Document Detail


Topical ER36009, a RARgamma-selective retinoid, decreases abdominal white adipose tissue and elicits changes in expression of genes related to adiposity and thermogenesis.
MedLine Citation:
PMID:  17185799     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Chronic topical treatment of rats with a new RARgamma-selective retinoid, ER36009, resulted in a significant reduction of epididymal white adipose tissue and a significant increase of interscapular brown adipose tissue without affecting food intake. ER36009 markedly decreased PPARgamma, 11beta-HSD1, and Bcl-2 mRNA levels, and increased Bax mRNA in white adipose tissue, while it upregulated UCP1 and UCP3 mRNAs in brown adipose tissue and UCP3 mRNA in gastrocnemial muscle. These results suggest that ER36009 has multiple effects on adipose tissue biology and the energy balance. Topically applied ER36009 may have potential for the treatment of obesity.
Authors:
Tomohiro Sakuta; Taro Uchiyama; Toshiji Kanayama
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Endocrine     Volume:  30     ISSN:  1355-008X     ISO Abbreviation:  Endocrine     Publication Date:  2006 Aug 
Date Detail:
Created Date:  2006-12-22     Completed Date:  2007-02-20     Revised Date:  2010-06-24    
Medline Journal Info:
Nlm Unique ID:  9434444     Medline TA:  Endocrine     Country:  United States    
Other Details:
Languages:  eng     Pagination:  113-9     Citation Subset:  IM    
Affiliation:
Shiseido Pharmaceutical Research Center, 2-12-1 Kanazawa-ku Fukuura, Yokohama, Japan 236-8643. tomohiro.sakuta@to.shiseido.co.jp
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MeSH Terms
Descriptor/Qualifier:
11-beta-Hydroxysteroid Dehydrogenases / biosynthesis,  genetics
Adipose Tissue, Brown / drug effects,  metabolism
Adipose Tissue, White / drug effects*,  metabolism
Adiposity / drug effects*,  genetics
Animals
Blotting, Northern
Body Weight / drug effects,  genetics
Eating / drug effects,  physiology
Ion Channels / biosynthesis,  genetics
Male
Mitochondrial Proteins / biosynthesis,  genetics
PPAR gamma / antagonists & inhibitors,  biosynthesis,  genetics
Proto-Oncogene Proteins c-bcl-2 / biosynthesis,  genetics
Quinoxalines / pharmacology*
RNA, Messenger / biosynthesis,  genetics
Rats
Rats, Sprague-Dawley
Reverse Transcriptase Polymerase Chain Reaction
Thermogenesis / drug effects,  genetics
Thiazoles / pharmacology*
Up-Regulation / drug effects
bcl-2-Associated X Protein / biosynthesis,  genetics
Chemical
Reg. No./Substance:
0/4-(4-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-quinoxalinyl)-1,3-thiazol-2-yl)benzoic acid; 0/Bax protein, rat; 0/Ion Channels; 0/Mitochondrial Proteins; 0/PPAR gamma; 0/Proto-Oncogene Proteins c-bcl-2; 0/Quinoxalines; 0/RNA, Messenger; 0/Thiazoles; 0/bcl-2-Associated X Protein; 0/mitochondrial uncoupling protein; 0/mitochondrial uncoupling protein 3; EC 1.1.1.146/11-beta-Hydroxysteroid Dehydrogenases

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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