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Text
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<a href="http://doi.org/10.1016/j.bmcl.2016.11.053" target="_blank" rel="noreferrer noopener">http://doi.org/10.1016/j.bmcl.2016.11.053</a>
Pages
303–308
Issue
2
Volume
27
Dublin Core
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Title
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Structure-activity and in vivo evaluation of a novel lipoprotein lipase (LPL) activator.
Publisher
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Bioorganic & medicinal chemistry letters
Date
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2017
2017-01
Subject
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*Diabetes; *High-fat diet; *Homology modeling; *Hyperlipidemia; *Lipoprotein lipase; *Liver cirrhosis; *Obesity; Animals; Benzeneacetamides/chemical synthesis/chemistry/*pharmacology; Dose-Response Relationship; Drug; Imidazoles/chemical synthesis/chemistry/*pharmacology; Lipoprotein Lipase/*metabolism; Mice; Molecular Docking Simulation; Molecular Structure; Structure-Activity Relationship
Creator
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Geldenhuys Werner J; Caporoso Joel; Leeper Thomas C; Lee Yoon-Kwang; Lin Li; Darvesh Altaf S; Sadana Prabodh
Description
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Elevated triglycerides (TG) contribute towards increased risk for cardiovascular disease. Lipoprotein lipase (LPL) is an enzyme that is responsible for the metabolism of core triglycerides of very-low density lipoproteins (VLDL) and chylomicrons in the vasculature. In this study, we explored the structure-activity relationships of our lead compound (C10d) that we have previously identified as an LPL agonist. We found that the cyclopropyl moiety of C10d is not absolutely necessary for LPL activity. Several substitutions were found to result in loss of LPL activity. The compound C10d was also tested in vivo for its lipid lowering activity. Mice were fed a high-fat diet (HFD) for four months, and treated for one week at 10mg/kg. At this dose, C10d exhibited in vivo biological activity as indicated by lower TG and cholesterol levels as well as reduced body fat content as determined by ECHO-MRI. Furthermore, C10d also reduced the HFD induced fat accumulation in the liver. Our study has provided insights into the structural and functional characteristics of this novel LPL activator.
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<a href="http://doi.org/10.1016/j.bmcl.2016.11.053" target="_blank" rel="noreferrer noopener">10.1016/j.bmcl.2016.11.053</a>
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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).
*Diabetes
*High-fat diet
*Homology modeling
*Hyperlipidemia
*Lipoprotein lipase
*Liver cirrhosis
*Obesity
2017
Animals
Benzeneacetamides/chemical synthesis/chemistry/*pharmacology
Bioorganic & medicinal chemistry letters
Caporoso Joel
Darvesh Altaf S
Department of Integrative Medical Sciences
Department of Pharmaceutical Sciences
Department of Pharmacy Practice
Dose-Response Relationship
Drug
Geldenhuys Werner J
Imidazoles/chemical synthesis/chemistry/*pharmacology
Lee Yoon-Kwang
Leeper Thomas C
Lin Li
Lipoprotein Lipase/*metabolism
Mice
Molecular Docking Simulation
Molecular Structure
NEOMED College of Graduate Studies
NEOMED College of Medicine
NEOMED College of Pharmacy
Sadana Prabodh
Structure-Activity Relationship