Discovery and Optimization of Quinolinone Derivatives as Potent, Selective and Orally Bioavailable mutant Isocitrate Dehydrogenase 1 (mIDH1) Inhibitors.
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DOI: 10.1021/acs.jmedchem.9b00362
Abstract: Mutations at the arginine residue (R132) in isocitrate dehydrogenase 1 (IDH1) are frequently identified in various human cancers. Inhibition of mutant IDH1 (mIDH1) with small molecules has been clinically validated as a promising therapeutic treatment… read more here.
Keywords: orally bioavailable; midh1; isocitrate dehydrogenase; discovery optimization ... See more keywords
Tight Regulation of H3K79 Methylation Levels in KMT2A-Rearranged AML
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DOI: 10.1182/blood-2018-99-114784
Abstract: Rationale: KMT2A-rearrangements (KMT2A-r) in acute myeloid leukemia (AML), encompassing both KMT2a-fusions (KMT2A-F) and KMT2A-partial tandem duplications (KMT2A-PTD), represent a subgroup of AML with a particularly poor prognosis. Both KMT2A-F and KMT2A-PTD share a dependency on… read more here.
Keywords: methylation; midh1; h3k79 methylation; kmt2a ... See more keywords
Frequency and prognostic significance of isocitrate dehydrogenase 1 mutations in cholangiocarcinoma: a systematic literature review.
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DOI: 10.21037/jgo.2019.03.10
Abstract: Background The recognition of distinct molecular subgroups within cholangiocarcinoma (CC), along with the increasing availability of targeted therapies, suggests that further characterization of the prevalence and prognosis of frequently occurring subgroups may assist with the… read more here.
Keywords: review; frequency; oncology; prognostic significance ... See more keywords
Molecular and morphological changes induced by ivosidenib correlate with efficacy in mutant-IDH1 cholangiocarcinoma.
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DOI: 10.2217/fon-2020-1274
Abstract: Background: IDH1 mutations occur in approximately 13% of intrahepatic cholangiocarcinomas (IHCCs). The oral, targeted, mutant IDH1 (mIDH1) inhibitor ivosidenib (AG-120) suppresses production of the oncometabolite D-2-hydroxyglutarate, promoting disease stabilization and improved progression-free survival (PFS) in mIDH1 IHCC. Materials… read more here.
Keywords: mutant idh1; midh1; morphological changes; efficacy ... See more keywords