Selective degradation of splicing factor CAPERα by anticancer sulfonamides
作者： Taku Yoshida , Miyuki Mabuchi , Akito Tanaka , Takashi Owa , Taisuke Uehara
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摘要: Target-protein degradation is an emerging field in drug discovery and development. In particular, the substrate-receptor proteins of cullin-ubiquitin ligase system play a key role selective protein degradation, which essential component anti-myeloma activity immunomodulatory drugs (IMiDs), such as lenalidomide. Here, we demonstrate that series anticancer sulfonamides NSC 719239 (E7820), indisulam, 339004 (chloroquinoxaline sulfonamide, CQS) induce proteasomal U2AF-related splicing factor coactivator activating protein-1 estrogen receptors (CAPERα) via CRL4DCAF15 mediated ubiquitination human cancer cell lines. Both CRISPR-Cas9-based knockout DCAF15 single amino acid substitution CAPERα conferred resistance against sulfonamide-induced cell-growth inhibition. Thus, these represent chemical probes for disrupting function designate DCAFs promising targets promoting therapy.
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