Protein Kinases in Drug Discovery

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Publisher : Academic Press
ISBN 13 : 0323853145
Total Pages : 350 pages
Book Rating : 4.3/5 (238 download)

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Book Synopsis Protein Kinases in Drug Discovery by : Rossen Donev

Download or read book Protein Kinases in Drug Discovery written by Rossen Donev and published by Academic Press. This book was released on 2021-02-22 with total page 350 pages. Available in PDF, EPUB and Kindle. Book excerpt: Protein Kinases in Drug Discovery, Volume 124 discusses the latest information on protein kinases and how they modify other proteins by chemically adding phosphate groups to them. New chapters in this release include Transport Proteins and AMPs: Implications in Human Disease, Protein kinase CK2 inhibition as a pharmacological strategy, Emerging role of Protein kinase in diabetes mellitus: From Mechanism to therapy, Dual Roles of ATP-binding site in Protein Kinases: Orthosteric inhibition and Allosteric Regulation, Pseudokinases in drug discovery and development: progress, challenges and future prospects, Comparison of knowledge-based vs. combinatorial peptide library approaches for the identification of protein kinase substrates, and more. Contains timely chapters written by well-renown authorities in their field Includes a number of high-quality illustrations, figures and tables, and targets a very wide audience of specialists, researchers and students Integrates experimental and computational methods for studying the role of protein kinases in different diseases, along with sections on the design of suitable protein kinase inhibitors for use in the treatment of patients

Protein Kinases as Drug Targets

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Publisher : John Wiley & Sons
ISBN 13 : 3527633499
Total Pages : 570 pages
Book Rating : 4.5/5 (276 download)

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Book Synopsis Protein Kinases as Drug Targets by : Bert Klebl

Download or read book Protein Kinases as Drug Targets written by Bert Klebl and published by John Wiley & Sons. This book was released on 2011-03-16 with total page 570 pages. Available in PDF, EPUB and Kindle. Book excerpt: This timely guide to kinase inhibitor drug development is the first to cover the entire drug pipeline, from target identification to compound development and clinical application. Edited by the pioneers in the field, on the drug development side this ready reference discusses classical medicinal chemistry approaches as well as current chemical genomics strategies. On the clinical side, both current and future therapeutic application areas for kinase inhibitor drugs are addressed, with a strong focus on oncology drugs. Backed by recent clinical experience with first-generation drugs in the battle against various forms of cancer, this is crucial reading for medicinal, pharmaceutical and biochemists, molecular biologists, and oncologists, as well as those working in the pharmaceutical industry.

Kinase Drug Discovery

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Publisher : Royal Society of Chemistry
ISBN 13 : 1788015630
Total Pages : 430 pages
Book Rating : 4.7/5 (88 download)

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Book Synopsis Kinase Drug Discovery by : Richard A Ward

Download or read book Kinase Drug Discovery written by Richard A Ward and published by Royal Society of Chemistry. This book was released on 2018-10-31 with total page 430 pages. Available in PDF, EPUB and Kindle. Book excerpt: Kinase inhibition remains an area of significant interest, and growing importance, across academia and the pharmaceutical industry. There are now many marketed drugs that target kinases and a significant number of compounds are currently in various stages of clinical development. This book is a forward-looking analysis of a number of key areas for kinase inhibition in the coming years and builds on the first volume. This includes topics such as screening approaches to target kinases along with different modes of inhibition such as allosteric and covalent. Novel approaches such as macrocyclisation are considered along with how the properties of kinase inhibitors have evolved, including the potential for brain penetration. Recent areas of great importance also covered include cutting edge molecular modelling approaches and the importance of kinase mutations. The evolving biology of kinases has also resulted in increased interest in the immuno-oncology area and also pseudokinases as a target family. As with the first volume the book finishes with a forward looking view of how research against this fascinating target class may evolve.

Kinase Drug Discovery

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Publisher : Royal Society of Chemistry
ISBN 13 : 1849731748
Total Pages : 333 pages
Book Rating : 4.8/5 (497 download)

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Book Synopsis Kinase Drug Discovery by : Richard A. Ward

