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Proteinases as Drug Targets

Author: Ben Dunn

Publisher: Royal Society of Chemistry

Published: 2011-11-22

Total Pages: 292

ISBN-13: 1849733155

This book provides vital information on a class of enzymes that have emerged as key drug targets in a number of human diseases, including HIV/AIDS, Hypertension, Cancer, and Alzheimer's disease. There is a gap in information due to the lack of recent international meetings on this subject and, thus, no recent summaries of current research have emerged. The book contains up-to-date information, especially with the genomics revolution of recent years, and includes new proteomics techniques. The story of this enzyme family also includes the most significant efforts in computer-aided drug discovery and structure-based drug design. With contributions from experts in the field, the book is edited by the previous President of the International Proteolysis Society, whose academic career in the field has spanned 35 years.

Proteinase and Peptidase Inhibition

Author: H. John Smith

Publisher: CRC Press

Published: 2002-03-28

Total Pages: 440

ISBN-13: 0203219171

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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

Structural Biology in Drug Discovery

Author: Jean-Paul Renaud

Publisher: John Wiley & Sons

Published: 2020-01-09

Total Pages: 1367

ISBN-13: 1118900502

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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

Burger's Medicinal Chemistry, Drug Discovery and Development

Author: Donald J. Abraham

Publisher:

Published: 2021

Total Pages:

ISBN-13: 9781119821519

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"Burger's is a flagship reference source for medicinal chemists and pharmaceutical professionals. This updated and expanded 8th edition has been thoroughly revised and improved to incorporate the concepts of drug hunting along with its existing coverage of the entire process of drug discovery and development. Bringing in a new and expert editorial board, this new edition updates existing chapters and adds 35 new ones, with topics including: opioid addiction treatments, antibody and gene therapy for cancer, blood-brain barrier, HIV treatments, and industrial-academic collaboration structures"--

Proteases As Drug Targets

Author: Joseph P. Vacca

Publisher: Wiley-VCH

Published: 2010-06-29

Total Pages: 380

ISBN-13: 9783527318124

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Part of a suite of three similarly organized books on proteases, the family of serine proteases is described from a drug developer's perspective. This book also contains numerous case studies from recently developed protease drugs.

Viral Proteases and Their Inhibitors

Author: Satya Prakash Gupta

Publisher: Academic Press

Published: 2017-07-03

Total Pages: 516

ISBN-13: 0128096829

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Viral Proteases and Their Inhibitors provides a thorough examination of viral proteases from their molecular components, to therapeutic applications. As information on three dimensional structures and biological functions of these viral proteases become known, unexpected protein folds and unique mechanisms of proteolysis are realized. This book investigates how this facilitates the design and development of potent antiviral agents used against life-threatening viruses. Users will find descriptions of each virus that detail the structure and function of viral proteases, discuss the design and development of inhibitors, and analyze the structure-activity relationships of inhibitors. This book is ideal biochemists, virologists and those working on antiviral agents. Provides comprehensive, state-of-the-art coverage of virus infections, the virus lifecycle, and mechanisms of protease inhibition Analyzes structure-activity relationships of inhibitors of each viral protease Presents an in-depth view of the structure and function of viral proteases

Proteases as Targets for Therapy

Author: Klaus von der Helm

Publisher: Springer Science & Business Media

Published: 2000

Total Pages: 440

ISBN-13: 9783540661184

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This volume is the first to combine latest information on viral, microbial and cellular proteolytic enzymes as potential targets for human therapeutics. Proteases control a large array of physiological reactions, and are involved in a variety of pathological processes for which effective medications are currently needed and/or being sought after. Although protease inhibitors have been investigated for many years, few have been employed therapeutically. Recent break- through by HIV protease inhibitors as therapeutic drugs has re-encouraged the search for inhibitors of other proteolytic enzymes. Klaus von der Helm, who described the first viral protease has brought leading experts together to discuss not only the success and problems of clinical use and continuing prospects, but to review further potential drug targets. This volume provides detailed information and evaluations of key viral, bacterial, fungal, and cellular proteases as potential future drug candidates.

Activity-Based Protein Profiling

Author: Benjamin F. Cravatt

Publisher: Springer

Published: 2019-01-25

Total Pages: 417

ISBN-13: 3030111431

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This volume provides a collection of contemporary perspectives on using activity-based protein profiling (ABPP) for biological discoveries in protein science, microbiology, and immunology. A common theme throughout is the special utility of ABPP to interrogate protein function and small-molecule interactions on a global scale in native biological systems. Each chapter showcases distinct advantages of ABPP applied to diverse protein classes and biological systems. As such, the book offers readers valuable insights into the basic principles of ABPP technology and how to apply this approach to biological questions ranging from the study of post-translational modifications to targeting bacterial effectors in host-pathogen interactions.

Protein Crystallography in Drug Discovery

Author: Robert E. Babine

Publisher: John Wiley & Sons

Published: 2008-07-15

Total Pages: 278

ISBN-13: 3527606351

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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.

Synthesis of Best-Seller Drugs

Author: Ruben Vardanyan

Publisher: Academic Press

Published: 2016-01-07

Total Pages: 870

ISBN-13: 0124115241

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Synthesis of Best-Seller Drugs is a key reference guide for all those involved with the design, development, and use of the best-selling drugs. Designed for ease of use, this book provides detailed information on the most popular drugs, using a practical layout arranged according to drug type. Each chapter reviews the main drugs in each of nearly 40 key therapeutic areas, also examining their classification, novel structural features, models of action, and synthesis. Of high interest to all those who work in the captivating areas of biologically active compounds and medicinal drug synthesis, in particular medicinal chemists, biochemists, and pharmacologists, the book aims to support current research efforts, while also encouraging future developments in this important field. Describes methods of synthesis, bioactivity and related drugs in key therapeutic areas Reviews the main drugs in each of nearly 40 key therapeutic areas, also examining their classification, novel structural features, models of action, and more Presents a practical layout designed for use as a quick reference tool by those working in drug design, development and implementation