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Text
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URL Address
<a href="http://doi.org/10.1016/j.bmcl.2018.03.061" target="_blank" rel="noreferrer noopener">http://doi.org/10.1016/j.bmcl.2018.03.061</a>
Pages
1937–1942
Issue
10
Volume
28
Dublin Core
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Title
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Novel compounds that target lipoprotein lipase and mediate growth arrest in acute lymphoblastic leukemia.
Publisher
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Bioorganic & medicinal chemistry letters
Date
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2018
2018-06
Subject
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*Acute lymphoblastic leukemia; *Cancer; *Co-culture model; *Lipids; *Lipoprotein lipase; *Metabolism; Amides/chemistry/metabolism/pharmacology; Antineoplastic Agents/*chemistry/metabolism/pharmacology; Binding Sites; Cell Line; Cell Proliferation/drug effects; Coculture Techniques; Dyslipidemias/complications/metabolism/pathology; Humans; Lipoprotein Lipase/antagonists & inhibitors/*metabolism; Mesenchymal Stem Cells/cytology/metabolism; Molecular Docking Simulation; Precursor Cell Lymphoblastic Leukemia-Lymphoma/complications/metabolism/pathology; Protein Binding; Protein Structure; Serum Albumin/chemistry/metabolism; Tertiary; Tumor
Creator
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Nair Rajesh R; Geldenhuys Werner J; Piktel Debbie; Sadana Prabodh; Gibson Laura F
Description
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Over the past decade, the therapeutic strategies employed to treat B-precursor acute lymphoblastic leukemia (ALL) have been progressively successful in treating the disease. Unfortunately, the treatment associated dyslipidemia, either acute or chronic, is very prevalent and a cause for decreased quality of life in the surviving patients. To overcome this hurdle, we tested a series of cylopropanecarboxamides, a family demonstrated to target lipid metabolism, for their anti-leukemic activity in ALL. Several of the compounds tested showed anti-proliferative activity, with one, compound 22, inhibiting both Philadelphia chromosome negative REH and Philadelphia chromosome positive SupB15 ALL cell division. The novel advantage of these compounds is the potential synergy with standard chemotherapeutic agents, while concomitantly blunting the emergence of dyslipidemia. Thus, the cylopropanecarboxamides represent a novel class of compounds that can be potentially used in combination with the present standard-of-care to limit treatment associated dyslipidemia in ALL patients.
Identifier
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<a href="http://doi.org/10.1016/j.bmcl.2018.03.061" target="_blank" rel="noreferrer noopener">10.1016/j.bmcl.2018.03.061</a>
Rights
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Article information provided for research and reference use only. All rights are retained by the journal listed under publisher and/or the creator(s).
*Acute lymphoblastic leukemia
*Cancer
*Co-culture model
*Lipids
*Lipoprotein lipase
*Metabolism
2018
Amides/chemistry/metabolism/pharmacology
Antineoplastic Agents/*chemistry/metabolism/pharmacology
Binding Sites
Bioorganic & medicinal chemistry letters
Cell Line
Cell Proliferation/drug effects
Coculture Techniques
Department of Pharmaceutical Sciences
Department of Pharmacy Practice
Dyslipidemias/complications/metabolism/pathology
Geldenhuys Werner J
Gibson Laura F
Humans
Lipoprotein Lipase/antagonists & inhibitors/*metabolism
Mesenchymal Stem Cells/cytology/metabolism
Molecular Docking Simulation
Nair Rajesh R
NEOMED College of Graduate Studies
NEOMED College of Pharmacy
Piktel Debbie
Precursor Cell Lymphoblastic Leukemia-Lymphoma/complications/metabolism/pathology
Protein Binding
Protein Structure
Sadana Prabodh
Serum Albumin/chemistry/metabolism
Tertiary
Tumor