The Design Of Synthetic Inhibitors Of Thrombin

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The Design of Synthetic Inhibitors of Thrombin

Author : Goran Claeson
Publisher : Springer Science & Business Media
ISBN 13 : 1489924183
Total Pages : 245 pages
Book Rating : 4.4/5 (899 download)

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Book Synopsis The Design of Synthetic Inhibitors of Thrombin by : Goran Claeson

Download or read book The Design of Synthetic Inhibitors of Thrombin written by Goran Claeson and published by Springer Science & Business Media. This book was released on 2013-06-29 with total page 245 pages. Available in PDF, EPUB and Kindle. Book excerpt: In one generation, the numerous factors involved in blood coagulation have become real protein entities, isolated in pure form, expressed by recombinant DNA techniques, and subjected to structure elucidation by the modem methods of physical chemistry, viz. , X-ray diffraction, and NMR, ESR and fluorescence spectroscopy. The major milestone in this field was the breakthrough achieved by W. Bode, R. Huber and their colleagues in 1989 in of human a-thrombin, inhibited with D-Phe-Pro-Arg determining the crystal structure chioromethyl ketone. The availability of this structure will greatly facilitate the interpretation of experiments designed to gain an understanding of the interatomic interactions between this enzyme and fibrinogen and its other substrates. At the same time, it provides a rational basis for the design and synthesis of inhibitors of thrombin, the subject of this symposium. The symposium was organized in four sessions: (1) Structural features of the interaction of thrombin with substrates and inhibitors, (2) Synthetic inhibitors, (3) Hirudin and its analogues, and (4) Pharmacological and clinical considerations. This book contains summaries of most of the papers presented, and takes its rigbful place among two others that provide a comprehensive picture of our current knowledge about thrombin, viz. the 1977 volume entitled "Chemistry and Biology of Thrombin", edited by R. L. Lundblad, J. W. Fenton II, and K. G. Mann, and the 1992 volume entitled "Thrombin: Structure and Function", edited by L. J. Berliner.

Smith and Williams' Introduction to the Principles of Drug Design and Action, Third Edition

Author : H. John Smith
Publisher : CRC Press
ISBN 13 : 9789057020377
Total Pages : 578 pages
Book Rating : 4.0/5 (23 download)

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Book Synopsis Smith and Williams' Introduction to the Principles of Drug Design and Action, Third Edition by : H. John Smith

Download or read book Smith and Williams' Introduction to the Principles of Drug Design and Action, Third Edition written by H. John Smith and published by CRC Press. This book was released on 1998-05-15 with total page 578 pages. Available in PDF, EPUB and Kindle. Book excerpt: The third edition of this popular textbook builds on the excellent foundations laid down by the earlier editions. It provides a thorough introduction to the principles of rational drug design, adopting a 'from the bench to the market place' approach. As knowledge of biological systems has expanded and the number of techniques available for exploring and visualizing their components has increased, it has become possible to design drugs specifically for a given target. This unique insight has revolutionized the process of drug development for specific disease states, and in this textbook both novel and established approaches are incorporated. The introductory text explains the principles of drug design using real examples. These illustrate the discovery of 'lead' compounds and their manipulation to produce non-toxic drug candidates that will be successfully metabolized to interact with target receptors in a predicted fashion. In addition to fully updating the contents of the previous edition, the Editor has included important new sections on the pharmacological consequences of drug chirality, agonists and antagonists of neurotransmitters, and the process involved in proceeding from program sanction to clinical trials

Smith and Williams' Introduction to the Principles of Drug Design and Action

Author : H. John Smith
Publisher : CRC Press
ISBN 13 : 1135299757
Total Pages : 863 pages
Book Rating : 4.1/5 (352 download)

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Book Synopsis Smith and Williams' Introduction to the Principles of Drug Design and Action by : H. John Smith

Download or read book Smith and Williams' Introduction to the Principles of Drug Design and Action written by H. John Smith and published by CRC Press. This book was released on 2005-10-10 with total page 863 pages. Available in PDF, EPUB and Kindle. Book excerpt: Advances in knowledge and technology have revolutionized the process of drug development, making it possible to design drugs for a given target or disease. Building on the foundation laid by the previous three editions, Smith and Williams Introduction to the Principles of Drug Design and Action, Fourth Edition includes the latest informatio

Integration of Pharmaceutical Discovery and Development

Author : Ronald T. Borchardt
Publisher : Springer Science & Business Media
ISBN 13 : 0306473844
Total Pages : 627 pages
Book Rating : 4.3/5 (64 download)

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Book Synopsis Integration of Pharmaceutical Discovery and Development by : Ronald T. Borchardt

