Article
Selective depletion of mutant p53 by cancer chemopreventive isothiocyanates and their structure-activity relationships.
Journal of medicinal chemistry - 10 Feb 2011
Wang Xiantao, Di Pasqua Anthony J, Govind Sudha, McCracken Erin, Hong Charles, Mi Lixin, Mao Yuehua, Wu Jessie Yu-Chieh, Tomita York, Woodrick Jordan C, Fine Robert L, Chung Fung-Lung
Abstract excerpt
Isothiocyanates (ITCs) derived from cruciferous vegetables induce apoptosis in cancer cells. We demonstrate that certain naturally occurring ITCs selectively deplete mutant p53 but not the wild-type and do so via a transcription-independent mechanism. Direct p53 binding followed by conformational changes appears to be a mechanism by which mutant p53 is depleted. Structure-activity relationship studies (SARs)...
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