Document Detail


Novel phospholipid analogues of pan-PPAR activator tetradecylthioacetic acid are more PPAR alpha selective.
MedLine Citation:
PMID:  20036122     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
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.
Authors:
Yushma Bhurruth-Alcor; Therese H Rost; Michael R Jorgensen; Rajender; Melanie Müller; Jon Skorve; Rolf K Berge; Andrew D Miller
Publication Detail:
Type:  Comparative Study; Journal Article; Research Support, Non-U.S. Gov't     Date:  2009-12-11
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  20     ISSN:  1464-3405     ISO Abbreviation:  Bioorg. Med. Chem. Lett.     Publication Date:  2010 Feb 
Date Detail:
Created Date:  2010-02-03     Completed Date:  2010-09-20     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  England    
Other Details:
Languages:  eng     Pagination:  1252-5     Citation Subset:  IM    
Copyright Information:
Copyright (c) 2009 Elsevier Ltd. All rights reserved.
Affiliation:
Department of Chemistry, Imperial College Genetic Therapies Centre, Imperial College London, London SW7 2AZ, UK.
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MeSH Terms
Descriptor/Qualifier:
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:
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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