Apo and inhibitor complex structures of BACE (β-secretase)

被引：179

作者：

Patel, S ^{[1
]}

Vuillard, L ^{[1
]}

Cleasby, A ^{[1
]}

Murray, CW ^{[1
]}

Yon, J ^{[1
]}

机构：

[1] Astex Technol, Cambridge CB4 0QA, England

来源：

JOURNAL OF MOLECULAR BIOLOGY | 2004年 / 343卷 / 02期

关键词：

BACE; crystallography; drug discovery; Alzheimer's disease;

D O I：

10.1016/j.jmb.2004.08.018

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：

Human BACE, also known as beta-secretase, shows promise as a potential therapeutic target for Alzheimer's disease. We determined the apo structure of BACE to 1.75 Angstrom, and a structure of a hydroxyethylamine inhibitor complex derived by soaking. These show significant active-site movements compared to previously described BACE structures. Additionally, the structures reveal two pockets that could be targeted by structure-based drug design. (C) 2004 Elsevier Ltd. All rights reserved.

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收藏

页码：407 / 416

页数：10

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