Selective degradation of splicing factor CAPERÎ± by anticancer sulfonamides.

Nat. Chem. Biol.2017 Jun;13(6):675-680. Epub 2017 Apr 24

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mediated ubiquitination in human cancer cell lines. Both CRISPR-Cas9-based knockout of DCAF15 and a single amino acid substitution of CAPERÎ± conferred resistance against sulfonamide-induced CAPERÎ± degradation and cell-growth inhibition. Thus, these sulfonamides represent selective chemical probes for disrupting CAPERÎ± function and designate DCAFs as promising drug targets for promoting selective protein degradation in cancer therapy.

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Selective degradation of splicing factor CAPERÎ± by anticancer sulfonamides.

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