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

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

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

http://www.wikidata.org/entity/Q33630257

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Targeting histone methylation for cancer therapy: enzymes, inhibitors, biological activity and perspectives Volasertib for AML: clinical use and patient consideration New developments in the pathogenesis and therapeutic targeting of the IDH1 mutation in glioma Isocitrate dehydrogenase mutations: new opportunities for translational research Crystallographic Investigation and Selective Inhibition of Mutant Isocitrate Dehydrogenase IDH mutations in tumorigenesis and their potential role as novel therapeutic targets.An inhibitor of mutant IDH1 delays growth and promotes differentiation of glioma cells.Metabolic consequences of oncogenic IDH mutations 2-Hydoxyglutarate: D/Riving Pathology in gLiomaS Detection of oncogenic IDH1 mutations using magnetic resonance spectroscopy of 2-hydroxyglutarate.Biochemical, cellular, and biophysical characterization of a potent inhibitor of mutant isocitrate dehydrogenase IDH1.Inhibition of cancer-associated mutant isocitrate dehydrogenases: synthesis, structure-activity relationship, and selective antitumor activity.Accumulation of 2-hydroxyglutarate in gliomas correlates with survival: a study by 3.0-tesla magnetic resonance spectroscopy.Genetic dissection of leukemia-associated IDH1 and IDH2 mutants and D-2-hydroxyglutarate in Drosophila.Proto-oncogenic role of mutant IDH2 in leukemia initiation and maintenance.Avoiding Fluorescence Assay Interference-The Case for Diaphorase.Diaphorase Coupling Protocols for Red-Shifting Dehydrogenase Assays Radiolabeled inhibitors as probes for imaging mutant IDH1 expression in gliomas: Synthesis and preliminary evaluation of labeled butyl-phenyl sulfonamide analogs.Inhibition of Cancer-Associated Mutant Isocitrate Dehydrogenases by 2-Thiohydantoin Compounds Isocitrate dehydrogenase 1 R132C mutation occurs exclusively in microsatellite stable colorectal cancers with the CpG island methylator phenotype Detection of Dual IDH1 and IDH2 Mutations by Targeted Next-Generation Sequencing in Acute Myeloid Leukemia and Myelodysplastic Syndromes.Cancer as a dysregulated epigenome allowing cellular growth advantage at the expense of the host Extreme Vulnerability of IDH1 Mutant Cancers to NAD+ Depletion.What a difference a hydroxyl makes: mutant IDH, (R)-2-hydroxyglutarate, and cancer.IDH1 mutations alter citric acid cycle metabolism and increase dependence on oxidative mitochondrial metabolism A comparative study of short- and long-TE ¹H MRS at 3 T for in vivo detection of 2-hydroxyglutarate in brain tumors.Frequent mutation of the major cartilage collagen gene COL2A1 in chondrosarcoma.Alterations of 5-hydroxymethylcytosine in human cancers.Non-invasive detection of 2-hydroxyglutarate in IDH-mutated gliomas using two-dimensional localized correlation spectroscopy (2D L-COSY) at 7 Tesla.Intracerebral Distribution of the Oncometabolite d-2-Hydroxyglutarate in Mice Bearing Mutant Isocitrate Dehydrogenase Brain Tumors: Implications for Tumorigenesis.(R)-2-hydroxyglutarate is sufficient to promote leukemogenesis and its effects are reversible Non-invasive in vivo assessment of IDH1 mutational status in glioma.Decreased expression of IDH1-R132H correlates with poor survival in gastrointestinal cancer.Isocitrate dehydrogenase mutations in leukemia.Diagnostic and Therapeutic Biomarkers in Glioblastoma: Current Status and Future Perspectives.HOT mutation screening in human glioblastomas.Functional roles of CSPG4/NG2 in chondrosarcoma.Discovery of 8-Membered Ring Sulfonamides as Inhibitors of Oncogenic Mutant Isocitrate Dehydrogenase 1.Molecular characterisation of cutaneous melanoma: creating a framework for targeted and immune therapies.Inhibition of mutant IDH1 decreases D-2-HG levels without affecting tumorigenic properties of chondrosarcoma cell lines.

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

http://www.wikidata.org/entity/Q33630257

description

2012 nî lūn-bûn

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2012 թուականի Սեպտեմբերին հրատարակուած գիտական յօդուած

@hyw

2012 թվականի սեպտեմբերին հրատարակված գիտական հոդված

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2012年の論文

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2012年論文

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2012年論文

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2012年論文

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2012年論文

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2012年論文

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2012年论文

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name

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

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

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type

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

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

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

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

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ACS Medicinal Chemistry Letters

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

@en

P2093

Derek Shi

http://www.w3.org/2001/XMLSchema#string

Fang Zhao

http://www.w3.org/2001/XMLSchema#string

Francesco G Salituro

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Hua Yang

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Janeta Popovici-Muller

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Jeffrey O Saunders

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Jeremy M Travins

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Kaiko Kunii

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Katharine E Yen

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Kimberly S Straley

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Cancer-associated IDH1 mutations produce 2-hydroxyglutarate

Oncometabolite 2-hydroxyglutarate is a competitive inhibitor of α-ketoglutarate-dependent dioxygenases

An integrated genomic analysis of human glioblastoma multiforme

IDH1 and IDH2 mutations in gliomas

The oncometabolite 2-hydroxyglutarate inhibits histone lysine demethylases

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

IDH1 mutation is sufficient to establish the glioma hypermethylator phenotype

Isocitrate dehydrogenase 1 and 2 mutations in cancer: alterations at a crossroads of cellular metabolism

IDH1 and IDH2 mutations are frequent events in central chondrosarcoma and central and periosteal chondromas but not in other mesenchymal tumours.

IDH1(R132H) mutation increases murine haematopoietic progenitors and alters epigenetics

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850-855

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10.1021/ML300225H

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10

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3

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2012-09-17T00:00:00Z

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24900389

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4025665

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