Sequence-function correlation of aromatase and its interaction with reductase.
Sequence-function correlation of aromatase and its interaction with reductase.
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DOI：
10.1016/j.jsbmb.2009.11.010
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发表时间：
2010-02-28
影响因子：
4.1
通讯作者：
Chen, Shiuan
中科院分区：
文献类型：
--
作者：
Hong, Yanyan;Li, Hongzhi;Yuan, Yate-Ching;Chen, Shiuan
芳香化酶是雄激素转化为雌激素所需的酶。雌激素是女性性激素，参与乳腺肿瘤的发展和生长。芳香化酶抑制剂在乳腺癌的治疗中显示出巨大的潜力，因此研究芳香化酶的结构与功能的关系具有重要意义。芳香化酶属于细胞色素P450家族，在芳构化反应中与其配偶体NADPH-细胞色素P450还原酶（CPR）形成电子转移复合物。芳香化酶在脊椎动物中广泛表达，底物雄烯二酮和睾酮独特，但其催化能力不同，反映了物种间Km、Vmax等的差异。本文综述了芳香化酶蛋白家族的序列-功能相关性分析以及芳香化酶与CPR相互作用的分子特征。这些研究可能为开发新的抑制剂开辟新的领域，这些抑制剂干扰芳香化酶和CPR之间的相互作用以抑制芳构化反应。
Aromatase is an enzyme required for the conversion of androgens to estrogens. Estrogens are female sex hormones involved in the development and growth of breast tumors. It has been of significant interest to investigate the structure-function relationship of aromatase 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 (CPR), during the aromatization reaction. Aromatase is found to be widely expressed in vertebrates with unique substrates androstenedione and testosterone, but with various catalytic capacities reflecting species differences in Km, Vmax, and etc. This report will summarize current progress in sequence-function correlation analysis of the aromatase protein family and molecular characterization of the interaction between aromatase and CPR. These studies may lead to a novel field for the development of new inhibitors which interfere with the interaction between aromatase and CPR in order to inhibit the aromatization reaction.
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影响因子：
--
作者：
Hong, Yanyan;Yu, Bin;Chen, Shiuan
通讯作者：
Chen, Shiuan
影响因子：
--
作者：
POMPON, D;LIU, RYK;CHEN, S
通讯作者：
CHEN, S
DOI：
10.1046/j.1432-1033.2001.01886.x
发表时间：
2001-01-01
期刊：
EUROPEAN JOURNAL OF BIOCHEMISTRY
影响因子：
--
作者：
Kao, YC;Korzekwa, KR;Chen, S
通讯作者：
Chen, S
影响因子：
5.8
作者：
Zhang, FM;Zhou, DJ;Chen, S
通讯作者：
Chen, S
DOI：
10.1073/pnas.85.23.8948
发表时间：
1988-12-01
影响因子：
11.1
作者：
CORBIN, CJ;GRAHAMLORENCE, S;SIMPSON, ER
通讯作者：
SIMPSON, ER