✦ LIBER ✦

The genesis of high-throughput structure-based drug discovery using protein crystallography

✍ Scribed by Peter Kuhn; Keith Wilson; Marianne G Patch; Raymond C Stevens

Book ID: 104414701
Publisher: Elsevier Science
Year: 2002
Tongue: English
Weight: 117 KB
Volume: 6
Category: Article
ISSN: 1367-5931
DOI: 10.1016/s1367-5931(02)00361-7

No coin nor oath required. For personal study only.

✦ Synopsis

Over the past 12 years, drugs have been developed using structure-based drug design relying upon traditional crystallographic methods. Established successes, such as the drugs designed against HIV-1 protease and neuraminidase, demonstrate the utility of a structure-based approach in the drug-discovery process. However, the approach has historically lacked throughput and reliability capabilities; these bottlenecks are being overcome by breakthroughs in high-throughput structural biology. Recent technological innovations such as submicroliter high-throughput crystallization, high-performance synchrotron beamlines and rapid binding-site analysis of de novo targets using virtual ligand screening and small molecule co-crystallization have resulted in a significant advance in structure-based drug discovery.

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