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A synthetic antagonist for the peroxisome proliferator-activated receptor gamma inhibits adipocyte differentiation.

A synthetic antagonist for the peroxisome proliferator-activated receptor gamma inhibits adipocyte differentiation.

Authors :
Wright, H M
Clish, C B
Mikami, T
Hauser, S
Yanagi, K
Hiramatsu, R
Serhan, C N
Spiegelman, B M
Source :
Journal of Biological Chemistry; January 2000, Vol. 275 Issue: 3 p1873-7, 5p
Publication Year :
2000

Abstract

While searching for natural ligands for the peroxisome proliferator-activated receptor (PPAR) gamma, we identified a synthetic compound that binds to this receptor. Bisphenol A diglycidyl ether (BADGE) is a ligand for PPARgamma with a K(d(app)) of 100 microM. This compound has no apparent ability to activate the transcriptional activity of PPARgamma; however, BADGE can antagonize the ability of agonist ligands such as rosiglitazone to activate the transcriptional and adipogenic action of this receptor. BADGE also specifically blocks the ability of natural adipogenic cell lines such as 3T3-L1 and 3T3-F442A cells to undergo hormone-mediated cell differentiation. These results provide the first pharmacological evidence that PPARgamma activity is required for the hormonally induced differentiation of adipogenic cells.

Details

Language :
English
ISSN :
00219258 and 1083351X
Volume :
275
Issue :
3
Database :
Supplemental Index
Journal :
Journal of Biological Chemistry
Publication Type :
Periodical
Accession number :
ejs7152216