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Delineation of molecular determinants for FR900359 inhibition of G unlocks inhibition of Gα

J Biol Chem. 2020; 
Michael W Boesgaard, Kasper Harpsøe, Michelle Malmberg, Christina R Underwood, Asuka Inoue, Jesper M Mathiesen, Gabriele M König, Evi Kostenis, David E Gloriam, Hans Bräuner-Osborne
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Mutagenesis Services … For Gs, the cDNA transcript of the human GNASS gene (homo sapiens G protein subunit alpha s short, mRNA, accession: AF493898) was used. All cDNAs and derived mutants were purchased from GenScript (Piscataway, NJ, USA) as inserts in a pcDNA3.1(+) vector … Get A Quote

摘要

Heterotrimeric G proteins are essential mediators of intracellular signaling of G protein-coupled receptors. The Gq/11subfamily consists of G, G, G and G proteins of which all but G 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 site for YM-254890/FR900359 can also be found in members of the other three G protein families; G, G and G, but none of the published analogs of YM-254890/FR900359 have shown any inhibitory activity for any of these. To explain why the YM-254890/FR900359 scaffold only inhibits G, the present study delineated the m... More

关键词

FR900359, G protein, G protein inhibitor, G protein-coupled receptor (GPCR), Gq, Gs, YM-254890, inhibitor, molecular pharmacology, site-directed mutagenesis