ArticleScientific reports2017
Assessing inhibitors of mutant isocitrate dehydrogenase using a suite of pre-clinical discovery assays.
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Article in Scientific reports, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 43 papers.
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43citing papers in PubMed
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Who cites it
43 citing papers in PubMed.
- Olutasidenib in combination with azacitidine induces durable complete remissions in patients with relapsed or refractory mIDH1 acute myeloid leukemia: a multicohort open-label phase 1/2 trial.Journal of hematology & oncology · 2025Trial
- Targeting Lung Cancer Metabolism: Therapeutic Opportunities and Challenges.Advances in experimental medicine and biology · 2026Review
- State of the Art of IDH Inhibitors: Emerging Questions and Perspectives.Anti-cancer agents in medicinal chemistry · 2026Review
- IDH status dictates oHSV mediated metabolic reprogramming affecting anti-tumor immunity.Nature communications · 2025Article
- Genetics and Molecular Pathogenesis of the Chondrosarcoma: A Review of the Literature.Current issues in molecular biology · 2024Review
- Radiosynthesis and biological evaluation of [European journal of nuclear medicine and molecular imaging · 2024Article
- Electrochemical Nanoreactor Provides a Comprehensive View of Isocitrate Dehydrogenase Cancer-drug Kinetics.Angewandte Chemie (Weinheim an der Bergstrasse, Germany) · 2023Article
- Electrochemical Nanoreactor Provides a Comprehensive View of Isocitrate Dehydrogenase Cancer-drug Kinetics.Angewandte Chemie (International ed. in English) · 2023Article
- Isocitrate Dehydrogenase 1 Mutation and Ivosidenib in Patients With Acute Myeloid Leukemia: A Comprehensive Review.Cureus · 2023Review
- The curious case of IDH mutant acute myeloid leukaemia: biochemistry and therapeutic approaches.Biochemical Society transactions · 2023Review
- Oxazolidinones as versatile scaffolds in medicinal chemistry.RSC medicinal chemistry · 2023Review
- Zinc Finger MYND-Type Containing 8 (ZMYND8) Is Epigenetically Regulated in Mutant Isocitrate Dehydrogenase 1 (IDH1) Glioma to Promote Radioresistance.Clinical cancer research : an official journal of the American Association for Cancer Research · 2023Article
- Differentiating Inhibition Selectivity and Binding Affinity of Isocitrate Dehydrogenase 1 Variant Inhibitors.Journal of medicinal chemistry · 2023Article
- Mutated Isocitrate Dehydrogenase (mIDH) as Target for PET Imaging in Gliomas.Molecules (Basel, Switzerland) · 2023Review
- Wild-type IDH1 inhibition enhances chemotherapy response in melanoma.Journal of experimental & clinical cancer research : CR · 2022Article
- Resistance to the isocitrate dehydrogenase 1 mutant inhibitor ivosidenib can be overcome by alternative dimer-interface binding inhibitors.Nature communications · 2022Article
- Limited nutrient availability in the tumor microenvironment renders pancreatic tumors sensitive to allosteric IDH1 inhibitors.Nature cancer · 2022Article
- Discovery of Small-Molecule VapC1 Nuclease Inhibitors by Virtual Screening and Scaffold Hopping from an Atomic Structure Revealing Protein-Protein Interactions with a Native VapB1 Inhibitor.Journal of chemical information and modeling · 2022Article
- Metabolic Rewiring in Glioblastoma Cancer:Frontiers in oncology · 2022Review
- A D-2-hydroxyglutarate biosensor based on specific transcriptional regulator DhdR.Nature communications · 2021Article
Corrections and comments
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Authors and funding
25 authors.
Daniel J UrbanNCATS Chemical Genomics Center, National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland, 20850, United States.
Natalia J MartinezNCATS Chemical Genomics Center, National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland, 20850, United States.
Mindy I DavisNCATS Chemical Genomics Center, National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland, 20850, United States.
