Results 21 to 30 of about 34,512 (245)
Haematologica, 2020 Mutant IDH1 (mIDH1) inhibitors have shown single-agent activity in relapsed/refractory AML, though most patients eventually relapse. We evaluated the efficacy and molecular mechanism of the combination treatment with azacitidine, which is currently the standard of care in older AML patients, and mIDH1 inhibitor BAY1436032. Both compounds were evaluated
Anuhar Chaturvedi, +17 more
openaire +6 more sources
Allosteric Mutant IDH1 Inhibitors Reveal Mechanisms for IDH1 Mutant and Isoform Selectivity [PDF]
Structure, 2017 Oncogenic IDH1 and IDH2 mutations contribute to cancer via production of R-2-hydroxyglutarate (2-HG). Here, we characterize two structurally distinct mutant- and isoform-selective IDH1 inhibitors that inhibit 2-HG production. Both bind to an allosteric pocket on IDH1, yet shape it differently, highlighting the plasticity of this site.
Julia Dooley +22 more
openaire +3 more sources
Evaluating Mechanisms of IDH1 Regulation through Site-Specific Acetylation Mimics
Biomolecules, 2021 Isocitrate dehydrogenase (IDH1) catalyzes the reversible NADP+-dependent oxidation of isocitrate to α-ketoglutarate (αKG). IDH1 mutations, primarily R132H, drive > 80% of low-grade gliomas and secondary glioblastomas and facilitate the NADPH-dependent ...
Joi Weeks +5 more
doaj +1 more source
The Frequency and clinical significance of IDH1 mutations in Chinese acute myeloid leukemia patients. [PDF]
PLoS ONE, 2013 OBJECTIVE: Mutations in the gene encoding isocitrate dehydrogenease 1 (IDH1) occur in various hematopoietic tumors including acute myeloid leukemia (AML), myeloproliferative neoplasms and myelodysplastic syndromes.
Lixun Guan +6 more
doaj +1 more source
IDH1 and IDH2: Not Your Typical Oncogenes [PDF]
Cancer Cell, 2010 Oncogenes usually increase their normal function when activated. However, seemingly oncogenic mutations in IDH1 and IDH2 reduce their native enzyme activity. In this issue of Cancer Cell, Ward et al. pin down a neomorphic enzyme activity as a possible oncogenic function for these alterations.
D. Williams Parsons +2 more
openaire +3 more sources
IDH1, Histone Methylation, and So Forth [PDF]
Cancer Cell, 2016 IDH mutants cause aberrant DNA and histone methylation and contribute to hematological and neuronal malignancies. In this issue of Cancer Cell, Inoue et al. describe a potential specific effect of IDH1 mutations that reduces Atm expression via inhibition of H3K9 demethylases, which may represent a first step toward cellular transformation.
Virginie Penard-Lacronique +1 more
openaire +5 more sources
Mutation analysis of IDH1 in paired gliomas revealed IDH1 mutation was not associated with malignant progression but predicted longer survival. [PDF]
PLoS ONE, 2013 Recurrence and progression to higher grade lesions are characteristic behaviors of gliomas. Though IDH1 mutation frequently occurs and is considered as an early event in gliomagenesis, little is known about its role in the recurrence and progression of ...
Yu Yao +10 more
doaj +1 more source
IDH1 mutations in a Brazilian series of Glioblastoma [PDF]
Clinics, 2011 GBM may manifest rapidly de novo(primary GBM), or may develop slowly from grade II orgrade III astrocytomas (secondary GBM), suggesting thatthey are distinct disease entities that evolve throughdifferent genetic pathways.In recent genome-wide analyses, high rates of sponta-neous mutations in the gene encoding cytosolic NADP-dependent isocitrate ...
Uno, Miyuki +15 more
openaire +5 more sources
npj Precision Oncology, 2022 The mutant IDH1 inhibitor ivosidenib improves outcomes for patients with IDH1-mutated cholangiocarcinoma, but resistance inevitably develops. Mechanisms of resistance and strategies to overcome resistance are poorly understood.
James M. Cleary +11 more
doaj +1 more source
Recent advances of IDH1 mutant inhibitor in cancer therapy
Frontiers in Pharmacology, 2022 Isocitrate dehydrogenase (IDH) is the key metabolic enzyme that catalyzes the conversion of isocitrate to α-ketoglutarate (α-KG). Two main types of IDH1 and IDH2 are present in humans.
Wangqi Tian +7 more
doaj +1 more source