Protein Crystallography in Drug Discovery

ACE is a highly glycosylated protein and has proved hard to crystallize for more than two decades. ... 3.0 Å). a D D D D 9.4 Improving Crystal Packing by Point Mutation It is well known that homologous proteins from different species do ...

Author: Robert E. Babine

Publisher: John Wiley & Sons

ISBN: 9783527606351

Category: Science

Page: 278

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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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Protein Crystallography

Illustration of how a crystal is built up by symmetric repetition of simple elements. (a) The asymmetric unit is the smallest entity that is necessary to build up the entire crystal. In this example, the asymmetric unit corresponds to a ...

Author: Eaton E. Lattman

Publisher: JHU Press

ISBN: 9780801888069

Category: Science

Page: 149

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The proteome remains a mysterious realm. Researchers have determined the structures of only a small fraction of the proteins encoded by the human genome. Crystallography continues to be the primary method used to determine the structures of the remaining unknown proteins. This imaging technique uses the diffraction of X-rays to determine a protein's three-dimensional molecular structure. Drawing on years of research and teaching experience, Eaton E. Lattman and Patrick J. Loll use clear examples and abundant illustrations to provide a concise and accessible primer on protein crystallography. Discussing the basics of diffraction, the behavior of two- and three-dimensional crystals, phase determination (including MIR and MAD phasing and molecular replacement), the Patterson function, and refinement, Lattman and Loll provide a complete overview of this important technique, illuminated by physical insights. The crisp writing style and simple illustrations will provide beginner crystallographers with a guide to the process of unraveling protein structure.
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Protein Crystallography

Significant numbers of proteins were being crystallised by biochemists. The advances in these fields of crystallography and protein biochemistry continued essentially in parallel. Up to the development of direct methods begun in 1953 by ...

Author: Gwyndaf Evans

Publisher: Royal Society of Chemistry

ISBN: 9781782627289

Category: Science

Page: 244

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Protein crystallography has become vital to further understanding the structure and function of many complex biological systems. In recent years, structure determination has progressed tremendously however the quality of crystals and data sets can prevent the best results from being obtained. With contributions from world leading researchers whose software are used worldwide, this book provides a coherent approach on how to handle difficult crystallographic data and how to assess its quality. The chapters will cover all key aspects of protein crystallography, from instrumentation and data processing through to model building. This book also addresses challenges that protein crystallographers will face such as dealing with data from microcrystals and multi protein complexes. This book is ideal for both academics and researchers in industry looking for a comprehensive guide to protein crystallography.
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Protein Crystallography

Significant numbers of proteins were being crystallised by biochemists. The advances in these fields of crystallography and protein biochemistry continued essentially in parallel. Up to the development of direct methods begun in 1953 by ...

Author: Konstantinos Beis

Publisher: Royal Society of Chemistry

ISBN: 9781788014779

Category: Science

Page: 228

View: 500

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Protein crystallography has become vital to further understanding the structure and function of many complex biological systems. In recent years, structure determination has progressed tremendously however the quality of crystals and data sets can prevent the best results from being obtained. With contributions from world leading researchers whose software are used worldwide, this book provides a coherent approach on how to handle difficult crystallographic data and how to assess its quality. The chapters will cover all key aspects of protein crystallography, from instrumentation and data processing through to model building. This book also addresses challenges that protein crystallographers will face such as dealing with data from microcrystals and multi protein complexes. This book is ideal for both academics and researchers in industry looking for a comprehensive guide to protein crystallography.
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Neutron Protein Crystallography

Flow chart of the experimental procedure for neutron protein crystallography When is it appropriate to carry out a neutron-protein crystallography (NPC) experiment? The basic principles of NPC are very similar to those of X-ray protein ...

