A fully integrated protein crystallization platform for small-molecule drug discovery

被引：57
作者：
Hosfield, D
Palan, J
Hilgers, M
Scheibe, D
McRee, DE
Stevens, RC
机构：
[1] Syrrx Inc, San Diego, CA 92121 USA
[2] Scripps Res Inst, Dept Mol Biol, La Jolla, CA 92037 USA
[3] Scripps Res Inst, Joint Ctr Struct Genom, La Jolla, CA 92037 USA
来源：
JOURNAL OF STRUCTURAL BIOLOGY | 2003年 / 142卷 / 01期
基金：
美国国家卫生研究院;
关键词：
crystallization; automation; protein structure; drug discovery; X-ray;
D O I：
10.1016/S1047-8477(03)00051-0
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：
Structure-based drug discovery in the pharmaceutical industry benefits from cost-efficient methodologies that quickly assess the feasibility of specific, often refractory, protein targets to form well-diffracting crystals. By tightly coupling construct and purification diversity with nanovolume crystallization, the Structural Biology Group at Syrrx has developed such a platform to support its small-molecule drug-discovery program. During the past 18 months of operation at Syrrx, the Structural Biology Group has executed several million crystallization and imaging trials on over 400 unique drug-discovery targets. Here, key components of the platform, as well as an analysis of some experimental results that allowed for platform optimization, will be described. (C) 2003 Elsevier Science (USA). All rights reserved.
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收藏
页码：207 / 217
页数：11
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