Determination and use of a transition state for the enzyme estrone sulfatase (ES) from a proposed reaction mechanism

被引：19

作者：

Ahmed, S ^{[1
]}

James, K ^{[1
]}

Owen, CP ^{[1
]}

Patel, CK ^{[1
]}

Patel, MB ^{[1
]}

机构：

[1] Kingston Univ, Sch Chem & Pharmaceut Sci, Kingston upon Thames KT1 2EE, Surrey, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 23期

关键词：

D O I：

10.1016/S0960-894X(01)00607-2

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Using the postulated mechanism for the enzyme estrone sulfatase (ES), we have determined a possible transition state for the reaction catalysed by ES as a representation of the active site. Using the derived structure, we have undertaken the molecular modelling of several steroidal and non-steroidal inhibitors in an attempt to rationalise the inhibitory activity of a number of potent inhibitors. (C) 2001 Elsevier Science Ltd. All rights reserved.

引用

页码：3001 / 3005

页数：5

共 10 条

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