Carbonic Anhydrase As Drug Target

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Carbonic Anhydrase as Drug Target

Author : Daumantas Matulis
Publisher : Springer
ISBN 13 : 303012780X
Total Pages : 358 pages
Book Rating : 4.0/5 (31 download)

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Book Synopsis Carbonic Anhydrase as Drug Target by : Daumantas Matulis

Download or read book Carbonic Anhydrase as Drug Target written by Daumantas Matulis and published by Springer. This book was released on 2019-05-21 with total page 358 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book offers deep insights into the thermodynamics and molecular structures of the twelve catalytically active isoforms of human carbonic anhydrase (CA) with a particular focus on inhibitor binding for drug design. X-ray crystallographic structures in combination with enzyme kinetic testing provide information on the interaction of CAs and their inhibitors, knowledge which is crucial for rational drug design. CAs are zinc carrying enzymes that catalyse the reversible interconversion of carbon dioxide and bicarbonate and are involved in numerous cellular processes. They are therefore a common target for drugs. The suppression of CA activities through inhibitory compounds has found application for example in diuretics and in glaucoma therapy. In this book methods used to determine binding thermodynamics of inhibitory compounds (Isothermal titration calorimetry, Fluorescent thermal shift assay/differential scanning fluorimetry and others) will be compared in detail. Also types and chemical synthesis of CA inhibitors, the use of antibodies against CAs as well as inhibitor application in animals are discussed.

In-cell NMR Spectroscopy

Author : Yutaka Ito
Publisher : Royal Society of Chemistry
ISBN 13 : 1839160934
Total Pages : 322 pages
Book Rating : 4.8/5 (391 download)

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Book Synopsis In-cell NMR Spectroscopy by : Yutaka Ito

Download or read book In-cell NMR Spectroscopy written by Yutaka Ito and published by Royal Society of Chemistry. This book was released on 2019-12-09 with total page 322 pages. Available in PDF, EPUB and Kindle. Book excerpt: In-cell NMR spectroscopy is a relatively new field. Despite its short history, recent in-cell NMR-related publications in major journals indicate that this method is receiving significant general attention. This book provides the first informative work specifically focused on in-cell NMR. It details the historical background of in-cell NMR, host cells for in-cell NMR studies, methods for in-cell biological techniques and NMR spectroscopy, applications, and future perspectives. Researchers in biochemistry, biophysics, molecular biology, cell biology, structural biology as well as NMR analysts interested in biological applications will all find this book valuable reading.

Carbonic Anhydrase: Mechanism, Regulation, Links to Disease, and Industrial Applications

Author : Susan C. Frost
Publisher : Springer Science & Business Media
ISBN 13 : 9400773595
Total Pages : 429 pages
Book Rating : 4.4/5 (7 download)

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Book Synopsis Carbonic Anhydrase: Mechanism, Regulation, Links to Disease, and Industrial Applications by : Susan C. Frost

Download or read book Carbonic Anhydrase: Mechanism, Regulation, Links to Disease, and Industrial Applications written by Susan C. Frost and published by Springer Science & Business Media. This book was released on 2013-10-22 with total page 429 pages. Available in PDF, EPUB and Kindle. Book excerpt: The study of carbonic anhydrase has spanned multiple generations of scientists. Carbonic anhydrase was first discovered in 1932 by Meldrum and Roughton. Inhibition by sulfanilamide was shown in 1940 by Mann and Keilin. Even Hans Krebs contributed to early studies with a paper in 1948 showing the relationship of 25 different sulfonamides to CA inhibition. It was he who pointed out the importance of both the charged and uncharged character of these compounds for physiological experiments. The field of study that focuses on carbonic anhydrase (CA) has exploded in recent years with the identification of new families and isoforms. The CAs are metalloenzymes which are comprised of 5 structurally different families: the alpha, beta, gamma, and delta, and epsilon classes. The alpha class is found primarily in animals with several isoforms associated with human disease. The beta CAs are expressed primarily in plants and are the most divergent. The gamma CAs are the most ancient. These are structurally related to the beta CAs, but have a mechanism more similar to the alpha CAs. The delta CAs are found in marine algae and diflagellates. The epsilon class is found in prokaryotes in which it is part of the carboxysome shell perhaps supplying RuBisCO with CO2 for carbon fixation. With the excitement surrounding the discovery of disease-related CAs, scientists have redoubled their efforts to better understand structure-function relationships, to design high affinity, isotype-specific inhibitors, and to delineate signaling systems that play regulatory roles over expression and activity. We have designed the book to cover basic information of mechanism, structure, and function of the CA families. The authors included in this book bring to light the newest data with regard to the role of CA in physiology and pathology, across phylums, and in unique environmental niches.

