ERRγ tethers strongly bisphenol A and 4-α-cumylphenol in an induced-fit manner

被引：64

作者：

Matsushima, Ayami ^{[1
,2
]}

Teramoto, Takamasa ^{[3
,4
]}

Okada, Hiroyuki ^{[1
,2
]}

Liu, Xiaohui ^{[1
,2
]}

Tokunaga, Takatoshi ^{[1
,2
]}

Kakuta, Yoshimitsu ^{[3
,4
]}

Shimohigashi, Yasuyuki ^{[1
,2
]}

机构：

[1] Kyushu Univ, Lab Struct Funct Biochem, Dept Chem, Res Educ Ctr Risk Sci,Fac Sci, Fukuoka 8128581, Japan

[2] Kyushu Univ, Lab Struct Funct Biochem, Dept Chem, Res Educ Ctr Risk Sci,Grad Sch Sci, Fukuoka 8128581, Japan

[3] Kyushu Univ, Biochem Lab, Dept Agr Chem, Fac Agr, Fukuoka 8128581, Japan

[4] Kyushu Univ, Biochem Lab, Dept Agr Chem, Grad Sch Agr, Fukuoka 8128581, Japan

来源：

BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS | 2008年 / 373卷 / 03期

关键词：

bisphenol A; 4-alpha-cumylphenol; endocrine disruptor; estrogen-related receptor gamma (ERR gamma); nuclear receptor; X-ray crystal structure;

D O I：

10.1016/j.bbrc.2008.06.050

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A receptor-binding assay and X-ray crystal structure analysis demonstrated that the endocrine disruptor bisphenol A (BPA) strongly binds to human estrogen-related receptor gamma (ERR gamma). BPA is well anchored to the ligand-binding pocket, forming hydrogen bonds with its two phenol-hydroxyl groups. In this study, we found that 4-alpha-cumylphenol lacking one of its phenol-hydroxyl groups also binds to ERR gamma very strongly. The 2.0 angstrom crystal structure of the 4-alpha-cumylphenol/ERR gamma complex clearly revealed that ERR gamma's Leu345-beta-isopropyl plays a role in the tight binding of 4-alpha-cumylphenol and BPA, rotating in a back-and-forth induced-fit manner. 2008 Elsevier Inc. All rights reserved.

引用

页码：408 / 413

页数：6

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