Article
Inhibition of Mutated Isocitrate Dehydrogenase 1 in Cancer.
Medicinal chemistry (Shariqah (United Arab Emirates)) - 1 Jan 2018
Wu Fangrui, Cheng Gang, Yao Yuan, Kogiso Mari, Jiang Hong, Li Xiao-Nan, Song Yongcheng
Abstract excerpt
BACKGROUND: R132H mutation of isocitrate dehydrogenase 1 (IDH1) is found in ~75% of low-grade gliomas and secondary glioblastomas as well as in several other types of cancer. More chemotypes of inhibitors of IDH1(R132H) are therefore needed. OBJECTIVE: The study aimed to develop a new class of IDH1(R132H) inhibitors as potent antitumor agents. METHOD: A biochemical assay was developed to find inhibitors of...
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