Carbonic Anhydrases and Metabolism

Author : Claudiu T. Supuran
Publisher : MDPI
ISBN 13 : 3038978000
Total Pages : 184 pages
Book Rating : 4.0/5 (389 download)

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Book Synopsis Carbonic Anhydrases and Metabolism by : Claudiu T. Supuran

Download or read book Carbonic Anhydrases and Metabolism written by Claudiu T. Supuran and published by MDPI. This book was released on 2019-04-08 with total page 184 pages. Available in PDF, EPUB and Kindle. Book excerpt: Carbonic anhydrases (CAs; EC 4.2.1.1) are metalloenzymes present in all kingdoms of life, as they equilibrate the reaction between three simple but essential chemical species: CO2, bicarbonate, and protons. Discovered more than 80 years ago, in 1933, these enzymes have been extensively investigated due to the biomedical application of their inhibitors, but also because they are an extraordinary example of convergent evolution, with seven genetically distinct CA families that evolved independently in Bacteria, Archaea, and Eukarya. CAs are also among the most efficient enzymes known in nature, due to the fact that the uncatalyzed hydration of CO2 is a very slow process and the physiological demands for its conversion to ionic, soluble species is very high. Inhibition of the CAs has pharmacological applications in many fields, such as antiglaucoma, anticonvulsant, antiobesity, and anticancer agents/diagnostic tools, but is also emerging for designing anti-infectives, i.e., antifungal, antibacterial, and antiprotozoan agents with a novel mechanism of action. Mitochondrial CAs are implicated in de novo lipogenesis, and thus selective inhibitors of such enzymes may be useful for the development of new antiobesity drugs. As tumor metabolism is diverse compared to that of normal cells, ultimately, relevant contributions on the role of the tumor-associated isoforms CA IX and XII in these phenomena have been published and the two isoforms have been validated as novel antitumor/antimetastatic drug targets, with antibodies and small-molecule inhibitors in various stages of clinical development. CAs also play a crucial role in other metabolic processes connected with urea biosynthesis, gluconeogenesis, and so on, since many carboxylation reactions catalyzed by acetyl-coenzyme A carboxylase or pyruvate carboxylase use bicarbonate, not CO2, as a substrate. In organisms other than mammals, e.g., plants, algae, and cyanobacteria, CAs are involved in photosynthesis, whereas in many parasites (fungi, protozoa), they are involved in the de novo synthesis of important metabolites (lipids, nucleic acids, etc.). The metabolic effects related to interference with CA activity, however, have been scarcely investigated. The present Special Issue of Metabolites aims to fill this gap by presenting the latest developments in the field of CAs and their role in metabolism.

Drug Design of Zinc-Enzyme Inhibitors

Author : Claudiu T. Supuran
Publisher : John Wiley & Sons
ISBN 13 : 9780470508152
Total Pages : 1040 pages
Book Rating : 4.5/5 (81 download)

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Book Synopsis Drug Design of Zinc-Enzyme Inhibitors by : Claudiu T. Supuran