Kyle R BrimacombeNCATS Chemical Genomics Center, National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland, 20850, United States.
Dorian M CheffNCATS Chemical Genomics Center, National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland, 20850, United States.
Tobie D LeeNCATS Chemical Genomics Center, National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland, 20850, United States.
Mark J HendersonNCATS Chemical Genomics Center, National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland, 20850, United States.
Steven A TitusNCATS Chemical Genomics Center, National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland, 20850, United States.
Rajan PraganiNCATS Chemical Genomics Center, National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland, 20850, United States.
Jason M RohdeNCATS Chemical Genomics Center, National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland, 20850, United States.
Li LiuNCATS Chemical Genomics Center, National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland, 20850, United States.
Yuhong FangNCATS Chemical Genomics Center, National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland, 20850, United States.
Surendra KaravadhiNCATS Chemical Genomics Center, National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland, 20850, United States.
Pranav ShahNCATS Chemical Genomics Center, National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland, 20850, United States.
Olivia W LeeNCATS Chemical Genomics Center, National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland, 20850, United States.
Amy WangNCATS Chemical Genomics Center, National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland, 20850, United States.
Andrew McIverCenter for Integrative Chemical Biology and Drug Discovery, Division of Chemical Biology and Medicinal Chemistry, Eshelman School of Pharmacy, University of North Carolina School of Medicine, Chapel Hill, 27599, North Carolina, United States.
Hongchao ZhengCenter for Integrative Chemical Biology and Drug Discovery, Division of Chemical Biology and Medicinal Chemistry, Eshelman School of Pharmacy, University of North Carolina School of Medicine, Chapel Hill, 27599, North Carolina, United States.
Xiaodong WangCenter for Integrative Chemical Biology and Drug Discovery, Division of Chemical Biology and Medicinal Chemistry, Eshelman School of Pharmacy, University of North Carolina School of Medicine, Chapel Hill, 27599, North Carolina, United States.
Xin XuNCATS Chemical Genomics Center, National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland, 20850, United States.
Ajit JadhavNCATS Chemical Genomics Center, National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland, 20850, United States.
Anton SimeonovNCATS Chemical Genomics Center, National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland, 20850, United States.
Min ShenNCATS Chemical Genomics Center, National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland, 20850, United States.
Matthew B BoxerNCATS Chemical Genomics Center, National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland, 20850, United States.
Matthew D HallNCATS Chemical Genomics Center, National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland, 20850, United States. hallma@mail.nih.gov.ORCID 0000-0002-5073-442X
Funding
Pharmacokinetics and Drug MetabolismZIATR000369 · NCATS · NATIONAL CENTER FOR ADVANCING TRANSLATIONAL SCIENCES · PI XU, XIN · 2018 to 2025
$27.3MAdvanced development of human mutant IDH1 inhibitors (Chemical Biology Consortium/NCI Experimental Therapeutics Collaboration)ZIATR000262 · NCATS · NATIONAL CENTER FOR ADVANCING TRANSLATIONAL SCIENCES · PI HALL, MATTHEW · 2016 to 2020
$1.3MAbstract
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 cancer target, a number of small molecule inhibitors have been developed to specifically inhibit mutant forms of IDH (mIDH1 and mIDH2). We present a comprehensive suite of in vitro preclinical drug development assays that can be used as a tool-box to identify lead compounds for mIDH drug discovery programs, as well as what we believe is the most comprehensive publically available dataset on the top mIDH inhibitors. This involved biochemical, cell-based, and tier-one ADME techniques.
Indexed as
Drug DiscoveryCell DifferentiationDrug Evaluation, PreclinicalEnzyme InhibitorsEnzyme StabilityFluorescenceGlutaratesHigh-Throughput Screening AssaysHistonesHumansIsocitrate DehydrogenaseMethylationModels, BiologicalMonocytesMutationSpheroids, Cellularalpha-hydroxyglutarateEnzyme InhibitorsGlutaratesHistonesIsocitrate Dehydrogenase
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.