Ontology highlight
ABSTRACT:
SUBMITTER: Okoye-Okafor UC
PROVIDER: S-EPMC5155016 | biostudies-literature | 2015 Nov
REPOSITORIES: biostudies-literature
Nature chemical biology 20151005 11
Neomorphic mutations in isocitrate dehydrogenase 1 (IDH1) are driver mutations in acute myeloid leukemia (AML) and other cancers. We report the development of new allosteric inhibitors of mutant IDH1. Crystallographic and biochemical results demonstrated that compounds of this chemical series bind to an allosteric site and lock the enzyme in a catalytically inactive conformation, thereby enabling inhibition of different clinically relevant IDH1 mutants. Treatment of IDH1 mutant primary AML cells ...[more]