Author: Nobuo Niimura

Publisher: Oxford University Press

ISBN: 9780199578863

Category: Science

Page: 250

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One of the first books dedicated to the emerging field of neutron protein crystallography (NPC). It covers all of the practical aspects of NPC and demonstrates how NPC can explore protein features such as hydrogen bonds, protonation and deprotonation of amino acid residues, and hydration structures.
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Practical Protein Crystallography

Appendix A contains formulae commonly used in protein crystallography, but with a twist: the formulae are coded in both FORTRAN77 and C. These two languages easily account for 99% of all protein crystallographic software.

Author: Duncan E. McRee

Publisher: Academic Press

ISBN: 9780323138888

Category: Science

Page: 386

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Designed for easy use by both new and experienced protein crystallographers, this much-needed book is for anyone interested in solving protein structures by the method of crystallography. It contains many examples ofactual experiments and data, including electron density maps. Computer methods and computer code samples are presented. Practical Protein Crystallography is loaded with new information on area detectors, synchrotron radiation techniques, and the latest computer methods, and features the XtalView software system. Graduate students and teachers in physical biochemistry and pharmaceutical researchers will find this text a timely and convenient aid.
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Principles of Protein X ray Crystallography

Introduction Students new to the protein X - ray crystallography laboratory may understandably be confused when colleagues discuss Fouriers and Pattersons or molecular replacement and molecular dynamics refinement .

Author: Jan Drenth

Publisher: Springer Science & Business Media

ISBN: 0387985875

Category: Science

Page: 368

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New textbooks at all levels of chemistry appear with great regularity. Some fields such as basic biochemistry, organic reaction mechanisms, and chemical thermodynamics are well represented by many excellent texts, and new or revised editions are published sufficiently often to keep up with progress in research. However, some areas of chemistry, especially many of those taught at the graduate level, suffer from a real lack of up to-date textbooks. The most serious needs occur in fields that are rapidly changing. Textbooks in these subjects usually have to be written by scientists actually involved in the research that is advancing the field. It is not often easy to persuade such individuals to set time aside to help spread the knowledge they have accumulated. Our goal, in this series, is to pinpoint areas of chemistry where recent progress has outpaced what is covered in any available textbooks, and then seek out and persuade experts in these fields to produce relatively concise but instructive intro ductions to their fields. These should serve the needs of one-semester or one-quarter graduate courses in chemistry and biochemistry. In some cases, the availability of texts in active research areas should help stimulate the creation of new courses. Charles R. Cantor v Preface to the Second Edition Since the publication of the previous edition in 1994, X-ray crystallography of proteins has advanced by improvements in existing techniques and by addition of new techniques.
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Protein Crystallography

1974 Fumio Oosawa and Sho Asakura. Thermodynamics of the Polymerization of Protein. 1975 Lawrence J. Berliner (Editor). Spin Labeling: Theory and Applications. 1976 T. Blundell and L. Johnson. Protein Crystallography.

Author: T. L. Blundell

Publisher: Academic Press

ISBN: MINN:31951P00354400S

Category: Science

Page: 565

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Membrane Protein Crystallization

Morphological eVects of ceramide on DMPC/DHPC bicelles. Journal de Microscopie, 230, 16–26. Carpenter, E. P., Beis, K., Cameron, A. D., & Iwata, S. (2008). Overcoming the challenges of membrane protein crystallography.

Author:

Publisher: Academic Press

ISBN: 0080961592

Category: Science

Page: 336

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This volume of Current Topics in Membranes focuses on Membrane Protein Crystallization, beginning with a review of past successes and general trends, then further discussing challenges of mebranes protein crystallization, cell free production of membrane proteins and novel lipids for membrane protein crystallization. This publication also includes tools to enchance membrane protein crystallization, technique advancements, and crystallization strategies used for photosystem I and its complexes, establishing Membrane Protein Crystallization as a needed, practical reference for researchers.
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Protein Crystallization

The groundbreaking work that firmly and finally established the value of protein crystallization, however, came in the 1930s with the early experiments of Crowfoot, Bernal, and Fankeuchen, who applied X-ray diffraction to protein ...

Author: Terese M. Bergfors

Publisher: Internat'l University Line

ISBN: 9780972077446

Category: Science

Page: 505

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