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• W2040473505 startingPage "156" @default.
• W2040473505 abstract "p90 ribosomal protein S6 kinases (RSKs) integrate upstream signals through two catalytic domains. Autophosphorylation of Ser386 by the regulatory C-terminal kinase domain (CTD) is thought to be essential for activation of the N-terminal kinase domain (NTD), which phosphorylates multiple downstream targets1. We recently reported fmk, an irreversible inhibitor of the CTD of RSK1 and RSK22. Here we describe fmk-pa, a propargylamine variant that has improved cellular potency and a 'clickable' tag for assessing the extent and selectivity of covalent RSK modification. Copper-catalyzed conjugation of an azidoalkyl reporter (the click reaction) revealed that fmk-pa achieves selective and saturable modification of endogenous RSK1 and RSK2 in mammalian cells. Saturating concentrations of fmk-pa inhibited Ser386 phosphorylation and downstream signaling in response to phorbol ester stimulation, but had no effect on RSK activation by lipopolysaccharide. RSK autoactivation by the CTD is therefore context dependent, which suggests that NTD and CTD inhibitors should have distinct physiological effects." @default.
• W2040473505 created "2016-06-24" @default.
• W2040473505 creator A5051950312 @default.
• W2040473505 creator A5065228408 @default.
• W2040473505 creator A5090535134 @default.
• W2040473505 date "2007-01-28" @default.
• W2040473505 modified "2023-10-10" @default.
• W2040473505 title "A clickable inhibitor reveals context-dependent autoactivation of p90 RSK" @default.
• W2040473505 cites W1542374364 @default.
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• W2040473505 doi "https://doi.org/10.1038/nchembio859" @default.
• W2040473505 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/3634365" @default.
• W2040473505 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/17259979" @default.
• W2040473505 hasPublicationYear "2007" @default.
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