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KMID : 0606920100180010077
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Biomolecules & Therapeutics
2010 Volume.18 No. 1 p.77 ~ p.82
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A Novel PPARγ Agonist, SP1818, Shows Different Coactivator Profile with Rosiglitazone
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Park Yun-Sun
Lim Jong-Seok
Yoon Suk-Joon
Yang Young
Choi Ji-Won
Kim Kun-Yong
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Abstract
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Peroxisome proliferator-activated receptor γ (PPARγ) is a ligand-activated transcription factor that is used as a target for anti-diabetic drug development. In a search for novel PPARγ agonists, the β-carboxyethyl-rhodanine derivative SP1818 was identified. We report here the characteristics of SP1818 as a selective PPARγ agonist. In transactivation assays, SP1818 selectively activated PPARγ, but the degree of PPARγ stimulation was less than with 1 μM 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 PPARγ activated by rosiglitazone but not PPARγ activated by SP1818.
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KEYWORD
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Adipogenesis, Diabetes, Rosiglitazone
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