Protein Crystallography In Drug Discovery (methods And Principles In Medicinal Chemistry)

E-Book Overview

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.

E-Book Content

Protein Crystallography in Drug Discovery Edited by R. E. Babine and S. S. Abdel-Meguid Protein Crystallography in Drug Discovery Edited by R. E. Babine and S. S. Abdel-Meguid Copyright ° 2004 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim ISBN: 3-527-30678-1 Methods and Principles in Medicinal Chemistry Edited by R. Mannhold H. Kubinyi G. Folkers Editorial Board H.-D. Hæltje, H. Timmerman, J. Vacca, H. van de Waterbeemd, T. Wieland Recently published Volumes: Vol. 12 Drug Targeting G. Molema, D. K. F. Meijer (eds.) 2001, ISBN 3-527-29989-0 Vol. 13 Pharmacokinetics and Metabolism in Drug Design D. Smith, D. Walker, H. van de Waterbeemd 2001, ISBN 3-527-30197-6 Vol. 14 Bioinformatics ± From Genomes to Drugs T. Lengauer (ed.) 2001, ISBN 3-527-29988-2 Vol. 15 Drug-Membrane Interactions J. K. Seydel, M. Wiese 2002, ISBN 3-527-30427-4 Vol. 16 BioNMR in Drug Research O. Zerbe (ed.) 2002, ISBN 3-527-30465-7 Vol. 17 Quantum Medicinal Chemistry P. Carloni, F. Alber (eds.) 2003, ISBN 3-527-30456-8 Vol. 18 Drug Bioavailability H. van de Waterbeemd, H. Lennernås, P. Artursson (eds.) 2003, ISBN 3-527-30438-X Vol. 19 Protein-Ligand Interactions H.-J. Bæhm, G. Schneider (eds.) 2003, ISBN 3-527-30521-1 Protein Crystallography in Drug Discovery Edited by R. E. Babine and S. S. Abdel-Meguid Series Editors: Prof. Dr. Raimund Mannhold Biomedical Research Center Molecular Drug Research Group Heinrich-Heine-Universitåt Universitåtsstraûe 1 40225 Dçsseldorf Germany [email protected] Prof. Dr. Hugo Kubinyi BASF AG Ludwigshafen c/o Donnersbergstraûe 9 67256 Weisenheim am Sand Germany [email protected] Prof. Dr. Gerd Folkers Department of Applied Biosciences ETH Zçrich Winterthurerstr. 190 8057 Zçrich Switzerland [email protected] Volume Editors: Dr. Robert E. Babine Suntory Pharmaceutical Research Laboratories One Kendall Square Cambridge, MA 02139 USA [email protected] Dr. Sherin S. Abdel-Meguid Suntory Pharmaceutical Research Laboratories One Kendall Square Cambridge, MA 02139 USA [email protected] n This book was carefully pro
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