Search Results - "Heaton, William L"
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shRNA library screening identifies nucleocytoplasmic transport as a mediator of BCR-ABL1 kinase-independent resistance
Published in Blood (12-03-2015)“…The mechanisms underlying tyrosine kinase inhibitor (TKI) resistance in chronic myeloid leukemia (CML) patients lacking explanatory BCR-ABL1 kinase domain…”
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Disarming an Electrophilic Warhead: Retaining Potency in Tyrosine Kinase Inhibitor (TKI)-Resistant CML Lines While Circumventing Pharmacokinetic Liabilities
Published in ChemMedChem (19-04-2016)“…Pharmacologic blockade of the activation of signal transducer and activator of transcription 3 (STAT3) in tyrosine kinase inhibitor (TKI)‐resistant chronic…”
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3
BCR-ABL1 Compound Mutations Combining Key Kinase Domain Positions Confer Clinical Resistance to Ponatinib in Ph Chromosome-Positive Leukemia
Published in Cancer cell (2014)“…Ponatinib is the only currently approved tyrosine kinase inhibitor (TKI) that suppresses all BCR-ABL1 single mutants in Philadelphia chromosome-positive (Ph+)…”
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4
Autocrine Tnf signaling favors malignant cells in myelofibrosis in a Tnfr2-dependent fashion
Published in Leukemia (01-11-2018)“…Tumor necrosis factor alpha (TNF) is increased in myelofibrosis (MF) and promotes survival of malignant over normal cells. The mechanisms altering TNF…”
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SIRT5 IS A DRUGGABLE METABOLIC VULNERABILITY IN ACUTE MYELOID LEUKEMIA
Published in Blood cancer discovery (01-05-2021)“…We discovered that the survival and growth of many primary acute myeloid leukemia (AML) samples and cell lines, but not normal CD34+ cells, are dependent on…”
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Identification and Characterization of AES-135, a Hydroxamic Acid-Based HDAC Inhibitor That Prolongs Survival in an Orthotopic Mouse Model of Pancreatic Cancer
Published in Journal of medicinal chemistry (14-03-2019)“…Pancreatic ductal adenocarcinoma (PDAC) is an aggressive, incurable cancer with a 20% 1 year survival rate. While standard-of-care therapy can prolong life in…”
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Nuclear-Cytoplasmic Transport Is a Therapeutic Target in Myelofibrosis
Published in Clinical cancer research (01-04-2019)“…Myelofibrosis is a hematopoietic stem cell neoplasm characterized by bone marrow reticulin fibrosis, extramedullary hematopoiesis, and frequent transformation…”
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Coordinated inhibition of nuclear export and Bcr-Abl1 selectively targets chronic myeloid leukemia stem cells
Published in Leukemia (01-06-2020)Get full text
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9
Femoral Heads from Total Hip Arthroplasty as a Source of Adult Hematopoietic Cells
Published in Acta haematologica (01-01-2021)“…Normal human bone marrow cells are critical for studies of hematopoiesis and as controls to assess toxicity. As cells from commercial vendors are expensive,…”
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Discovery and characterization of AZD9272 and AZD6538—Two novel mGluR5 negative allosteric modulators selected for clinical development
Published in Bioorganic & medicinal chemistry letters (15-11-2012)“…AZD9272 and AZD6538 are two novel mGluR5 negative allosteric modulators selected for further clinical development. An initial high-throughput screening…”
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Inside Cover: Disarming an Electrophilic Warhead: Retaining Potency in Tyrosine Kinase Inhibitor (TKI)-Resistant CML Lines While Circumventing Pharmacokinetic Liabilities (ChemMedChem 8/2016)
Published in ChemMedChem (19-04-2016)“…The inside cover picture shows the small molecule AM‐1‐124, an inhibitor of imatinib‐resistant chronic myeloid leukemia (CML) cells. Pharmacologic blockade of…”
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3H-Quinazolin-4-ones as a new calcilytic template for the potential treatment of osteoporosis
Published in Bioorganic & medicinal chemistry letters (15-03-2005)“…Structure-activity relationship studies, focused on identification of the active pharmacophore fragments in a single high-throughput screening calcilytic hit,…”
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13
Design, new synthesis, and calcilytic activity of substituted 3H-pyrimidin-4-ones
Published in Bioorganic & medicinal chemistry letters (16-05-2005)“…Design, new synthesis, structure–activity relationship studies and calcium receptor antagonist (calcilytic) properties of novel 3H-pyrimidin-4-ones are…”
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Combined STAT3 and BCR-ABL1 inhibition induces synthetic lethality in therapy-resistant chronic myeloid leukemia
Published in Leukemia (01-03-2015)“…Mutations in the BCR-ABL1 kinase domain are an established mechanism of tyrosine kinase inhibitor (TKI) resistance in Philadelphia chromosome-positive…”
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Abstract LB109: A critical role for SIRT5 in acute myeloid leukemia metabolism
Published in Cancer research (Chicago, Ill.) (01-07-2021)“…Standard of care for AML includes chemotherapy and stem cell transplant, with 5-year survival rates <30%. We sought to identify genes critical to AML cells,…”
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Stroma-Based Activation of pSTAT3Y705 Confers Resistance to FLT3 Inhibitors in FLT3 ITD-Positive AML
Published in Blood (02-12-2016)“…Acute myeloid leukemia (AML) is an aggressive hematopoietic neoplasm that carries the worst prognosis among the hematologic malignancies. Up to 30% of AML…”
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TNFR2 Signaling Promotes Myeloproliferative Disease Progression: A Role for MAPK8?
Published in Blood (02-12-2016)“…The majority of patients diagnosed with Philadelphia negative (Ph-) myeloproliferative neoplasms (MPNs) harbor somatic, gain-of-function mutations in JAK2,…”
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SIRT5 As a Therapeutic Target in Acute Myeloid Leukemia
Published in Blood (29-11-2018)“…Acute myeloid leukemia (AML) is an aggressive hematopoietic neoplasm with five-year overall survival rates <30% on standard of care therapy. Relapse is common…”
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Inhibition of Nucleocytoplasmic Export Enhances Selective Elimination of Leukemic Stem Cells in Chronic Myeloid Leukemia
Published in Blood (08-12-2017)“…Chronic myeloid leukemia (CML) is a hematopoietic stem cell malignancy driven by BCR-ABL1 tyrosine kinase and effectively managed with tyrosine kinase…”
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Effect of a TNFα Blocker and Peginfa on Polycythemia Vera Clonal Hematopoiesis and Suppressed Normal Dormant Hematopoiesis
Published in Blood (06-12-2014)“…Polycythemia vera (PV) is a clonal disorder arising from a single stem cell while normal stem cells are present in the marrow but are suppressed by the PV…”
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