芳香化酶的分子特征
Molecular characterization of aromatase.
作者信息
Hong Yanyan, Li Hongzhi, Yuan Yate-Ching, Chen Shiuan
机构信息
Department of Surgical Research, Beckman Research Institute of City of Hope, Duarte, California 91010, USA.
出版信息
Ann N Y Acad Sci. 2009 Feb;1155:112-20. doi: 10.1111/j.1749-6632.2009.03703.x.
Abstract
Aromatase is an estrogen synthetase. Estrogens are female sex hormones involved in the development and growth of breast tumors. Elucidation of the structure-function relationship of aromatase has been of significant interest since its inhibitors have shown great promise in fighting breast cancer. Aromatase belongs to the cytochrome P450 family and forms an electron-transfer complex with its partner, NADPH-cytochrome P450 reductase. Because of the membrane-bound character and heme-binding instability, no crystal structure of aromatase has been reported so far. Much remains to be investigated, including the 3-dimensional structure of aromatase, interaction between aromatase and reductase, catalytic mechanism of estrogen synthesis by aromatase, and the binding mechanism of aromatase inhibitors. This review presents current knowledge about structural and functional characteristics of aromatase to address unsolved mysteries about this enzyme.
摘要
芳香化酶是一种雌激素合成酶。雌激素是参与乳腺肿瘤发生和生长的女性性激素。自从其抑制剂在对抗乳腺癌方面显示出巨大潜力以来，阐明芳香化酶的结构 - 功能关系一直备受关注。芳香化酶属于细胞色素P450家族，并与其伴侣NADPH - 细胞色素P450还原酶形成电子传递复合物。由于其膜结合特性和血红素结合不稳定性，迄今为止尚未报道过芳香化酶的晶体结构。仍有许多问题有待研究，包括芳香化酶的三维结构、芳香化酶与还原酶之间的相互作用、芳香化酶合成雌激素的催化机制以及芳香化酶抑制剂的结合机制。本综述介绍了关于芳香化酶结构和功能特征的当前知识，以解决有关该酶的未解之谜。
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