Selective Inhibition of Mutant Isocitrate Dehydrogenase 1 (IDH1) via Disruption of a Metal Binding Network by an Allosteric Small Molecule

Biochemical, Cellular, and Biophysical Characterization of a Potent Inhibitor of Mutant Isocitrate Dehydrogenase IDH1

(2014) Mindy I. Davis et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Mutant IDH1 Enhances the Production of 2-Hydroxyglutarate Due to Its Kinetic Mechanism

(2013) Alan R. Rendina et al.   BIOCHEMISTRY

An Inhibitor of Mutant IDH1 Delays Growth and Promotes Differentiation of Glioma Cells

(2013) D. Rohle et al.   SCIENCE

Targeted Inhibition of Mutant IDH2 in Leukemia Cells Induces Cellular Differentiation

(2013) F. Wang et al.   SCIENCE

Crystallographic Investigation and Selective Inhibition of Mutant Isocitrate Dehydrogenase

(2013) Baisong Zheng et al.   ACS Medicinal Chemistry Letters

Disruption of Wild-Type IDH1 Suppresses D-2-Hydroxyglutarate Production in IDH1-Mutated Gliomas

(2012) G. Jin et al.   CANCER RESEARCH

Transformation by the (R)-enantiomer of 2-hydroxyglutarate linked to EGLN activation

(2012) Peppi Koivunen et al.   NATURE

Discovery of the First Potent Inhibitors of Mutant IDH1 That Lower Tumor 2-HG in Vivo

(2012) Janeta Popovici-Muller et al.   ACS Medicinal Chemistry Letters

A Tale of Two Subunits: How the Neomorphic R132H IDH1 Mutation Enhances Production of αHG

(2011) Beth Pietrak et al.   BIOCHEMISTRY

Oncometabolite 2-Hydroxyglutarate Is a Competitive Inhibitor of α-Ketoglutarate-Dependent Dioxygenases

(2011) Wei Xu et al.   CANCER CELL

The oncometabolite 2-hydroxyglutarate inhibits histone lysine demethylases

(2011) Rasheduzzaman Chowdhury et al.   EMBO REPORTS

Features and development ofCoot

(2010) P. Emsley et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

Prognostic impact of IDH2 mutations in cytogenetically normal acute myeloid leukemia

(2010) F. Thol et al.   BLOOD

Leukemic IDH1 and IDH2 Mutations Result in a Hypermethylation Phenotype, Disrupt TET2 Function, and Impair Hematopoietic Differentiation

(2010) Maria E. Figueroa et al.   CANCER CELL

Molecular mechanisms of “off-on switch” of activities of human IDH1 by tumor-associated mutation R132H

(2010) Bei Yang et al.   CELL RESEARCH

Impact of IDH1 R132 Mutations and an IDH1 Single Nucleotide Polymorphism in Cytogenetically Normal Acute Myeloid Leukemia: SNP rs11554137 Is an Adverse Prognostic Factor

(2010) Katharina Wagner et al.   JOURNAL OF CLINICAL ONCOLOGY

IDH1 and IDH2 Mutations Are Frequent Genetic Alterations in Acute Myeloid Leukemia and Confer Adverse Prognosis in Cytogenetically Normal Acute Myeloid Leukemia With NPM1 Mutation Without FLT3 Internal Tandem Duplication

(2010) Peter Paschka et al.   JOURNAL OF CLINICAL ONCOLOGY

Isocitrate Dehydrogenase 1 and 2 Mutations in Cancer: Alterations at a Crossroads of Cellular Metabolism

(2010) Z. J. Reitman et al.   JNCI-Journal of the National Cancer Institute

The Control of the Metabolic Switch in Cancers by Oncogenes and Tumor Suppressor Genes

(2010) A. J. Levine et al.   SCIENCE

IDH mutations in glioma and acute myeloid leukemia

(2010) Lenny Dang et al.   TRENDS IN MOLECULAR MEDICINE

Cancer-associated IDH1 mutations produce 2-hydroxyglutarate

(2009) Lenny Dang et al.   NATURE

IDH1andIDH2Mutations in Gliomas

(2009) Hai Yan et al.   NEW ENGLAND JOURNAL OF MEDICINE

Glioma-Derived Mutations in IDH1 Dominantly Inhibit IDH1 Catalytic Activity and Induce HIF-1 

(2009) S. Zhao et al.   SCIENCE

BF3·Et2O catalyzed diastereoselective nucleophilic reactions of 3-silyloxypiperidine N,O-acetal with silyl enol ether and application to the asymmetric synthesis of (+)-febrifugine

(2009) Ru-Cheng Liu et al.   TETRAHEDRON LETTERS

An Integrated Genomic Analysis of Human Glioblastoma Multiforme

(2008) D. W. Parsons et al.   SCIENCE