Download or read book Integration of Pharmaceutical Discovery and Development written by Ronald T. Borchardt and published by Springer Science & Business Media. This book was released on 2006-01-19 with total page 627 pages. Available in PDF, EPUB and Kindle. Book excerpt: In the late 1980s, it became painfully evident to the pharmaceutical industry that the old paradigm of drug discovery, which involved highly segmented drug - sign and development activities, would not produce an acceptable success rate in the future. Therefore, in the early 1990s a paradigm shift occurred in which drug design and development activities became more highly integrated. This new str- egy required medicinal chemists to design drug candidates with structural f- tures that optimized pharmacological (e. g. , high affinity and specificity for the target receptor), pharmaceutical (e. g. , solubility and chemical stability), bioph- maceutical (e. g. , cell membrane permeability), and metabolic/pharmacokinetic (e. g. , metabolic stability, clearance, and protein binding) properties. Successful implementation of this strategy requires a multidisciplinary team effort, incl- ing scientists from drug design (e. g. , medicinal chemists, cell biologists, en- mologists, pharmacologists) and drug development (e. g. , analytical chemists, pharmaceutical scientists, physiologists, and molecular biologists representing the disciplines of pharmaceutics, biopharmaceutics, and pharmacokinetics/drug metabolism). With this new, highly integrated approach to drug design now widely utilized by the pharmaceutical industry, the editors of this book have provided the sci- tific community with case histories to illustrate the nature of the interdisciplinary interactions necessary to successfully implement this new approach to drug d- covery. In the first chapter, Ralph Hirschmann provides a historical perspective of why this paradigm shift in drug discovery has occurred.

Structure-Based Drug Design

Author : Pandi Veerapandian
Publisher : Routledge
ISBN 13 : 1351413058
Total Pages : 527 pages
Book Rating : 4.3/5 (514 download)

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Book Synopsis Structure-Based Drug Design by : Pandi Veerapandian

Download or read book Structure-Based Drug Design written by Pandi Veerapandian and published by Routledge. This book was released on 2018-03-29 with total page 527 pages. Available in PDF, EPUB and Kindle. Book excerpt: Introducing the most recent advances in crystallography, nuclear magnetic resonance, molecular modeling techniques, and computational combinatorial chemistry, this unique, interdisciplinary reference explains the application of three-dimensional structural information in the design of pharmaceutical drugs. Furnishing authoritative analyses by world-renowned experts, Structure-Based Drug Design discusses protein structure-based design in optimizing HIV protease inhibitors and details the biochemical, genetic, and clinical data on HIV-1 reverse transcriptase presents recent results on the high-resolution three-dimensional structure of the catalytic core domain of HIV-1 integrase as a foundation for divergent combination therapy focuses on structure-based design strategies for uncovering receptor antagonists to treat inflammatory diseases demonstrates a systematic approach to the design of inhibitory compounds in cancer treatment reviews current knowledge on the Interleukin-1 (IL-1) system and progress in the development of IL-1 modulators describes the influence of structure-based methods in designing capsid-binding inhibitors for relief of the common cold and much more!

Current Pharmaceutical Design

Author :
Publisher :
ISBN 13 :
Total Pages : 206 pages
Book Rating : 4./5 ( download)

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Book Synopsis Current Pharmaceutical Design by :

Download or read book Current Pharmaceutical Design written by and published by . This book was released on 1995-12 with total page 206 pages. Available in PDF, EPUB and Kindle. Book excerpt:

Proteinase and Peptidase Inhibition

Author : H. John Smith
Publisher : CRC Press
ISBN 13 : 0203219171
Total Pages : 440 pages
Book Rating : 4.2/5 (32 download)

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Book Synopsis Proteinase and Peptidase Inhibition by : H. John Smith

Download or read book Proteinase and Peptidase Inhibition written by H. John Smith and published by CRC Press. This book was released on 2002-03-28 with total page 440 pages. Available in PDF, EPUB and Kindle. Book excerpt: Cellular proteinases and their physiological role in normal and disease states have been the subject of great interest over recent decades. At present, specific protease inhibitors are exploited both as tools in unraveling the role of individual proteinases in particular cellular processes and for the development of chemotherapeutic agents for the

Cumulated Index Medicus

Author :
Publisher :
ISBN 13 :
Total Pages : 1836 pages
Book Rating : 4.3/5 (243 download)

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Book Synopsis Cumulated Index Medicus by :

Download or read book Cumulated Index Medicus written by and published by . This book was released on 2000 with total page 1836 pages. Available in PDF, EPUB and Kindle. Book excerpt:

