Article
Structural bioinformatics-based design of selective, irreversible kinase inhibitors.
Science (New York, N.Y.) - 27 May 2005
Cohen Michael S, Zhang Chao, Shokat Kevan M, Taunton Jack
Abstract excerpt
The active sites of 491 human protein kinase domains are highly conserved, which makes the design of selective inhibitors a formidable challenge. We used a structural bioinformatics approach to identify two selectivity filters, a threonine and a cysteine, at defined positions in the active site of p90 ribosomal protein S6 kinase (RSK). A fluoromethylketone inhibitor, designed to exploit both selectivity filters,...
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