Ontology highlight
ABSTRACT:
SUBMITTER: Popovici-Muller J
PROVIDER: S-EPMC5900343 | biostudies-literature | 2018 Apr
REPOSITORIES: biostudies-literature
ACS medicinal chemistry letters 20180119 4
Somatic point mutations at a key arginine residue (R132) within the active site of the metabolic enzyme isocitrate dehydrogenase 1 (IDH1) confer a novel gain of function in cancer cells, resulting in the production of d-2-hydroxyglutarate (2-HG), an oncometabolite. Elevated 2-HG levels are implicated in epigenetic alterations and impaired cellular differentiation. IDH1 mutations have been described in an array of hematologic malignancies and solid tumors. Here, we report the discovery of AG-120 ...[more]