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Article

Delineation of molecular determinants for FR900359 inhibition of Gq/11 unlocks inhibition of Gαs.

The Journal of biological chemistry - 2 Oct 2020

Boesgaard Michael W, Harpsøe Kasper, Malmberg Michelle, Underwood Christina R, Inoue Asuka, Mathiesen Jesper M, König Gabriele M, Kostenis Evi, Gloriam David E, Bräuner-Osborne Hans

Abstract excerpt

Heterotrimeric G proteins are essential mediators of intracellular signaling of G protein-coupled receptors. The Gq/11 subfamily consists of Gq, G11, G14, and G16 proteins, of which all but G16 are inhibited by the structurally related natural products YM-254890 and FR900359. These inhibitors act by preventing the GDP/GTP exchange, which is necessary for activation of all G proteins. A homologous putative binding...

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Identifiers

PMID: 32753482
DOI: 10.1074/jbc.RA120.013002
PMCID: PMC7535923

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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