Optimization in Drug Discovery, Gary W. Caldwell; Zhengyin Yan

Автор: Gary W. Caldwell; Zhengyin Yan
Название: Optimization in Drug Discovery
ISBN: 1627037411 ISBN-13(EAN): 9781627037419
Издательство: Springer
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Цена: 130430.00 T
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Описание: This fresh edition features new assay variations and the latest protocols for optimizing drug discovery. With expert tips and troubleshooting advice, and revised throughout for this second edition, it covers cutting-edge techniques such as cytochrome P450.

Автор: Bernard Testa
Название: Pharmacokinetic Optimization in Drug Research: Biological, Physicochemical, and Computational Strategies
ISBN: 3906390225 ISBN-13(EAN): 9783906390222
Издательство: Wiley
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Цена: 153120.00 T
Наличие на складе: Невозможна поставка.
Описание: In this age of combinatorial chemistry and high-throughput technologies, bioactive compounds called hits are discovered by the thousands. However, the road that leads from hits to lead compounds and then to pharmacokinetically optimized clinical and drug candidates is very long indeed. As a result, the screening, design, and optimization of pharmacokinetic properties has become the bottleneck and a major challenge in drug research. To shorten the time-consuming develop-ment and high rate of attrition of active compounds ultimately doomed by hidden pharmacokinetic defects, drug researchers are coming to incorporate structure-permeation, structure-distribution, structure-metabolism, and structure-toxicity relations into drug-design strategies. To this end, powerful biological, physicochemical, and computational approaches are being developed whose objectives are to increase the clinical relevance of drug design, and to eliminate as soon as possible compounds with unfavorable physicochemical properties and pharmacokinetic profiles. Toxicological issues are also of utmost importance in this paradigm. There was, hence, an urgent need for a book covering this field in an authoritative, didactic, comprehensive, factual, and conceptual manner. In this work of unique breadth and depth, international authorities and practicing experts from academia and industry present the most modern biological, physicochemical, and computational strategies to optimize gastrointestinal absorption, protein binding and distribution, brain permeation, and metabolic profile. The biological strategies emphasized in the book include cell cultures and high-throughput screens. The physicochemical strategies focus on the determination and interpretation of solubility, lipophilicity, and related molecular properties as factors and predictors of pharmacokinetic bahavior. Particular attention is paid to the lipophilicity profiles of ionized compounds, to lipophicity measurements in anisotropic media (liposomes/water, IAM columns), and to permeability across artificial membranes. Computational strategies comprise virtual screening, molecular modelling, lipophilicity, and H-bonding fields and their importance for structure-disposition relations. This book is both about theoretical and technological breakthroughs. Thus, molecular properties are contemplated from a dual perspective, namely a) their interpretation in biological and/or physicochemical terms, and b) their value in screening, lead optimization, and drug-candidate selection. In addition to its 33 chapters, the book includes a CD-ROM containing the invited lectures, oral communications and posters (in full version) presented at the Second LogP Symposium, 'Lipophilicity in Drug Disposition -- Practical and Computational Approaches to Molecular Properties Related to Drug Permeation, Disposition and Metabolism', held at the University of Lausanne in March 2000.

Автор: Anthony E. Klon
Название: Fragment-Based Methods in Drug Discovery
ISBN: 1493924850 ISBN-13(EAN): 9781493924851
Издательство: Springer
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Цена: 130430.00 T
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Описание: This volume covers the techniques necessary for a successful fragment-based drug design project, beginning from defining the problem in terms of preparing the protein model, identifying potential binding sites, and the consideration of various candidate fragments for simulation.

Автор: Haiyong Han; Paul Grippo
Название: Drug Discovery in Pancreatic Cancer
ISBN: 1489982752 ISBN-13(EAN): 9781489982759
Издательство: Springer
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Цена: 174130.00 T
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Описание: There have been tremendous advances in cancer drug discovery, and in the area of molecular and genetic models and technologies. In this book, experts describe the latest developments in the application of these models and technologies in pancreatic cancer.

Автор: David Borsook; Lino R. Beccera; Edward Bullmore; R
Название: Imaging in CNS Drug Discovery and Development
ISBN: 1489984747 ISBN-13(EAN): 9781489984746
Издательство: Springer
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Цена: 174130.00 T
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Описание: Distilling the most salient developments in the use of imaging in drug development and disease mapping, this text integrates new imaging technologies and paradigms with molecular medicine and molecular profiling, and considers the relevant ethical issues.

Автор: Alexander Heifetz
Название: Computational Methods for GPCR Drug Discovery
ISBN: 1493974645 ISBN-13(EAN): 9781493974641
Издательство: Springer
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Цена: 139750.00 T
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Описание: This volume looks at modern computational strategies and techniques used in GPCR drug discovery including structure and ligand-based approaches and cheminformatics.

Автор: Frank E. Koehn
Название: Natural Products and Cancer Drug Discovery
ISBN: 148999565X ISBN-13(EAN): 9781489995650
Издательство: Springer
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Цена: 148010.00 T
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Описание: With reliable commentary and analysis in a sector often associated with outlandish claims, this volume provides a valuable overview of how natural products could generate new cancer therapeutics as well as mitigating the deleterious effects of chemotherapy.

Автор: Jurgen Moll; Riccardo Colombo
Название: Target Identification and Validation in Drug Discovery
ISBN: 1493962787 ISBN-13(EAN): 9781493962785
Издательство: Springer
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Цена: 121110.00 T
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Описание: The major reason for the elevated costs of drug development in the pharmaceutical industry is the high attrition rate. In Target Identification and Validation in Drug Discovery: Methods and Protocols, expert researchers in the field detail many of the methods which are now commonly used to identify and validate new target. These include methods and approaches covering biochemical, cell based, in vivo models and translational methods. Chapters also include selected case reports that demonstrate the integration of these technologies to real life experiences and to demonstrate the multiple use of more than one technology to increase knowledge on a specific target. These Written in the highly successful Methods in Molecular Biology™ series format, the chapters include the kind of detailed description and implementation advice that is crucial for getting optimal results in the laboratory. Thorough and intuitive, Target Identification and Validation in Drug Discovery: Methods and Protocols contains a comprehensive list of essential methods and clear protocols to follow.

Автор: Ye Fang
Название: Label-Free Biosensor Methods in Drug Discovery
ISBN: 1493926160 ISBN-13(EAN): 9781493926169
Издательство: Springer
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Цена: 139750.00 T
Наличие на складе: Есть у поставщика Поставка под заказ.