Article
Pharmaceutical-Grade Rigosertib Is a Microtubule-Destabilizing Agent.
Molecular cell - 2 Jul 2020
Jost Marco, Chen Yuwen, Gilbert Luke A, Horlbeck Max A, Krenning Lenno, Menchon Grégory, Rai Ankit, Cho Min Y, Stern Jacob J, Prota Andrea E, Kampmann Martin, Akhmanova Anna, Steinmetz Michel O, Tanenbaum Marvin E, Weissman Jonathan S
Abstract excerpt
We recently used CRISPRi/a-based chemical-genetic screens and cell biological, biochemical, and structural assays to determine that rigosertib, an anti-cancer agent in phase III clinical trials, kills cancer cells by destabilizing microtubules. Reddy and co-workers (Baker et al., 2020, this issue of Molecular Cell) suggest that a contaminating degradation product in commercial formulations of rigosertib is...
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