A Synthetic Antagonist for the Peroxisome Proliferator-activated Receptor γ Inhibits Adipocyte Differentiation
While searching for natural ligands for the peroxisome proliferator-activated receptor (PPAR) γ, we identified a synthetic compound that binds to this receptor. Bisphenol A diglycidyl ether (BADGE) is a ligand for PPARγ with aKd(app) of 100 μm. This compound has no apparent ability to activate the t...
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Published in: | The Journal of biological chemistry 2000-01, Vol.275 (3), p.1873-1877 |
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Main Authors: | , , , , , , , |
Format: | Article |
Language: | eng |
Subjects: | |
Online Access: | Get full text |
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Summary: | While searching for natural ligands for the peroxisome proliferator-activated receptor (PPAR) γ, we identified a synthetic compound that binds to this receptor. Bisphenol A diglycidyl ether (BADGE) is a ligand for PPARγ with aKd(app) of 100 μm. This compound has no apparent ability to activate the transcriptional activity of PPARγ; 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 PPARγ activity is required for the hormonally induced differentiation of adipogenic cells. |
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ISSN: | 0021-9258 1083-351X |