Anesthetic Pharmacology

Author : Alex S. Evers
Publisher : Cambridge University Press
ISBN 13 : 1139497022
Total Pages : 2902 pages
Book Rating : 4.1/5 (394 download)

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Book Synopsis Anesthetic Pharmacology by : Alex S. Evers

Download or read book Anesthetic Pharmacology written by Alex S. Evers and published by Cambridge University Press. This book was released on 2011-03-10 with total page 2902 pages. Available in PDF, EPUB and Kindle. Book excerpt: In recent years our understanding of molecular mechanisms of drug action and interindividual variability in drug response has grown enormously. Meanwhile, the practice of anesthesiology has expanded to the preoperative environment and numerous locations outside the OR. Anesthetic Pharmacology: Basic Principles and Clinical Practice, 2nd edition, is an outstanding therapeutic resource in anesthesia and critical care: Section 1 introduces the principles of drug action, Section 2 presents the molecular, cellular and integrated physiology of the target organ/functional system and Section 3 reviews the pharmacology and toxicology of anesthetic drugs. The new Section 4, Therapeutics of Clinical Practice, provides integrated and comparative pharmacology and the practical application of drugs in daily clinical practice. Edited by three highly acclaimed academic anesthetic pharmacologists, with contributions from an international team of experts, and illustrated in full colour, this is a sophisticated, user-friendly resource for all practitioners providing care in the perioperative period.

Current Pharmaceutical Design

Author :
Publisher :
ISBN 13 :
Total Pages : 206 pages
Book Rating : 4./5 ( download)

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Book Synopsis Current Pharmaceutical Design by :

Download or read book Current Pharmaceutical Design written by and published by . This book was released on 1995-12 with total page 206 pages. Available in PDF, EPUB and Kindle. Book excerpt:

The Chemical Biology of Thrombin

Author : Roger L. Lundblad
Publisher : CRC Press
ISBN 13 : 1351677721
Total Pages : 308 pages
Book Rating : 4.3/5 (516 download)

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Book Synopsis The Chemical Biology of Thrombin by : Roger L. Lundblad

Download or read book The Chemical Biology of Thrombin written by Roger L. Lundblad and published by CRC Press. This book was released on 2022-05-01 with total page 308 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book is a comprehensive review of thrombin, especially as regulatory protease. The ready availability of highly purified thrombin has stimulated rapid advances in the cell biology of this important macromolecule. The text focuses on research findings from the discovery of thrombin by Andrew Buchanan in 1842 to the present. A substantial amount of this work was conducted by the author and his colleagues. His work on the purification of thrombin was seminal to much subsequent work on thrombin. This volume provides a framework for future studies now made possible by the discovery of the importance of exosites in the physiology of thrombin function. The current work describes the process of the development of an oral inhibitor of thrombin used in the prevention of thrombosis. Key Features Reviews the history of Thrombin (Fibrin Ferment) Documents the relation of protein engineering and chemical modification in the study of thrombin Summarizes the interaction of thrombin with fibrinogen and fibrin Outlines the role of exosites in thrombin function Describes the development of an oral inhibitor for thrombin

Natural Products in Medicinal Chemistry

Author : Stephen Hanessian
Publisher : John Wiley & Sons
ISBN 13 : 3527676554
Total Pages : 652 pages
Book Rating : 4.5/5 (276 download)

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Book Synopsis Natural Products in Medicinal Chemistry by : Stephen Hanessian

Download or read book Natural Products in Medicinal Chemistry written by Stephen Hanessian and published by John Wiley & Sons. This book was released on 2013-12-18 with total page 652 pages. Available in PDF, EPUB and Kindle. Book excerpt: The inspiration provided by biologically active natural products to conceive of hybrids, congeners, analogs and unnatural variants is discussed by experts in the field in 16 highly informative chapters. Using well-documented studies over the past decade, this timely monograph demonstrates the current importance and future potential of natural products as starting points for the development of new drugs with improved properties over their progenitors. The examples are chosen so as to represent a wide range of natural products with therapeutic relevance among others, as anticancer agents, antimicrobials, antifungals, antisense nucleosides, antidiabetics, and analgesics. From the content: * Part I: Natural Products as Sources of Potential Drugs and Systematic Compound Collections * Part II: From Marketed Drugs to Designed Analogs and Clinical Candidates * Part III: Natural Products as an Incentive for Enabling Technologies * Part IV: Natural Products as Pharmacological Tools * Part V: Nature: The Provider, the Enticer, and the Healer

Current Pharmaceutical Design

Author :
Publisher :
ISBN 13 :
Total Pages : 206 pages
Book Rating : 4./5 ( download)

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Book Synopsis Current Pharmaceutical Design by :

