ArticleThe Journal of pharmacology and experimental therapeutics2019
An Inhibitor of Fatty Acid Synthase Thioesterase Domain with Improved Cytotoxicity against Breast Cancer Cells and Stability in Plasma.
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Article in The Journal of pharmacology and experimental therapeutics, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
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10citing papers in PubMed
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10 citing papers in PubMed, 31 citations in OpenAlex.
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- Integrated multi-omics analyses reveal Jorunnamycin A as a novel suppressor for muscle-invasive bladder cancer by targeting FASN and TOP1.Journal of translational medicine · 2023Article
- Lipid metabolic reprogramming by traditional Chinese medicine and its role in effective cancer therapy.Journal of Cancer · 2023Review
- A Comparison of Dinoflagellate Thiolation Domain Binding Proteins Using In Vitro and Molecular Methods.Marine drugs · 2022Article
- Hepatic circadian and differentiation factors control liver susceptibility for fatty liver disease and tumorigenesis.FASEB journal : official publication of the Federation of American Societies for Experimental Biology · 2022Article
- Power of two: combination of therapeutic approaches involving glucose transporter (GLUT) inhibitors to combat cancer.Biochimica et biophysica acta. Reviews on cancer · 2020Review
- Endocytosis of very low-density lipoproteins: an unexpected mechanism for lipid acquisition by breast cancer cells.Journal of lipid research · 2020Article
- Identification of the fatty acid synthase interaction network via iTRAQ-based proteomics indicates the potential molecular mechanisms of liver cancer metastasis.Cancer cell international · 2020Article
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Authors and funding
10 authors at 1 institution in 1 country.
Leslie E LupienDivision of Endocrinology and Metabolism, Department of Medicine, Norris Cotton Cancer Center (W.B.K.) and Section of Clinical Pharmacology & The Clinical Pharmacology Shared Resource (L.D.L., D.B.P.), The Geisel School of Medicine (L.E.L., W.B.K.), and Program in Experimental and Molecular Medicine, Dartmouth-Hitchcock Medical Center (L.E.L.), Dartmouth College, Lebanon, New Hampshire; and Department of Chemistry, Keene State College, Keene, New Hampshire (E.M.D., M.J.M., I.B.L., M.G.F., M.E.O., P.W.B.).
Evan M DunkleyDivision of Endocrinology and Metabolism, Department of Medicine, Norris Cotton Cancer Center (W.B.K.) and Section of Clinical Pharmacology & The Clinical Pharmacology Shared Resource (L.D.L., D.B.P.), The Geisel School of Medicine (L.E.L., W.B.K.), and Program in Experimental and Molecular Medicine, Dartmouth-Hitchcock Medical Center (L.E.L.), Dartmouth College, Lebanon, New Hampshire; and Department of Chemistry, Keene State College, Keene, New Hampshire (E.M.D., M.J.M., I.B.L., M.G.F., M.E.O., P.W.B.).
Margaret J MaloyDivision of Endocrinology and Metabolism, Department of Medicine, Norris Cotton Cancer Center (W.B.K.) and Section of Clinical Pharmacology & The Clinical Pharmacology Shared Resource (L.D.L., D.B.P.), The Geisel School of Medicine (L.E.L., W.B.K.), and Program in Experimental and Molecular Medicine, Dartmouth-Hitchcock Medical Center (L.E.L.), Dartmouth College, Lebanon, New Hampshire; and Department of Chemistry, Keene State College, Keene, New Hampshire (E.M.D., M.J.M., I.B.L., M.G.F., M.E.O., P.W.B.).
Ian B LehnerDivision of Endocrinology and Metabolism, Department of Medicine, Norris Cotton Cancer Center (W.B.K.) and Section of Clinical Pharmacology & The Clinical Pharmacology Shared Resource (L.D.L., D.B.P.), The Geisel School of Medicine (L.E.L., W.B.K.), and Program in Experimental and Molecular Medicine, Dartmouth-Hitchcock Medical Center (L.E.L.), Dartmouth College, Lebanon, New Hampshire; and Department of Chemistry, Keene State College, Keene, New Hampshire (E.M.D., M.J.M., I.B.L., M.G.F., M.E.O., P.W.B.).
Maxwell G FoiseyDivision of Endocrinology and Metabolism, Department of Medicine, Norris Cotton Cancer Center (W.B.K.) and Section of Clinical Pharmacology & The Clinical Pharmacology Shared Resource (L.D.L., D.B.P.), The Geisel School of Medicine (L.E.L., W.B.K.), and Program in Experimental and Molecular Medicine, Dartmouth-Hitchcock Medical Center (L.E.L.), Dartmouth College, Lebanon, New Hampshire; and Department of Chemistry, Keene State College, Keene, New Hampshire (E.M.D., M.J.M., I.B.L., M.G.F., M.E.O., P.W.B.).
