensitization and internalization, and such effects were mediated by the activation of conventional protein kinase C.


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