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

Authors
Ahmed, S James, K Owen, CP Patel, CK Patel, MB
Citation
S. Ahmed et al., Determination and use of a transition state for the enzyme estrone sulfatase (ES) from a proposed reaction mechanism, BIOORG MED, 11(23), 2001, pp. 3001-3005
Citations number
10
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
23
Year of publication
2001
Pages
3001 - 3005
Database
ISI
SICI code
0960-894X(200112)11:23<3001:DAUOAT>2.0.ZU;2-6
Abstract
Using the postulated mechanism for the enzyme estrone sulfatase (ES), we ha ve determined a possible transition state for the reaction catalysed by ES as a representation of the active site. Using the derived structure, we hav e undertaken the molecular modelling of several steroidal and non-steroidal inhibitors in an attempt to rationalise the inhibitory activity of a numbe r of potent inhibitors. (C) 2001 Elsevier Science Ltd. All rights reserved.