Download or read book Drug Design of Zinc-Enzyme Inhibitors written by Claudiu T. Supuran and published by John Wiley & Sons. This book was released on 2009-10-22 with total page 1040 pages. Available in PDF, EPUB and Kindle. Book excerpt: Brings together functional and structural informationrelevant to the design of drugs targeting zinc enzymes The second most abundant transition element in living organisms, zinc spans all areas of metabolism, with zinc-containing proteins offering both established and potential drug targets. Drug Design of Zinc-Enzyme Inhibitors brings together functional and structural information relevant to these zinc-containing targets. With up-to-date overviews of the latest developments field, this unique and comprehensive text enables readers to understand zinc enzymes and evaluate them in a drug design context. With contributions from the leaders of today's research, Drug Design of Zinc-Enzyme Inhibitors covers such key topics as: Major drug targets like carbonic anhydrases, matrix metalloproteinases, bacterial proteases, angiotensin-converting enzyme, histone deacetylase, and APOBEC3G Roles of recently discovered zinc-containing isozymes in cancer, obesity, epilepsy, pain management, malaria, and other conditions Cross reactivity of zinc-enzyme inhibitors and activators The extensive use of X-ray crystallography and QSAR studies for understanding zinc-containing proteins Clinical applications An essential resource for the discovery and development of new drug molecules, Drug Design of Zinc-Enzyme Inhibitors gives researchers, professionals, students, and academics the foundation to understand and work with zinc enzyme inhibitors and activators.

Carbonic Anhydrase

Author : Claudiu T. Supuran
Publisher : CRC Press
ISBN 13 : 1134400152
Total Pages : 560 pages
Book Rating : 4.1/5 (344 download)

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Book Synopsis Carbonic Anhydrase by : Claudiu T. Supuran

Download or read book Carbonic Anhydrase written by Claudiu T. Supuran and published by CRC Press. This book was released on 2004-05-27 with total page 560 pages. Available in PDF, EPUB and Kindle. Book excerpt: Carbonic Anhydrase: Its Inhibitors and Activators provides a state-of-the-art overview of the latest developments and challenges in carbonic anhydrase research. Authors describe the mechanisms of action of specific inhibitors in relation to physiological function, and present previously unpublished research on CA activators. Written by a team of in

Carbonic Anhydrases

Author : Claudiu T. Supuran
Publisher : Academic Press
ISBN 13 : 9780128164761
Total Pages : 512 pages
Book Rating : 4.1/5 (647 download)

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Book Synopsis Carbonic Anhydrases by : Claudiu T. Supuran

Download or read book Carbonic Anhydrases written by Claudiu T. Supuran and published by Academic Press. This book was released on 2019-09 with total page 512 pages. Available in PDF, EPUB and Kindle. Book excerpt: Carbonic Anhydrases provides an interdisciplinary review of the burgeoning carbonic anhydrase (CA) research area, spanning from CAs classification (biochemical and structural features) to drug design and pharmacology of CA inhibitors and activators, finally touching on the biotechnological applications of these metalloenzymes. The book adopts a clear step-by-step approach and introduction to this intricate and highly interdisciplinary field. A diverse range of chapters from international experts speak to CA classification and distribution, the mechanisms of action and drug design of inhibitors and activators, the druggability of the various isoforms in the treatment of a multitude of diseases, and threats to human health. Carbonic Anhydrases provides biology, biochemistry, and medicinal chemistry students and researchers a thorough discussion and update on the evergreen and expanding research area of CAs. ● Offers a full overview of CAs' biochemical and structural features, as well as drug design and pharmacology of inhibitors and activators. ● Provides a thorough update on the newly identified isoforms, modulating chemotypes, and innovative biomedical applications. ● Describes the current biotechnological applications of CAs, including processes for CO2 capture. ● Features chapter contributions from international leaders in CA biology, medicinal chemistry, and pharmacology.

