Structures of Human Acetylcholinesterase in Complex with Pharmacologically Important Ligands

被引：1110

作者：

Cheung, Jonah ^{[1
]}

Rudolph, Michael J. ^{[1
]}

Burshteyn, Fiana ^{[1
]}

Cassidy, Michael S. ^{[1
]}

Gary, Ebony N. ^{[1
]}

Love, James ^{[1
]}

Franklin, Matthew C. ^{[1
]}

Height, Jude J. ^{[2
]}

机构：

[1] New York Struct Biol Ctr, New York, NY 10027 USA

[2] Edgewood Chem Biol Ctr, Aberdeen Proving Ground, MD 21010 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2012年 / 55卷 / 22期

关键词：

3-DIMENSIONAL STRUCTURE; TORPEDO-CALIFORNICA; BINDING; SITE; INHIBITORS; DESIGN; E2020;

D O I：

10.1021/jm300871x

中图分类号：

R914 [药物化学];

学科分类号：

100705 [微生物与生化药学];

摘要：

Human acetylcholinesterase (AChE) is a significant target for therapeutic drugs. Here we present high resolution crystal structures of human AChE, alone and in complexes with drug ligands; donepezil, an Alzheimer's disease drug, binds differently to human AChE than it does to Torpedo AChE. These crystals of human AChE provide a more accurate platform for further drug development than previously available.

引用

收藏

页码：10282 / 10286

页数：5

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