Ontology highlight
ABSTRACT:
SUBMITTER: Zheng M
PROVIDER: S-EPMC5546478 | biostudies-literature | 2017 Jul
REPOSITORIES: biostudies-literature
Zheng Mengzhu M Sun Weiguang W Gao Suyu S Luan Shanshan S Li Dan D Chen Renqi R Zhang Qian Q Chen Lixia L Huang Jiangeng J Li Hua H
Oncotarget 20170701 27
Isocitrate dehydrogenase (IDH) plays an indispensable role in the tricarboxylic acid cycle, and IDH mutations are present in nearly 75% of glioma and 20% of acute myeloid leukemia. One IDH1R132H inhibitor (clomifene citrate) was found by virtual screening method, which can selectively suppress mutant enzyme activities in vitro and in vivo with a dose-dependent manner. The molecular docking indicated that clomifene occupied the allosteric site of the mutant IDH1. Enzymatic kinetics also demonstra ...[more]