Isocitrate dehydrogenase 1 sustains a hybrid cytoplasmic-mitochondrial tricarboxylic acid cycle that can be targeted for therapeutic purposes in prostate cancer.
Sign Up to like & getrecommendations! Published in 2023 at "Molecular oncology"
DOI: 10.1002/1878-0261.13441
Abstract: The androgen receptor (AR) is an established orchestrator of cell metabolism in prostate cancer (PCa), notably by inducing an oxidative mitochondrial program. Intriguingly, AR regulates cytoplasmic isocitrate dehydrogenase 1 (IDH1) but not its mitochondrial counterparts… read more here.
Keywords: cycle; prostate cancer; idh1; isocitrate dehydrogenase ... See more keywords
3129 – ROLE OF MICROGLIA IN TP53/IDH1 MUTANT GLIOMAS DEVELOPMENT.
Sign Up to like & getrecommendations! Published in 2020 at "Experimental Hematology"
DOI: 10.1016/j.exphem.2020.09.138
Abstract: The origin of glial macrophages and their role in pathology is debated (Gutmann and Kettenmann 2019). In gliomas, paired TP53/IDH1 mutations are associated with lower immune infiltration and better outcomes (Cancer Genome Atlas Research Network… read more here.
Keywords: role; pathology; tp53 idh1; gliomas ... See more keywords
Reliability of noncontrast-enhancing tumor as a biomarker of IDH1 mutation status in glioblastoma
Sign Up to like & getrecommendations! Published in 2017 at "Journal of Clinical Neuroscience"
DOI: 10.1016/j.jocn.2017.01.007
Abstract: Isocitrate dehydrogenase 1 (IDH1) mutations in gliomas have been associated with a frontal lobe location and a greater proportion of noncontrast-enhancing tumour (nCET). The purpose of our study was to validate the utility of MRI… read more here.
Keywords: idh1 wildtype; glioblastoma; frontal lobe; idh1 ... See more keywords
Differentiating Inhibition Selectivity and Binding Affinity of Isocitrate Dehydrogenase 1 Variant Inhibitors
Sign Up to like & getrecommendations! Published in 2023 at "Journal of Medicinal Chemistry"
DOI: 10.1021/acs.jmedchem.3c00203
Abstract: Isocitrate dehydrogenase (IDH) 1/2 gain-of-function variants catalyze the production of the oncometabolite 2-hydroxyglutarate and are validated targets for leukemia treatment. We report binding and inhibition studies on 13 IDH1/2 variant inhibitors, including clinical candidates and… read more here.
Keywords: inhibition selectivity; binding affinity; inhibition; idh1 ... See more keywords
Novel Modes of Inhibition of Wild-Type Isocitrate Dehydrogenase 1 (IDH1): Direct Covalent Modification of His315.
Sign Up to like & getrecommendations! Published in 2018 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.8b00305
Abstract: IDH1 plays a critical role in a number of metabolic processes and serves as a key source of cytosolic NADPH under conditions of cellular stress. However, few inhibitors of wild-type IDH1 have been reported. Here… read more here.
Keywords: inhibition wild; covalent; idh1; novel modes ... See more keywords
Structure-based design and identification of FT-2102 (olutasidenib), a potent mutant-selective IDH1 inhibitor.
Sign Up to like & getrecommendations! Published in 2020 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.9b01423
Abstract: Inhibition of mutant IDH1 is being evaluated clinically as a treatment option for oncology. Here we describe structure-based design and optimization of quinoline lead compounds to identify FT-2102, a potent, orally bioavailable, brain pene-trant and… read more here.
Keywords: structure based; idh1; potent; based design ... See more keywords
Pan-mutant-IDH1 inhibitor BAY1436032 is highly effective against human IDH1 mutant acute myeloid leukemia in vivo
Sign Up to like & getrecommendations! Published in 2017 at "Leukemia"
DOI: 10.1038/leu.2017.46
Abstract: Neomorphic mutations in isocitrate dehydrogenase 1 (IDH1) are frequently found in several human cancer types including acute myeloid leukemia (AML) and lead to the production of high levels of the oncometabolite (R)-2-hydroxyglutarate (R-2HG). Here we… read more here.
Keywords: idh1; myeloid; bay1436032; leukemia ... See more keywords
IDH1/2 mutations in acute myeloid leukemia patients and risk of coronary artery disease and cardiac dysfunction—a retrospective propensity score analysis
Sign Up to like & getrecommendations! Published in 2020 at "Leukemia"
DOI: 10.1038/s41375-020-01043-x
Abstract: Clonal hematopoiesis of indeterminate potential (CHIP) is linked to leukemia gene mutations and associates with an increased risk for coronary artery disease and poor prognosis in ischemic cardiomyopathy. Two recurrently mutated genes in CHIP and… read more here.
Keywords: coronary artery; disease; idh1; leukemia ... See more keywords
PRMT1 driven PTX3 regulates ferritinophagy in glioma.
Sign Up to like & getrecommendations! Published in 2023 at "Autophagy"
DOI: 10.1080/15548627.2023.2165757
Abstract: Mutations in the Krebs cycle enzyme IDH1 (isocitrate dehydrogenase (NADP(+)) 1) are associated with better prognosis in gliomas. Though IDH1 mutant (IDH1R132H) tumors are characterized by their antiproliferative signatures maintained through hypermethylation of DNA and… read more here.
Keywords: idh1 mutant; idh1; ptx3; prmt1 ... See more keywords
IDH1 fine-tunes cap-dependent translation initiation
Sign Up to like & getrecommendations! Published in 2019 at "Journal of Molecular Cell Biology"
DOI: 10.1093/jmcb/mjz082
Abstract: Abstract The metabolic enzyme isocitrate dehydrogenase 1 (IDH1) catalyzes the oxidative decarboxylation of isocitrate to α-ketoglutarate (α-KG). Its mutation often leads to aberrant gene expression in cancer. IDH1 was reported to bind thousands of RNA… read more here.
Keywords: dependent translation; translation initiation; idh1 fine; idh1 ... See more keywords
Targeting IDH1-Mutated Malignancies with NRF2 Blockade.
Sign Up to like & getrecommendations! Published in 2019 at "Journal of the National Cancer Institute"
DOI: 10.1093/jnci/djy230
Abstract: Background Neomorphic IDH1 mutations disrupt the redox balance by promoting reactive oxygen species (ROS) production. However, the mechanism by which IDH1-mutant cells maintain ROS homeostasis remains elusive. It is also not known whether reprogrammed ROS… read more here.
Keywords: nrf2 blockade; mutated cells; idh1 mutated; idh1 ... See more keywords