Carbonic Anhydrases as Biocatalysts

Author : Claudiu T. Supuran
Publisher : Elsevier
ISBN 13 : 0444632638
Total Pages : 398 pages
Book Rating : 4.4/5 (446 download)

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Book Synopsis Carbonic Anhydrases as Biocatalysts by : Claudiu T. Supuran

Download or read book Carbonic Anhydrases as Biocatalysts written by Claudiu T. Supuran and published by Elsevier. This book was released on 2015-01-14 with total page 398 pages. Available in PDF, EPUB and Kindle. Book excerpt: Carbonic anhydrases (CAs, EC 4.2.1.1) are ubiquitous metalloenzymes, present throughout most living organisms and encoded by five evolutionarily unrelated gene families. The Carbonic Anhydrases as Biocatalysts: From Theory to Medical and Industrial Applications presents information on the growing interest in the study of this enzyme family and their applications to both medicine and biotechnology. - Offers comprehensive coverage of the carbonic anhydrases enzyme family and their properties as biocatalysts - Includes current applications of carbonic anhydrases in biotechnology on the basis of their catalytic efficiency, including new technologies for CO2 capture processes - Identifies new targets for drug design studies - Provides a selectivity profile for the different carbonic anhydrases and their related biomedical applications

The Carbonic Anhydrases: Current and Emerging Therapeutic Targets

Author : W. Richard Chegwidden
Publisher :
ISBN 13 : 9783030795122
Total Pages : 0 pages
Book Rating : 4.7/5 (951 download)

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Book Synopsis The Carbonic Anhydrases: Current and Emerging Therapeutic Targets by : W. Richard Chegwidden

Download or read book The Carbonic Anhydrases: Current and Emerging Therapeutic Targets written by W. Richard Chegwidden and published by . This book was released on 2021 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt: This volume assembles and integrates the wealth of diverse information that is now accumulating in this burgeoning field. The existing and potential therapeutic applications of targeting CA cover a remarkably wide-range of diseases and disorders and have generated increasing and extensive interest in recent years. Its inter-disciplinary approach embraces both the most up-to-date therapeutic application of CA-targeting and the latest research data that will provide a platform for the development of novel applications. The interested audience comprises scientists and clinicians from many relevant disciplines within science and medicine.

Structure-based Design of Drugs and Other Bioactive Molecules

Author : Arun K. Ghosh
Publisher : John Wiley & Sons
ISBN 13 : 3527333657
Total Pages : 474 pages
Book Rating : 4.5/5 (273 download)

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Book Synopsis Structure-based Design of Drugs and Other Bioactive Molecules by : Arun K. Ghosh

Download or read book Structure-based Design of Drugs and Other Bioactive Molecules written by Arun K. Ghosh and published by John Wiley & Sons. This book was released on 2014-08-11 with total page 474 pages. Available in PDF, EPUB and Kindle. Book excerpt: Drug design is a complex, challenging and innovative research area. Structure-based molecular design has transformed the drug discovery approach in modern medicine. Traditionally, focus has been placed on computational, structural or synthetic methods only in isolation. This one-of-akind guide integrates all three skill sets for a complete picture of contemporary structure-based design. This practical approach provides the tools to develop a high-affinity ligand with drug-like properties for a given drug target for which a high-resolution structure exists. The authors use numerous examples of recently developed drugs to present "best practice" methods in structurebased drug design with both newcomers and practicing researchers in mind. By way of a carefully balanced mix of theoretical background and case studies from medicinal chemistry applications, readers will quickly and efficiently master the basic skills of successful drug design. This book is aimed at new and active medicinal chemists, biochemists, pharmacologists, natural product chemists and those working in drug discovery in the pharmaceutical industry. It is highly recommended as a desk reference to guide students in medicinal and chemical sciences as well as to aid researchers engaged in drug design today.

Structural Biology in Drug Discovery

Author : Jean-Paul Renaud
Publisher : John Wiley & Sons
ISBN 13 : 1118900502
Total Pages : 1437 pages
Book Rating : 4.1/5 (189 download)

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Book Synopsis Structural Biology in Drug Discovery by : Jean-Paul Renaud