Maddison E OuelletteDivision of Endocrinology and Metabolism, Department of Medicine, Norris Cotton Cancer Center (W.B.K.) and Section of Clinical Pharmacology & The Clinical Pharmacology Shared Resource (L.D.L., D.B.P.), The Geisel School of Medicine (L.E.L., W.B.K.), and Program in Experimental and Molecular Medicine, Dartmouth-Hitchcock Medical Center (L.E.L.), Dartmouth College, Lebanon, New Hampshire; and Department of Chemistry, Keene State College, Keene, New Hampshire (E.M.D., M.J.M., I.B.L., M.G.F., M.E.O., P.W.B.).
Lionel D LewisDivision of Endocrinology and Metabolism, Department of Medicine, Norris Cotton Cancer Center (W.B.K.) and Section of Clinical Pharmacology & The Clinical Pharmacology Shared Resource (L.D.L., D.B.P.), The Geisel School of Medicine (L.E.L., W.B.K.), and Program in Experimental and Molecular Medicine, Dartmouth-Hitchcock Medical Center (L.E.L.), Dartmouth College, Lebanon, New Hampshire; and Department of Chemistry, Keene State College, Keene, New Hampshire (E.M.D., M.J.M., I.B.L., M.G.F., M.E.O., P.W.B.).
Darcy Bates PoolerDivision of Endocrinology and Metabolism, Department of Medicine, Norris Cotton Cancer Center (W.B.K.) and Section of Clinical Pharmacology & The Clinical Pharmacology Shared Resource (L.D.L., D.B.P.), The Geisel School of Medicine (L.E.L., W.B.K.), and Program in Experimental and Molecular Medicine, Dartmouth-Hitchcock Medical Center (L.E.L.), Dartmouth College, Lebanon, New Hampshire; and Department of Chemistry, Keene State College, Keene, New Hampshire (E.M.D., M.J.M., I.B.L., M.G.F., M.E.O., P.W.B.).
William B KinlawDivision of Endocrinology and Metabolism, Department of Medicine, Norris Cotton Cancer Center (W.B.K.) and Section of Clinical Pharmacology & The Clinical Pharmacology Shared Resource (L.D.L., D.B.P.), The Geisel School of Medicine (L.E.L., W.B.K.), and Program in Experimental and Molecular Medicine, Dartmouth-Hitchcock Medical Center (L.E.L.), Dartmouth College, Lebanon, New Hampshire; and Department of Chemistry, Keene State College, Keene, New Hampshire (E.M.D., M.J.M., I.B.L., M.G.F., M.E.O., P.W.B.).
Paul W BauresDivision of Endocrinology and Metabolism, Department of Medicine, Norris Cotton Cancer Center (W.B.K.) and Section of Clinical Pharmacology & The Clinical Pharmacology Shared Resource (L.D.L., D.B.P.), The Geisel School of Medicine (L.E.L., W.B.K.), and Program in Experimental and Molecular Medicine, Dartmouth-Hitchcock Medical Center (L.E.L.), Dartmouth College, Lebanon, New Hampshire; and Department of Chemistry, Keene State College, Keene, New Hampshire (E.M.D., M.J.M., I.B.L., M.G.F., M.E.O., P.W.B.) pbaures@keene.edu.ORCID 0000-0003-3879-8428
Dartmouth College · US
Funding
Translational Engineering in Cancer (TEC)P30CA023108 · NCI · DARTMOUTH COLLEGE · PI Steven D Leach · 1985 to 2026
$91.3MUltrastructural analysis of axonal Kv2-mediated endoplasmic reticulum/plasma membrane (ER/PM) junctionsP20GM103506 · NIGMS · DARTMOUTH COLLEGE · PI STEVEN FIERING · 2012 to 2026
$60.1MRole of Protein S14 in Normal and Neoplastic Mammary GlandR01CA126618 · NCI · DARTMOUTH COLLEGE · PI KINLAW, WILLIAM B · 2007 to 2017
$2.8MRole of Protein (S14)in Normal and Neoplastic MammaryR01DK058961 · NIDDK · DARTMOUTH COLLEGE · PI KINLAW, WILLIAM B · 2002 to 2005
$1.0MNCI NIH HHS P30 CA023108NCI NIH HHS R01 CA126618NIDDK NIH HHS R01 DK058961NIGMS NIH HHS P20 GM103506
Abstract
It is well recognized that many cancers are addicted to a constant supply of fatty acids (FAs) and exhibit brisk de novo FA synthesis. Upregulation of a key lipogenic enzyme, fatty acid synthase (FASN), is a near-universal feature of human cancers and their precursor lesions, and has been associated with chemoresistance, tumor metastasis, and diminished patient survival. FASN inhibition has been shown to be effective in killing cancer cells, but progress in the field has been hindered by off-target effects and poor pharmaceutical properties of candidate compounds. Our initial hit (compound
Indexed as
Catalytic DomainAntineoplastic AgentsCell ProliferationEnzyme InhibitorsEpithelial CellsFatty Acid SynthasesHumansMCF-7 CellsProtein BindingSubstrate SpecificityThiolester HydrolasesAntineoplastic AgentsEnzyme InhibitorsFatty Acid SynthasesThiolester Hydrolases
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.