Binding Model of Amentoflavone to Peroxisome Proliferator-Activated Receptor γ

Bulletin of the Korean chemical society

Eun-Rhan Woo¹  Jin-Kyoung Kim¹  Qinglong Jin¹  Soyoung Shin¹  Do-Young Yoon¹  Eunjung Lee¹  Sojung Lee¹  Yangmee Kim¹  Jee-Young Lee¹ 

关键词: PPARγ;    Agonist;    Flavonoid;    Amentoflavone;    Docking;   

DOI  :  

学科分类：化学（综合）

来源: Korean Chemical Society

【 摘 要 】

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.

【 授权许可】

Unknown