Search Results - "Artin, Erin"
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AG-221, a First-in-Class Therapy Targeting Acute Myeloid Leukemia Harboring Oncogenic IDH2 Mutations
Published in Cancer discovery (01-05-2017)“…Somatic gain-of-function mutations in isocitrate dehydrogenases ( ) 1 and 2 are found in multiple hematologic and solid tumors, leading to accumulation of the…”
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Discovery of AG-120 (Ivosidenib): A First-in-Class Mutant IDH1 Inhibitor for the Treatment of IDH1 Mutant Cancers
Published in ACS medicinal chemistry letters (12-04-2018)“…Somatic point mutations at a key arginine residue (R132) within the active site of the metabolic enzyme isocitrate dehydrogenase 1 (IDH1) confer a novel gain…”
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Vorasidenib (AG-881): A First-in-Class, Brain-Penetrant Dual Inhibitor of Mutant IDH1 and 2 for Treatment of Glioma
Published in ACS medicinal chemistry letters (13-02-2020)“…Inhibitors of mutant isocitrate dehydrogenase (mIDH) 1 and 2 cancer-associated enzymes prevent the accumulation of the oncometabolite d-2-hydroxyglutarate…”
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Biochemical, Cellular, and Biophysical Characterization of a Potent Inhibitor of Mutant Isocitrate Dehydrogenase IDH1
Published in The Journal of biological chemistry (16-05-2014)“…Two mutant forms (R132H and R132C) of isocitrate dehydrogenase 1 (IDH1) have been associated with a number of cancers including glioblastoma and acute myeloid…”
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Differential Aspartate Usage Identifies a Subset of Cancer Cells Particularly Dependent on OGDH
Published in Cell reports (Cambridge) (11-10-2016)“…Although aberrant metabolism in tumors has been well described, the identification of cancer subsets with particular metabolic vulnerabilities has remained…”
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Targeted Inhibition of Mutant IDH2 in Leukemia Cells Induces Cellular Differentiation
Published in Science (American Association for the Advancement of Science) (03-05-2013)“…A number of human cancers harbor somatic point mutations in the genes encoding isocitrate dehydrogenases 1 and 2 (IDH1 and IDH2). These mutations alter…”
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Abstract 4910: AI predicts drug response from the genomic features of cells and the kinase activity changes induced by compounds
Published in Cancer research (Chicago, Ill.) (22-03-2024)“…Abstract Human protein kinases are playing an important role in various biological activities including tumorigenesis and cancer progression, and for this…”
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Selective Vulnerability to Pyrimidine Starvation in Hematologic Malignancies Revealed by AG-636, a Novel Clinical-Stage Inhibitor of Dihydroorotate Dehydrogenase
Published in Molecular cancer therapeutics (01-12-2020)“…Agents targeting metabolic pathways form the backbone of standard oncology treatments, though a better understanding of differential metabolic dependencies…”
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Insight into the Mechanism of Inactivation of Ribonucleotide Reductase by Gemcitabine 5′-Diphosphate in the Presence or Absence of Reductant
Published in Biochemistry (Easton) (15-12-2009)“…Gemcitabine 5′-diphosphate (F2CDP) is a potent inhibitor of ribonucleotide reductases (RNRs), enzymes that convert nucleotides (NDPs) to deoxynucleotides and…”
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Abstract B126: AG-881, a brain penetrant, potent, pan-mutant IDH (mIDH) inhibitor for use in mIDH solid and hematologic malignancies
Published in Molecular cancer therapeutics (01-01-2018)“…Abstract AG-881 is an orally available, brain penetrant, potent, small-molecule inhibitor of isocitrate dehydrogenase (IDH) 1 and IDH2 mutant proteins…”
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Structural Biology of Mutant IDH2 Inhibition
Published in Acta crystallographica. Section A, Foundations and advances (05-08-2014)“…Abstract only A number of human cancers harbor somatic point mutations in the genes encoding isocitrate dehydrogenases- 1 and -2 (IDH1, IDH2)[1]. These…”
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Structure of the Nucleotide Radical Formed during Reaction of CDP/TTP with the E441Q-α2β2 of E. coli Ribonucleotide Reductase
Published in Journal of the American Chemical Society (14-01-2009)“…The Escherichia coli ribonucleotide reductase (RNR) catalyzes the conversion of nucleoside diphosphates to deoxynucleotides and requires a diferric-tyrosyl…”
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Structure of the Nucleotide Radical Formed during Reaction of CDP/TTP with the E441Q- alpha 2 beta 2 of E. coli Ribonucleotide Reductase
Published in Journal of the American Chemical Society (14-01-2009)“…The Escherichia coli ribonucleotide reductase (RNR) catalyzes the conversion of nucleoside diphosphates to deoxynucleotides and requires a diferric-tyrosyl…”
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A small molecule inhibitor of mutant IDH2 rescues cardiomyopathy in a D-2-hydroxyglutaric aciduria type II mouse model
Published in Journal of inherited metabolic disease (01-11-2016)“…D-2-hydroxyglutaric aciduria (D2HGA) type II is a rare neurometabolic disorder caused by germline gain-of-function mutations in isocitrate dehydrogenase 2 (…”
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Structure of the Nitrogen-Centered Radical Formed during Inactivation of E. coli Ribonucleotide Reductase by 2‘-Azido-2‘-deoxyuridine-5‘-diphosphate: Trapping of the 3‘-Ketonucleotide
Published in Journal of the American Chemical Society (01-06-2005)“…Ribonucleotide reductases (RNRs) catalyze the conversion of nucleotides to deoxynucleotides providing the monomeric precursors required for DNA replication and…”
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Structure of the nucleotide radical formed during reaction of CDP/TTP with the E441Q-alpha2beta2 of E. coli ribonucleotide reductase
Published in Journal of the American Chemical Society (14-01-2009)“…The Escherichia coli ribonucleotide reductase (RNR) catalyzes the conversion of nucleoside diphosphates to deoxynucleotides and requires a diferric-tyrosyl…”
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