| Novel phospholipid analogues of pan-PPAR activator tetradecylthioacetic acid are more PPAR alpha selective. | |
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MedLine Citation:
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PMID: 20036122 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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Tetradecylthioacetic acid (TTA) is a modified fatty acid that appears to improve insulin sensitivity, lower blood lipid levels, enhance fatty acid oxidation and promote anti-inflammatory action in vivo, through mechanisms partly dependent upon peroxisome proliferator-activated receptors (PPARs). In order to improve the biological efficacy of TTA as a PPAR agonist, two novel phospholipid analogue lyso tetradecylthioacetyl-L-alpha-phosphatidylcholine and di-tetradecylthioacetyl-L-alpha-phosphatidylglycerol have been developed. Here we report on the syntheses of these novel phospholipids and their relative potential to act as PPAR agonists in vitro, in comparison to TTA and other positive controls. |
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Authors:
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Yushma Bhurruth-Alcor; Therese H Rost; Michael R Jorgensen; Rajender; Melanie Müller; Jon Skorve; Rolf K Berge; Andrew D Miller |
Publication Detail:
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Type: Comparative Study; Journal Article; Research Support, Non-U.S. Gov't Date: 2009-12-11 |
Journal Detail:
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Title: Bioorganic & medicinal chemistry letters Volume: 20 ISSN: 1464-3405 ISO Abbreviation: Bioorg. Med. Chem. Lett. Publication Date: 2010 Feb |
Date Detail:
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Created Date: 2010-02-03 Completed Date: 2010-09-20 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 9107377 Medline TA: Bioorg Med Chem Lett Country: England |
Other Details:
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Languages: eng Pagination: 1252-5 Citation Subset: IM |
Copyright Information:
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Copyright (c) 2009 Elsevier Ltd. All rights reserved. |
Affiliation:
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Department of Chemistry, Imperial College Genetic Therapies Centre, Imperial College London, London SW7 2AZ, UK. |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Animals Cell Line Humans PPAR alpha / metabolism* Peroxisome Proliferator-Activated Receptors / agonists*, metabolism Phospholipids / chemical synthesis*, metabolism, pharmacology* Rats Rats, Wistar Sulfides / chemistry*, pharmacology* |
| Chemical | |
Reg. No./Substance:
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0/PPAR alpha; 0/Peroxisome Proliferator-Activated Receptors; 0/Phospholipids; 0/Sulfides; 2921-20-2/1-(carboxymethylthio)tetradecane |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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