Download or read book Current Pharmaceutical Design written by and published by . This book was released on 1995-12 with total page 206 pages. Available in PDF, EPUB and Kindle. Book excerpt:

Structural Biology in Drug Discovery

Author : Jean-Paul Renaud
Publisher : John Wiley & Sons
ISBN 13 : 1118900405
Total Pages : 688 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 2020-01-27 with total page 688 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

Drug Discovery

Author : Jie Jack Li
Publisher : John Wiley & Sons
ISBN 13 : 111835446X
Total Pages : 572 pages
Book Rating : 4.1/5 (183 download)

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Book Synopsis Drug Discovery by : Jie Jack Li

Download or read book Drug Discovery written by Jie Jack Li and published by John Wiley & Sons. This book was released on 2013-04-03 with total page 572 pages. Available in PDF, EPUB and Kindle. Book excerpt: Sets forth the history, state of the science, and future directions of drug discovery Edited by Jie Jack Li and Nobel laureate E. J. Corey, two leading pioneers in drug discovery and medicinal chemistry, this book synthesizes great moments in history, the current state of the science, and future directions of drug discovery into one expertly written and organized work. Exploring all major therapeutic areas, the book introduces readers to all facets and phases of drug discovery, including target selection, biological testing, drug metabolism, and computer-assisted drug design. Drug Discovery features chapters written by an international team of pharmaceutical and medicinal chemists. Contributions are based on a thorough review of the current literature as well as the authors' firsthand laboratory experience in drug discovery. The book begins with the history of drug discovery, describing groundbreaking moments in the field. Next, it covers such topics as: Target identification and validation Drug metabolism and pharmacokinetics Central nervous system drugs In vitro and in vivo assays Cardiovascular drugs Cancer drugs Each chapter features a case study, helping readers understand how science is put into practice throughout all phases of drug discovery. References at the end of each chapter serve as a gateway to groundbreaking original research studies and reviews in the field. Drug Discovery is ideal for newcomers to medicinal chemistry and drug discovery, providing a comprehensive overview of the field. Veterans in the field will also benefit from the perspectives of leading international experts in all aspects of drug discovery.

Anticoagulant Drugs

Author : Mojca Božič-Mijovski
Publisher : BoD – Books on Demand
ISBN 13 : 1789236223
Total Pages : 122 pages
Book Rating : 4.7/5 (892 download)

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Book Synopsis Anticoagulant Drugs by : Mojca Božič-Mijovski

Download or read book Anticoagulant Drugs written by Mojca Božič-Mijovski and published by BoD – Books on Demand. This book was released on 2018-08-29 with total page 122 pages. Available in PDF, EPUB and Kindle. Book excerpt: Anticoagulant drugs are among the most frequently prescribed drugs in everyday clinical practice. In the past decades, several new direct oral anticoagulants were developed that changed the anticoagulant therapy landscape considerably. This book provides an extensive overview of all the known anticoagulants that can be useful for studying different aspects of the haemostatic system or as a starting point for new drug development. It is also a valuable tool for clinicians providing a description of the mode of action and management of therapy for anticoagulant drugs used in everyday clinical practice in different clinical settings, including direct oral anticoagulants dabigatran, rivaroxaban, apixaban and edoxaban.

The Practice of Medicinal Chemistry

Author : Camille Georges Wermuth
Publisher : Elsevier
ISBN 13 : 0080497772
Total Pages : 792 pages
Book Rating : 4.0/5 (84 download)

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Book Synopsis The Practice of Medicinal Chemistry by : Camille Georges Wermuth

Download or read book The Practice of Medicinal Chemistry written by Camille Georges Wermuth and published by Elsevier. This book was released on 2003-06-11 with total page 792 pages. Available in PDF, EPUB and Kindle. Book excerpt: The Practice of Medicinal Chemistry, 2E, is a single-volume source on the practical aspects of medicinal chemistry. The successful first edition was nicknamed "The Bible" by medicinal chemists, and the second edition has been updated, expanded and refocused to reflect developments over the last decade. Emphasis is put on how medicinal chemists conduct their search for and design of new drug entities. In contrast to competing books, it focuses on the chemistry rather than pharmacological concepts or descriptions of the various therapeutic classes of drugs. Most medicinal chemists working in the pharmaceutical industry are organic synthetic chemists who must acquire a strong knowledge of medicinal chemistry as they enter the industry. This book aims to be their practical handbook - a complete guide to the drug discovery process. The only book available dealing with the practical aspects of medicinal chemistry Serves as a complete guide to the drug discovery process, from conception of the molecules to drug production Updated chapters devoted to the discovery of new lead compounds, including combinatorial chemistry