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Curr Opin Chem Biol. 2002 Oct;6(5):704-10.

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

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Stanford Synchrotron Radiation Laboratory, Stanford University, 2575 Sand Hill Road, Menlo Park, CA 94025, USA.


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.

[Indexed for MEDLINE]

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