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Protein Crystallography in Drug Discovery



Protein Crystallography in Drug Discovery


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.
Molecular Recognition of Nuclear Hormone Receptor-Ligand Complexes
The Proteasome as a Drug Target
Antibiotics and the Ribosome
Strucutre-based Design of Cathepsin K Inhibitors
Structure-based Design of Potent and Selective Cdk4 Inhibitors
Crystallization and Analysis of Serine Proteases with Ecotin
X-ray Crystallography in the Development of Orthogonal Ligand-Receptor Pairs
Engineering Proteins to Promote Crystallization
High-throughput Crystallography
"Medicinal chemists will find the book invaluable whether they are working in an area of one of the chapters or wish to apply the methods described to other projects. Structural and computational biologists should also find it useful and thought-provoking."
ChemBioChem August

Lars-Oliver Essen, Fachbereich Chemie, Philipps-Universität Marburg, Angewandte Chemie, 3. Dezemberheft 2004-116/47 und Angewandte Chemie International Edition, 3rd December Issue 2004-43/47

"The quality of the individual chapters of this volume is high, and each of the contributors is to be commended for their efforts."

Steven W. Muchmore, Department of Structural Biology, Global Pharmaceutical Research Division, Abbott Laboratories, Abbott Park, Illinois, Journal of Medicinal Chemistry, Vol. 47, No. 26, 2004

"... an important contribution to pharmaceutical research and development."
American Journal of Therapeutics