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mtKO: A dedicated guide RNA library for mitochondria research. [PDF]
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Radioprotection of IDH1-Mutated Cancer Cells by the IDH1-Mutant Inhibitor AGI-5198
Cancer Research, 2015Abstract Isocitrate dehydrogenase 1 (IDH1) is mutated in various types of human cancer to IDH1R132H, a structural alteration that leads to catalysis of α-ketoglutarate to the oncometabolite D-2-hydroxyglutarate. In this study, we present evidence that small-molecule inhibitors of IDH1R132H that are being developed for cancer therapy may ...
Molenaar, R.J. +19 more
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Structure-based discovery of IHMT-IDH1-053 as a potent irreversible IDH1 mutant selective inhibitor
European Journal of Medicinal Chemistry, 2023Through a structure-based irreversible drug design approach, we have discovered a highly potent IDH1-mutant inhibitor compound 16 (IHMT-IDH1-053) (IC50 = 4.7 nM), which displays high selectivity against IDH1 mutants over IDH1 wt and IDH2 wt/mutants.
Qianmao Liang +16 more
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Targeting IDH1/IDH2 mutations in gliomas
Current Opinion in Neurology, 2022Purpose of review Somatic point mutations in the metabolic enzyme isocitrate dehydrogenase (IDH) are a defining feature of the majority of WHO grade 2–3 diffuse glioma and the most powerful positive prognostic factor for survival in gliomas. The purpose is to review experimental therapeutic approaches targeting IDH mutations in
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IDH1/2 mutation detection in gliomas
Brain Tumor Pathology, 2014Somatic mutations of isocitrate dehydrogenase 1 and 2 (IDH1/2) are strongly associated with pathological subtypes, genetic profiles, and clinical features in gliomas. The IDH1/2 status is currently regarded as one of the most important molecular markers in gliomas and should be assessed accurately and robustly.
Hideyuki, Arita +5 more
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Abstract 4620: Wild-type IDH1: A molecular target in IDH1 mutant cancers
Cancer Research, 2014Abstract Neomorphic mutations targeting R132 of the TCA cycle enzyme, IDH1, have been identified in multiple cancer types and lead to a build up of (R)-2-hydroxyglutarate ((R)-2HG). Several mechanisms have been proposed to account for mutant-IDH1-mediated transformation: due to its structure similarity with alpha-ketoglutarate (α-KG), (R)
Julie A. Wickenden +9 more
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Metabolism of glioma and IDH1/IDH2 mutations
Revue Neurologique, 2011Many known oncogenic signaling pathways involved in gliomagenesis have strong consequences on tumor cell metabolism, and promote the switch from oxidative phosphorylation to aerobic glycolysis, for ATP generation. However, the interest on metabolism has been recently renewed by the discovery of recurrent mutation of IDH1 genes by systematic sequencing ...
M, Rossetto +4 more
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