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Bulletin of the Korean Chemical Society (BKCS)

ISSN 0253-2964(Print)
ISSN 1229-5949(Online)
Volume 33, Number 5
BKCSDE 33(5)
May 20, 2012 

Binding Model of Amentoflavone to Peroxisome Proliferator-Activated Receptor γ
Jee-Young Lee, Jin-Kyoung Kim, Sojung Lee, Eunjung Lee, Soyoung Shin, Qinglong Jin, Do-Young Yoon, Eun-Rhan Woo, Yangmee Kim*
PPARγ, Agonist, Flavonoid, Amentoflavone, Docking
Human peroxisome proliferator-activated receptor gamma (hPPARγ) has been implicated in numerous pathologies, including obesity, diabetes, and cancer. In this study, we verified that amentoflavone is an agonist of hPPARγ and probed the molecular basis of its action. It was demonstrated that amentoflavone bound hPPARγ with high (picomolar) affinity and increased the binding between hPPARγ and steroid receptor coactivator-1 (SRC-1) by approximately 4-fold. Based on a docking study, for the first time, we propose a model of amentoflavone and hPPARγ binding in which amentoflavone forms three hydrogen bonds with the side chains of His323, Tyr327, and Arg280 in hPPARγ and participates in two hydrophobic interactions.
1475 - 1479
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