Search Results - "Narayanaswamy, Rohini"
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Structure and inhibition mechanism of the catalytic domain of human squalene epoxidase
Published in Nature communications (09-01-2019)“…Squalene epoxidase (SQLE), also known as squalene monooxygenase, catalyzes the stereospecific conversion of squalene to 2,3( S )-oxidosqualene, a key step in…”
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A chemical biology screen identifies a vulnerability of neuroendocrine cancer cells to SQLE inhibition
Published in Nature communications (09-01-2019)“…Aberrant metabolism of cancer cells is well appreciated, but the identification of cancer subsets with specific metabolic vulnerabilities remains challenging…”
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Quantitation of uridine and L-dihydroorotic acid in human plasma by LC–MS/MS using a surrogate matrix approach
Published in Journal of pharmaceutical and biomedical analysis (05-01-2021)“…•A validated LC–MS/MS assay for the quantitation of endogenous analytes, Uridine and L-Dihydroorotic Acid, in human plasma.•A surrogate matrix approach with…”
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Enasidenib-induced differentiation promotes sensitivity to venetoclax in IDH2-mutated acute myeloid leukemia
Published in Leukemia (01-03-2022)Get full text
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Simultaneous determination of oxysterols, cholesterol and 25-hydroxy-vitamin D3 in human plasma by LC-UV-MS
Published in PloS one (13-04-2015)“…Oxysterols are promising biomarkers of neurodegenerative diseases that are linked with cholesterol and vitamin D metabolism. There is an unmet need for methods…”
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Idh1 mutations contribute to the development of T-cell malignancies in genetically engineered mice
Published in Proceedings of the National Academy of Sciences - PNAS (02-02-2016)“…Gain-of-function mutations in isocitrate dehydrogenase 1 (IDH1) are key drivers of hematopoietic malignancies. Although these mutations are most commonly…”
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Abstract 1339: Investigations into rational combination approaches with ivosidenib in a mutant IDH1 acute myeloid leukemia patient-derived xenograft model
Published in Cancer research (Chicago, Ill.) (01-07-2021)“…Abstract Background: Somatic mutations in isocitrate dehydrogenase 1 (IDH1) arise in roughly 6-10% of patients with acute myeloid leukemia (AML). These…”
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The pyruvate kinase activator mitapivat reduces hemolysis and improves anemia in a β-thalassemia mouse model
Published in The Journal of clinical investigation (17-05-2021)“…Anemia in β-thalassemia is related to ineffective erythropoiesis and reduced red cell survival. Excess free heme and accumulation of unpaired α-globin chains…”
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Quantitation of ivosidenib in human plasma via LC–MS/MS and its application in clinical trials
Published in Bioanalysis (01-06-2021)“…Ivosidenib is a potent and selective small molecule inhibitor of mutant isocitrate dehydrogenase 1. Accurate measurement of ivosidenib is the key to ivosidenib…”
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The IDH2 R172K mutation associated with angioimmunoblastic T-cell lymphoma produces 2HG in T cells and impacts lymphoid development
Published in Proceedings of the National Academy of Sciences - PNAS (27-12-2016)“…Oncogenic isocitrate dehydrogenase (IDH)1 and IDH2 mutations at three hotspot arginine residues cause an enzymatic gain of function that leads to the…”
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Abstract 3607: Inhibition of mutant IDH enzymes reduces production of 2-HG but does not restore wild type IDH activity in vitro or in vivo
Published in Cancer research (Chicago, Ill.) (01-07-2019)“…Abstract Mutations in isocitrate dehydrogenase (IDH) 1 and 2 occur in variety of malignancies, and notably >70% of low grade gliomas. These mutations lead to…”
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EXTH-15. INHIBITION OF 2-HG LEADS TO UPREGULATION OF A PRO-INFLAMMATORY GENE SIGNATURE IN A NOVEL HLA-A2/HLA-DR1 TRANSGENIC MOUSE MODEL OF IDH1R132H-EXPRESSING GLIOMA
Published in Neuro-oncology (Charlottesville, Va.) (09-11-2020)“…Abstract Recent studies have demonstrated the impacts of 2-HG on the anti-tumor immune response in isocitrate dehydrogenase (IDH)-mutant gliomas. Our…”
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Identification of Environmental Quaternary Ammonium Compounds as Direct Inhibitors of Cholesterol Biosynthesis
Published in Toxicological sciences (01-06-2016)“…In this study, we aim to identify environmental molecules that can inhibit cholesterol biosynthesis, potentially leading to the same biochemical defects as…”
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2031 - DELINEATING MECHANISMS OF ACQUIRED RESISTANCE TO IDH INHIBITORS IN AML
Published in Experimental hematology (01-08-2019)“…Approximately 20% of acute myeloid leukaemia (AML) patients carry mutations in genes that encode the metabolic enzymes isocitrate dehydrogenase (IDH) 1 and -2…”
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Preclinical toxicology profile of squalene epoxidase inhibitors
Published in Toxicology and applied pharmacology (15-08-2020)“…Small cell lung cancer (SCLC) is a particularly aggressive subset of lung cancer, and identification of new therapeutic options is of significant interest. We…”
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Abstract 3510: IDH1-R132H tumor cells are not robustly sensitive to PARP inhibition in a 2-HG dependent manner
Published in Cancer research (Chicago, Ill.) (01-07-2019)“…Abstract Mutations in the metabolic enzymes isocitrate dehydrogenase (IDH) 1 or 2 arise in a variety of malignancies and lead to the production of the…”
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Abstract 1810: The mutant IDH1 inhibitor ivosidenib promotes tumor cell differentiation and anti-tumor immunity in intrahepatic cholangiocarcinoma
Published in Cancer research (Chicago, Ill.) (15-08-2020)“…Abstract Intrahepatic cholangiocarcinoma (ICC) is a cancer of the liver bile ducts, which has been rising in incidence and carries a 5-year survival rate of…”
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Quantitation of 2-hydroxyglutarate in human plasma via LC–MS/MS using a surrogate analyte approach
Published in Bioanalysis (01-08-2020)“…2-Hydroxyglutarate (2-HG) is a target engagement biomarker in patients after treatment with inhibitors of mutated isocitrate dehydrogenase (mIDH). Accurate…”
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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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Combination of Enasidenib and Venetoclax Shows Superior Anti-Leukemic Activity Against IDH2 Mutated AML in Patient-Derived Xenograft Models
Published in Blood (29-11-2018)“…Mutations in isocitrate dehydrogenase 2 (IDH2) promote AML pathogenesis through production of 2-hydroxyglutarate (2-HG). Enasidenib is an inhibitor of mutant…”
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