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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.
Macromolecular crystallography is the study of macromolecules using X-ray crystallographic techniques to determine their molecular structure. This title synthesises contributions from a team of internationally recognized leaders, offering chapters on conventional and high-throughput methods.
Proteases are enzymes that essentially "eat" protein. Without proteases, infectious organisms cannot properly mount an attack against a host. It is for this reason that proteases have become popular targets for drug discovery. Research has shown that if you can inhibit the protease, you can defend against the invading microbe. The defense against HIV, the virus that causes AIDS, is the best-documented case of the efficacy of protease inhibitors. Researchers are now trying to deploy this strategy against several infectious agents. This book gives information that is useful in that search.Proteases of Infectious Agents collects reviews from leading experts describing the latest information on ...
Navigate the complex and multidisciplinary path of drug discovery procedures with Drug Discovery Strategies and Methods-a well-organized and timely reference that analyzes methods in target identification and validation, lead detection, compound optimization, and biological testing. This volume addresses challenges encountered during the discovery
In this masterful account, a historian of science surveys the molecular biology revolution, its origin and continuing impact. Since the 1930s, a molecular vision has been transforming biology. Michel Morange provides an incisive and overarching history of this transformation, from the early attempts to explain organisms by the structure of their chemical components, to the birth and consolidation of genetics, to the latest technologies and discoveries enabled by the new science of life. Morange revisits A History of Molecular Biology and offers new insights from the past twenty years into his analysis. The Black Box of Biology shows that what led to the incredible transformation of biology w...
The American Heart Association’s Scientific Sessions 2016 is bringing big science, big technology, and big networking opportunities to New Orleans, Louisiana this November. This event features five days of the best in science and cardiovascular clinical practice covering all aspects of basic, clinical, population and translational content.
The critically acclaimed laboratory standard, Methods in Enzymology, is one of the most highly respected publications in the field of biochemistry. Since 1955, each volume has been eagerly awaited, frequently consulted, and praised by researchers and reviewers alike. The series contains much material still relevant today - truly an essential publication for researchers in all fields of life sciences.