Download or read book Structural Biology in Drug Discovery written by Jean-Paul Renaud and published by John Wiley & Sons. This book was released on 2020-01-09 with total page 1437 pages. Available in PDF, EPUB and Kindle. Book excerpt: With the most comprehensive and up-to-date overview of structure-based drug discovery covering both experimental and computational approaches, Structural Biology in Drug Discovery: Methods, Techniques, and Practices describes principles, methods, applications, and emerging paradigms of structural biology as a tool for more efficient drug development. Coverage includes successful examples, academic and industry insights, novel concepts, and advances in a rapidly evolving field. The combined chapters, by authors writing from the frontlines of structural biology and drug discovery, give readers a valuable reference and resource that: Presents the benefits, limitations, and potentiality of major techniques in the field such as X-ray crystallography, NMR, neutron crystallography, cryo-EM, mass spectrometry and other biophysical techniques, and computational structural biology Includes detailed chapters on druggability, allostery, complementary use of thermodynamic and kinetic information, and powerful approaches such as structural chemogenomics and fragment-based drug design Emphasizes the need for the in-depth biophysical characterization of protein targets as well as of therapeutic proteins, and for a thorough quality assessment of experimental structures Illustrates advances in the field of established therapeutic targets like kinases, serine proteinases, GPCRs, and epigenetic proteins, and of more challenging ones like protein-protein interactions and intrinsically disordered proteins

Biophysical Approaches Determining Ligand Binding to Biomolecular Targets

Author : Alberto Podjarny
Publisher : Royal Society of Chemistry
ISBN 13 : 1849732663
Total Pages : 373 pages
Book Rating : 4.8/5 (497 download)

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Book Synopsis Biophysical Approaches Determining Ligand Binding to Biomolecular Targets by : Alberto Podjarny

Download or read book Biophysical Approaches Determining Ligand Binding to Biomolecular Targets written by Alberto Podjarny and published by Royal Society of Chemistry. This book was released on 2011-04-01 with total page 373 pages. Available in PDF, EPUB and Kindle. Book excerpt: The binding of small ligands to biological molecules is central to most aspects of biological function. The past twenty years has seen the development of an increasing armoury of biophysical methods that not only detect such binding, but also provide varying degrees of information about the kinetics, thermodynamics and structural aspects of the process. These methods have received increasing attention with the growth in more rational approaches to drug discovery and design. This book reviews the latest advances in the application of biophysics to the study of ligand binding. It provides a complete overview of current techniques to identify ligands, characterise their binding sites and understand their binding mechanisms. Particular emphasis is given to the combined use of different techniques and their relative strengths and weaknesses. Consistency in the way each technique is described makes it easy for readers to select the most suitable protocol for their research. The introduction explains why some techniques are more suitable than others and emphasizes the possible synergies between them. The following chapters, all written by a specialist in the particular technique, focus on each method individually. The book finishes by describing how several complimentary techniques can be used together for maximum effectiveness. This book is suitable for biomolecular scientists at graduate or post-doctoral level in academia and industry. Biologists and chemists will also find it a useful introduction to the techniques available.

Thermodynamics and Kinetics of Drug Binding

Author : György Keserü
Publisher : John Wiley & Sons
ISBN 13 : 352733582X
Total Pages : 360 pages
Book Rating : 4.5/5 (273 download)

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Book Synopsis Thermodynamics and Kinetics of Drug Binding by : György Keserü

Download or read book Thermodynamics and Kinetics of Drug Binding written by György Keserü and published by John Wiley & Sons. This book was released on 2015-08-17 with total page 360 pages. Available in PDF, EPUB and Kindle. Book excerpt: This practical reference for medicinal and pharmaceutical chemists combines the theoretical background with modern methods as well as applications from recent lead finding and optimization projects. Divided into two parts on the thermodynamics and kinetics of drug-receptor interaction, the text provides the conceptual and methodological basis for characterizing binding mechanisms for drugs and other bioactive molecules. It covers all currently used methods, from experimental approaches, such as ITC or SPR, right up to the latest computational methods. Case studies of real-life lead or drug development projects are also included so readers can apply the methods learned to their own projects. Finally, the benefits of a thorough binding mode analysis for any drug development project are summarized in an outlook chapter written by the editors.

