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Article

Identification and characterization of a novel mutant isocitrate dehydrogenase 1 inhibitor for glioma treatment.

Biochemical and biophysical research communications - 30 Apr 2021

Zhang Na, Zheng Bowen, Yao Xiaojun, Huang Xiaoming, Du Jingjing, Shen Yunfu, Huang Zhe, Chen Junhe, Lin Qianyu, Lan Wenjian, Lin Wanjun, Ma Wenzhe

Abstract excerpt

Isocitrate dehydrogenase 1 (IDH1) mutant R132H, promoting the oncometabolite D-2-hydroxyglutarate (D2HG), is a driver mutation and an emerging therapeutic target in glioma. This study identified a novel mutant IDH1 inhibitor, WM17, by virtual screening and enzymatic confirmation. It could bind to and increase mutant IDH1 protein's thermostability in both endogenous heterozygous cells and exogenous overexpressed...

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PMID: 33714758
DOI: 10.1016/j.bbrc.2021.02.112

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