Article
Anticancer sulfonamides target splicing by inducing RBM39 degradation via recruitment to DCAF15.
Science (New York, N.Y.) - 28 Apr 2017
Han Ting, Goralski Maria, Gaskill Nicholas, Capota Emanuela, Kim Jiwoong, Ting Tabitha C, Xie Yang, Williams Noelle S, Nijhawan Deepak
Abstract excerpt
Indisulam is an aryl sulfonamide drug with selective anticancer activity. Its mechanism of action and the basis for its selectivity have so far been unknown. Here we show that indisulam promotes the recruitment of RBM39 (RNA binding motif protein 39) to the CUL4-DCAF15 E3 ubiquitin ligase, leading to RBM39 polyubiquitination and proteasomal degradation. Mutations in RBM39 that prevent its recruitment to...
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