The Carbonic Anhydrases

Author : W.R. Chegwidden
Publisher : Birkhäuser
ISBN 13 : 303488446X
Total Pages : 614 pages
Book Rating : 4.0/5 (348 download)

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Book Synopsis The Carbonic Anhydrases by : W.R. Chegwidden

Download or read book The Carbonic Anhydrases written by W.R. Chegwidden and published by Birkhäuser. This book was released on 2013-11-11 with total page 614 pages. Available in PDF, EPUB and Kindle. Book excerpt: Carbonic anhydrase (CA) is a seemingly ubiquitous enzyme of profound physiological importance, which plays essential roles in respiration, acid-base homeostasis, bone resorption, calcification, photosynthesis, several biosynthetic pathways and a variety of processes involving ion, gas and fluid transfer. This enzyme, which is present in at least three gene families (a, ß, ?), has found favour as a model for the study of evolution of gene families and for site-directed mutagenesis in structure/function relationships, for protein folding and for transgenic and gene target studies. Since the early use of CA inhibitors as diuretics and in treating congestive heart failure, the enzyme has been target of considerable clinical attention. Much of this is now focused on endeavours to produce a new generation of such drugs for the effective treatment of glaucoma and other potential applications. Recent data, suggesting links between CA and various disease processes, including cancer, have stimulated further...

Protein-Ligand Interactions

Author : Hans-Joachim Böhm
Publisher : John Wiley & Sons
ISBN 13 : 3527605517
Total Pages : 262 pages
Book Rating : 4.5/5 (276 download)

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Book Synopsis Protein-Ligand Interactions by : Hans-Joachim Böhm

Download or read book Protein-Ligand Interactions written by Hans-Joachim Böhm and published by John Wiley & Sons. This book was released on 2006-03-06 with total page 262 pages. Available in PDF, EPUB and Kindle. Book excerpt: The lock-and-key principle formulated by Emil Fischer as early as the end of the 19th century has still not lost any of its significance for the life sciences. The basic aspects of ligand-protein interaction may be summarized under the term 'molecular recognition' and concern the specificity as well as stability of ligand binding. Molecular recognition is thus a central topic in the development of active substances, since stability and specificity determine whether a substance can be used as a drug. Nowadays, computer-aided prediction and intelligent molecular design make a large contribution to the constant search for, e. g., improved enzyme inhibitors, and new concepts such as that of pharmacophores are being developed. An up-to-date presentation of an eternally young topic, this book is an indispensable information source for chemists, biochemists and pharmacologists dealing with the binding of ligands to proteins.

Drug Selectivity

Author : Norbert Handler
Publisher : John Wiley & Sons
ISBN 13 : 3527335382
Total Pages : 538 pages
Book Rating : 4.5/5 (273 download)

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Book Synopsis Drug Selectivity by : Norbert Handler

Download or read book Drug Selectivity written by Norbert Handler and published by John Wiley & Sons. This book was released on 2018-02-27 with total page 538 pages. Available in PDF, EPUB and Kindle. Book excerpt: The book "Drug Selectivity - An Evolving Concept in Medicinal Chemistry" provides a current overview and comprehensive compilation for medicinal chemists that discusses the effects of aiming for multiple targets on the entire drug development process. The result is a broad survey of current and future strategies for drug selectivity in medicinal chemistry with theoretical but also practical aspects. Different strategies are presented and evaluated, such as various design approaches, merged multiple ligands, discovery technologies and a broad range of successful examples of unselective drugs taken from all major disease areas. With its wide-ranging view of an emerging new paradigm in drug development, this handbook is of prime importance for every medicinal and pharmaceutical chemist.

Protein Crystallography in Drug Discovery, Volume 20

Author : Robert E. Babine
Publisher : John Wiley & Sons
ISBN 13 : 9783527306787
Total Pages : 284 pages
Book Rating : 4.3/5 (67 download)

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Book Synopsis Protein Crystallography in Drug Discovery, Volume 20 by : Robert E. Babine

Download or read book Protein Crystallography in Drug Discovery, Volume 20 written by Robert E. Babine and published by John Wiley & Sons. This book was released on 2004-02-13 with total page 284 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.