Description
Researchers from academia and from pharmaceutical companies present information on how to obtain protein structures suited for rational drug design and how to exploit crystallographic data for the drug discovery process. They examine the crystallography of target classes such as kinases and proteases, look at the structure-based design of protease and kinase inhibitors, and discuss ribosome and proteasome as drug targets. Other topics discussed include molecular recognition of nuclear hormone receptor-ligand complexes, crystallization and analysis of serine proteases with ecotin, engineering proteins to promote crystallization, and micro-crystallization. Babine and Abdel-Meguid are both affiliated with a drug discovery company. Annotation ©2004 Book News, Inc., Portland, OR (booknews.com)
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The rational, structure-based approach has become standard in present-day drug design. As a consequence, the availability of high-resolution structures of target proteins is more often than not the basis for an entire drug development program. Protein structures suited for rational drug design are almost exclusively derived from crystallographic studies, and drug developers are relying heavily on the power of this method.Here, researchers from leading pharmaceutical companies present valuable first-hand information, much of it published for the first time. They discuss strategies to derive high-resolution structures for such important target protein classes as kinases or proteases, as well as selected examples of successful protein crystallographic studies. A special section on recent methodological developments, such as for high-throughput crystallography and microcrystallization, is also included.A valuable companion for crystallographers involved in protein structure determination as well as drug developers pursuing the structure-based approach for use in their daily work.
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