| Fenofibrate but not fenofibric acid inhibits 11beta-hydroxysteroid dehydrogenase 1 in C2C12 myotubes. | |
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MedLine Citation:
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PMID: 20614230 Owner: NLM Status: In-Process |
Abstract/OtherAbstract:
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Fibrates and WY-14643 are widely used as lipid-lowering drugs via modulation of peroxisome proliferator-activated receptor alpha (PPAR α) for the treatment of a wide range of metabolic disorders. Here, to address the question whether PPAR α agonists can affect the enzymatic activity of 11beta-hydroxysteroid dehydrogenase1 (11β-HSD1), we tested fibrates and WY-14643 for the inhibition of cellular 11β-HSD1 activity in C2C12 myotubes. Only fenofibrate but not fenofibric acid, an active agonist of PPAR α, exerted a potent inhibitory activity in the cell based assay, showing an IC(50) of 1.6 μM. Furthermore, we also demonstrated that the masking of carboxyl group in fenofibric acid via esterification or amidation was required for the inhibitory potencies of fenofibric acid derivatives against 11β-HSD1. In this presentation, we propose that fenofibrate can display a pharmacodynamic role distinct from fenofibric acid through masking of carboxyl group in fenofibric acid. |
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Authors:
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Chi Hyun Kim; Ravirala Ramu; Jin Hee Ahn; Myung Ae Bae; Young Sik Cho |
Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't Date: 2010-07-08 |
Journal Detail:
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Title: Molecular and cellular biochemistry Volume: 344 ISSN: 1573-4919 ISO Abbreviation: Mol. Cell. Biochem. Publication Date: 2010 Nov |
Date Detail:
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Created Date: 2010-10-12 Completed Date: - Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 0364456 Medline TA: Mol Cell Biochem Country: Netherlands |
Other Details:
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Languages: eng Pagination: 91-8 Citation Subset: IM |
Affiliation:
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Pharmacology Research Center, Bio-Organic Science Division, Korea Research Institute of Chemical Technology, Yuseong-gu, Daejeon, South Korea. |
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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