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KMID : 0603820040100020137
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Journal of Experimental & Biomedical Science
2004 Volume.10 No. 2 p.137 ~ p.142
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Two Synthetic Ligands for Peroxisome Proliferator-Activated Receptor γ
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김미나:Kim Mi-Na
정선효:Jeong Sun-Hyo/송양헌:Song Yang-Heon/김대일:Kim Dae-Il/윤미정:Yoon Mi-Chung
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Abstract
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The peroxisome proliferator-activated receptor γ (PPARγ) is the molecular target for a class of drugs, the antidiabetic thiazolidnediones (TZDs). The heterodimer of PPARγ with retinoid X receptor (RXR) plays a central role in the regulation of adipogenesis and insulin sensitization. We synthesized two chemicals, DANA87 and DANA88, sharing structural characteristics with TZDs. Given this structural similarity, it was hypothesized that DANA87 and DANA88 may act as PPARγ ligands. In transient transfection assays, DANA87 and DANA88 caused slight increases in the endogenous expression of a luciferase reporter gene containing the PPAR responsive element in 3T3-L1 preadipocytes. However, DANA87 and DANA88 significantly inhibited troglitazone-induced reporter gene activation when cells were treated with a combination of DANA87 or DANA 88 and troglitazone, one of the TZDs that activate PPARγ. These results suggest that DANA87 and DANA88 are not only weak agonists of PPARγ transactivation, but also competitively antagonize troglitazone-induced PPARγ reporter activity.
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KEYWORD
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PPARγ, Synthetic ligand, Transient transfection assay
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