Article
Synthetic lethality by targeting EZH2 methyltransferase activity in ARID1A-mutated cancers.
Nature medicine - 1 Mar 2015
Bitler Benjamin G, Aird Katherine M, Garipov Azat, Li Hua, Amatangelo Michael, Kossenkov Andrew V, Schultz David C, Liu Qin, Shih Ie-Ming, Conejo-Garcia Jose R, Speicher David W, Zhang Rugang
Abstract excerpt
The gene encoding ARID1A, a chromatin remodeler, shows one of the highest mutation rates across many cancer types. Notably, ARID1A is mutated in over 50% of ovarian clear cell carcinomas, which currently have no effective therapy. To date, clinically applicable targeted cancer therapy based on ARID1A mutational status has not been described. Here we show that inhibition of the EZH2 methyltransferase acts in a...
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