Discovery and Optimization of 2H-1λ2-Pyridin-2-one Inhibitors of Mutant Isocitrate Dehydrogenase 1 for the Treatment of Cancer

Structure-Based Design and Identification of FT-2102 (Olutasidenib), a Potent Mutant-Selective IDH1 Inhibitor

(2020) Justin A. Caravella et al.   JOURNAL OF MEDICINAL CHEMISTRY

Vorasidenib (AG-881): A First-in-Class, Brain-Penetrant Dual Inhibitor of Mutant IDH1 and 2 for Treatment of Glioma

(2020) Zenon Konteatis et al.   ACS Medicinal Chemistry Letters

Predictive Models of Aqueous Solubility of Organic Compounds Built on A Large Dataset of High Integrity

(2019) Hongmao Sun et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Mutant Isocitrate Dehydrogenase Inhibitors as Targeted Cancer Therapeutics

(2019) Danielle Golub et al.   Frontiers in Oncology

Biological Role and Therapeutic Potential of IDH Mutations in Cancer

(2018) Matthew S. Waitkus et al.   CANCER CELL

A widely-applicable high-throughput cellular thermal shift assay (CETSA) using split Nano Luciferase

(2018) Natalia J. Martinez et al.   Scientific Reports

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

(2017) Daniel J. Urban et al.   Scientific Reports

IDH mutations in cancer and progress toward development of targeted therapeutics

(2016) L. Dang et al.   ANNALS OF ONCOLOGY

Idh1mutations contribute to the development of T-cell malignancies in genetically engineered mice

(2016) Zhenyue Hao et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

New IDH1 mutant inhibitors for treatment of acute myeloid leukemia

(2015) Ujunwa C Okoye-Okafor et al.   Nature Chemical Biology

The driver and passenger effects of isocitrate dehydrogenase 1 and 2 mutations in oncogenesis and survival prolongation

(2014) Remco J. Molenaar et al.   BIOCHIMICA ET BIOPHYSICA ACTA-REVIEWS ON CANCER

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

(2014) Gejing Deng et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

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

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

Serum 2-hydroxyglutarate levels predict isocitrate dehydrogenase mutations and clinical outcome in acute myeloid leukemia

(2013) C. D. DiNardo et al.   BLOOD

What a difference a hydroxyl makes: mutant IDH, (R)-2-hydroxyglutarate, and cancer

(2013) J.-A. Losman et al.   GENES & DEVELOPMENT

(R)-2-Hydroxyglutarate Is Sufficient to Promote Leukemogenesis and Its Effects Are Reversible

(2013) J.-A. Losman et al.   SCIENCE

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

(2013) D. Rohle et al.   SCIENCE

Oncogenic Isocitrate Dehydrogenase Mutations: Mechanisms, Models, and Clinical Opportunities

(2013) R. A. Cairns et al.   Cancer Discovery

Frequent IDH1/2 mutations in intracranial chondrosarcoma: a possible diagnostic clue for its differentiation from chordoma

(2012) Motohiro Arai et al.   Brain Tumor Pathology

IDH mutation impairs histone demethylation and results in a block to cell differentiation

(2012) Chao Lu et al.   NATURE

IDH1 mutation is sufficient to establish the glioma hypermethylator phenotype

(2012) Sevin Turcan et al.   NATURE

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

Acute Myeloid Leukemia WithIDH1orIDH2Mutation

(2010) Keyur P. Patel et al.   AMERICAN JOURNAL OF CLINICAL PATHOLOGY

The Common Feature of Leukemia-Associated IDH1 and IDH2 Mutations Is a Neomorphic Enzyme Activity Converting α-Ketoglutarate to 2-Hydroxyglutarate

(2010) Patrick S. Ward et al.   CANCER CELL

Cancer-associated metabolite 2-hydroxyglutarate accumulates in acute myelogenous leukemia with isocitrate dehydrogenase 1 and 2 mutations

(2010) Stefan Gross et al.   JOURNAL OF EXPERIMENTAL MEDICINE

Erratum: Cancer-associated IDH1 mutations produce 2-hydroxyglutarate

(2010) Lenny Dang et al.   NATURE

Cancer-associated IDH mutations: biomarker and therapeutic opportunities

(2010) K E Yen et al.   ONCOGENE

Cancer-associated IDH1 mutations produce 2-hydroxyglutarate

(2009) Lenny Dang et al.   NATURE

Recurring Mutations Found by Sequencing an Acute Myeloid Leukemia Genome

(2009) Elaine R. Mardis et al.   NEW ENGLAND JOURNAL OF MEDICINE

IDH1andIDH2Mutations in Gliomas

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