Biomolecules & Therapeutics

The Korean Society of Applied Pharmacology (한국응용약물학회)
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A Novel PPARγ Agonist, SP1818, Shows Different Coactivator Profile with Rosiglitazone

  • Park, Yun-Sun (Department of Life Science, Research Center for Women's Diseases, Sookmyung Womens University) ;
  • Choi, Ji-Won (Department of Life Science, Research Center for Women's Diseases, Sookmyung Womens University) ;
  • Kim, Kun-Yong (Department of Life Science, Research Center for Women's Diseases, Sookmyung Womens University) ;
  • Lim, Jong-Seok (Department of Life Science, Research Center for Women's Diseases, Sookmyung Womens University) ;
  • Yoon, Suk-Joon (Department of Life Science, Research Center for Women's Diseases, Sookmyung Womens University) ;
  • Yang, Young (Department of Life Science, Research Center for Women's Diseases, Sookmyung Womens University)
  • Published : 2010.01.31
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Abstract

Peroxisome proliferator-activated receptor $\gamma$ (PPAR${\gamma}$) is a ligand-activated transcription factor that is used as a target for anti-diabetic drug development. In a search for novel PPAR${\gamma}$ agonists, the $\beta$-carboxyethyl-rhodanine derivative SP1818 was identified. We report here the characteristics of SP1818 as a selective PPAR${\gamma}$ agonist. In transactivation assays, SP1818 selectively activated PPAR${\gamma}$, but the degree of PPAR${\gamma}$ stimulation was less than with $1{\mu}M$ rosiglitazone. SP1818 also stimulated glucose uptake in a concentration-dependent manner. The adipocyte differentiation markers adiponectin, scavenger receptor CD36 and aP2 were weakly induced by treatment with SP1818, and TRAP220 subunit was specifically recruited into PPAR${\gamma}$ activated by rosiglitazone but not PPAR${\gamma}$ activated by SP1818.

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