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Two Synthetic Ligands for Peroxisome Proliferator- Activated Receptor $gamma$
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  • Two Synthetic Ligands for Peroxisome Proliferator- Activated Receptor $gamma$
저자명
Kim. Min-A,Jeong. Sun-Hyo,Song. Yang-Heon,Kim. Dae-Il,Yoon. Mi-Chung
간행물명
Journal of experimental & biomedical sciences
권/호정보
2004년|10권 2호|pp.137-142 (6 pages)
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대한의생명과학회
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이 논문은 한국과학기술정보연구원과 논문 연계를 통해 무료로 제공되는 원문입니다.
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기타언어초록

The peroxisome proliferator-activated receptor $gamma$ (PPAR${gamma}$) is the molecular target for a class of drugs, the antidiabetic thiazolidnediones (TZDs). The heterodimer of PPAR${gamma}$ 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 PPAR$gamma$ 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 PPAR$gamma$. These results suggest that DANA87 and DANA88 are not only weak agonists of PPAR${gamma}$ transactivation, but also competitively antagonize troglitazone-induced PPAR$gamma$ reporter activity.