Binding Model of Amentoflavone to Peroxisome Proliferator-Activated Receptor γ

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 amentofla...

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Bibliographic Details
Published in:Bulletin of the Korean Chemical Society 2012, 33(5), , pp.1475-1479
Main Authors: 이지영, 김진경, 이소정, 이은정, 신소영, Qinglong Jin, 윤도영, 우은란, 김양미
Format: Article
Language:English
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화학
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Summary: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. KCI Citation Count: 0
ISSN:0253-2964
1229-5949
DOI:10.5012/bkcs.2012.33.5.1475