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Article

Assessing inhibitors of mutant isocitrate dehydrogenase using a suite of pre-clinical discovery assays.

Scientific reports - 6 Oct 2017

Urban Daniel J, Martinez Natalia J, Davis Mindy I, Brimacombe Kyle R, Cheff Dorian M, Lee Tobie D, Henderson Mark J, Titus Steven A, Pragani Rajan, Rohde Jason M, Liu Li, Fang Yuhong, Karavadhi Surendra, Shah Pranav, Lee Olivia W, Wang Amy, McIver Andrew, Zheng Hongchao, Wang Xiaodong, Xu Xin, Jadhav Ajit, Simeonov Anton, Shen Min, Boxer Matthew B, Hall Matthew D

Abstract excerpt

Isocitrate dehydrogenase 1 and 2 (IDH1 and IDH2) are key metabolic enzymes that are mutated in a variety of cancers to confer a gain-of-function activity resulting in the accumulation of an oncometabolite, D-2-hydroxyglutarate (2-HG). Accumulation of 2-HG can result in epigenetic dysregulation and a block in cellular differentiation, suggesting these mutations play a role in neoplasia. Based on its potential as a...

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Identifiers

PMID: 28986582
DOI: 10.1038/s41598-017-12630-x
PMCID: PMC5630632

Genes

IDH1
IDH2

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 5 Sept 2026. Manifest publication-graph-cohort-2026-09-05.1.

Source receipt: pubmed, retrieved 5 Sept 2026.

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