Chemical Name:2,2-Bis[4-(2,3-epoxypropoxy)phenyl]propane
Biological Activity:
PPARγ pure antagonist with
micromolar affinity in 3T3-L1 and 3T3-F442A preadipocyte cells; selective over
PPARδ and PPARα. Antagonises the ability of rosiglitazone to stimulate
transcriptional activity of PPARγ. Acts as a PPARγ agonist in an ECV304 cell line. Also produces PPARγ-independent apoptosis of
tumour cells via several mechanisms. Active in vivo.
Wrightet al (2000) A synthetic antagonist for the peroxisome
proliferator-activated receptor g inhibits adipocyte differentiation.
J.Biol.Chem. 275 1873. Bishop-Baileyet al (2000)
Bisphenol A diglycidyl ether (BADGE) is a PPARγ agonist in an ECV304
cell line. Br.J.Pharmacol. 131 651. Fehlberget al
(2003) Bisphenol A diglycidyl ether-induced apoptosis involves
Bax/Bid-dependent mitochondrial release of apoptosis-inducing factor (AIF),
cytochrome c and Smac/DIABLO. Br.J.Pharmacol. 139 495. Cuzzocreaet al (2004) Rosiglitazone, a ligand of the peroxisome
proliferator-activated receptor-γ, reduces acute inflammation.
Eur.J.Pharmacol. 483 79.
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