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High-throughput crystallography to enhance drug discovery

✍ Scribed by Andrew Sharff; Harren Jhoti

Book ID: 104414777
Publisher: Elsevier Science
Year: 2003
Tongue: English
Weight: 268 KB
Volume: 7
Category: Article
ISSN: 1367-5931
DOI: 10.1016/s1367-5931(03)00062-0

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✦ Synopsis

Protein crystallography has traditionally been regarded as a resource-intensive, time-consuming technique that, with some notable exceptions, has not made a significant impact on drug discovery. However, inspired by successes in the genome-sequencing initiatives, recent years have seen major changes in X-ray crystallography methodologies and the concept of high-throughput crystallography has emerged. Advances have been made in all phases of the process, including improved molecular biology, protein expression, crystallization and structure determination. This transformation has allowed X-ray crystallography to impact more broadly in the drug-discovery process, extending its utility from structure-based lead optimisation to novel fragment-based lead generation approaches.

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