Download or read book Kinase Drug Discovery written by Richard A. Ward and published by Royal Society of Chemistry. This book was released on 2012 with total page 333 pages. Available in PDF, EPUB and Kindle. Book excerpt: Kinase drug discovery remains an area of significant interest across academia and in the pharmaceutical industry. There are now around 13 FDA approved small molecule drugs which target kinases and many more compounds in various stages of clinical development. Although there have been a number of reviews/publications on kinase research, this book fills a gap in the literature by considering the current and future opportunities and challenges in targeting this important family of enzymes. The book is forward-looking and identifies a number of hot topics and key areas for kinase drug discovery over the coming years. It includes contributions from highly respected authors with a combined experience in the industry of well over 200 years, which has resulted in a book of great interest to the kinase field and across drug discovery more generally. Readers will gain a real insight into the huge challenges and opportunities which this target class has presented drug discovery scientists. The many chapters cover a wide breadth of topics, are well written and include high quality colour and black and white images. Topics covered include an outline of how medicinal chemistry has been able to specifically exploit this unique target class, along with reflections on the mechanisms of kinases inhibitors. Also covered is resistance to kinase inhibitors caused by amino acid mutations, case studies of kinase programs and reviews areas beyond protein kinases and beyond the human kinome. Also described are modern approaches to finding kinase leads and the book finishes with a reflection of how kinase drug discovery may progress over the coming years.

Protein Kinase Inhibitors

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Publisher : Academic Press
ISBN 13 : 0323913490
Total Pages : 832 pages
Book Rating : 4.3/5 (239 download)

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Book Synopsis Protein Kinase Inhibitors by : Md. Imtaiyaz Hassan

Download or read book Protein Kinase Inhibitors written by Md. Imtaiyaz Hassan and published by Academic Press. This book was released on 2022-05-19 with total page 832 pages. Available in PDF, EPUB and Kindle. Book excerpt: Protein Kinase Inhibitors: From Discovery to Therapeutics offers a foundational, pragmatic overview of protein kinases inhibitors and their potential role in disease modulation and treatment. Here, international experts in the field offer an integrated discussion of kinase inhibitor biology, biomarker discovery, and methods for drug design and development. After a brief overview of kinases and kinase inhibitors, subsequent chapters discuss individual kinases that are representative of the wider kinases and kinase families, including their roles in disease pathogenesis, underlying mechanisms, potential inhibitors and their modes of action for therapeutic modulation. Several potential drugs under different stages of clinical trials are discussed, including their relevance to cancer, diabetes, obesity, cardiovascular, neurological, and auto-immune and inflammatory disease, among other disorders. The book also addresses the challenges and opportunities for future kinase inhibitor development. Provides a thorough overview of kinase inhibitor biology and its role in disease progression and modulation Examines protein kinase inhibitor drugs in various stages of clinical trials and development Offers methods and protocols for protein kinase inhibitor research studies and drug design and development Includes chapter contributions from international leaders in the field

Protein Tyrosine Kinases

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Publisher : Springer Science & Business Media
ISBN 13 : 1592599621
Total Pages : 599 pages
Book Rating : 4.5/5 (925 download)

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Book Synopsis Protein Tyrosine Kinases by : Doriano Fabbro

Download or read book Protein Tyrosine Kinases written by Doriano Fabbro and published by Springer Science & Business Media. This book was released on 2007-11-13 with total page 599 pages. Available in PDF, EPUB and Kindle. Book excerpt: Leading researchers, from the Novartis group that pioneered Gleevec/GlivecTM and around the world, comprehensively survey the state of the art in the drug discovery processes (bio- and chemoinformatics, structural biology, profiling, generation of resistance, etc.) aimed at generating PTK inhibitors for the treatment of various diseases, including cancer. Highlights include a discussion of the rationale and the progress made towards generating "selective" low molecular-weight kinase inhibitors; an analysis of the normal function, role in disease, and application of platelet-derived growth factor antagonists; and a summary of the factors involved in successful structure-based drug design. Additional chapters address the advantages and disadvantages of in vivo preclinical models for testing protein kinase inhibitors with antitumor activity and the utility of different methods in the drug discovery and development process for determining "on-target" vs "off-target" effects of kinase inhibitors.

Kinase Inhibitor Drugs

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Publisher : John Wiley & Sons
ISBN 13 : 1118210905
Total Pages : 463 pages
Book Rating : 4.1/5 (182 download)

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Book Synopsis Kinase Inhibitor Drugs by : Rongshi Li

Download or read book Kinase Inhibitor Drugs written by Rongshi Li and published by John Wiley & Sons. This book was released on 2011-09-20 with total page 463 pages. Available in PDF, EPUB and Kindle. Book excerpt: A comprehensive resource on case studies of marketed kinase drugs and promising drug trials Since the discovery of protein kinase activity in 1954, the field of protein kinase drug discovery has advanced dramatically. With the ongoing clinical success of the Bcr-Abl kinase inhibitor Gleevec in the treatment of chronic myelogenous leukemia and seven additional marketed kinase inhibitor drugs, researchers have compelling evidence that kinase inhibitors can be highly efficacious in the treatment of diseases caused by aberrant activity of protein kinase. Currently more than 100 protein kinase inhibitors are in clinical development. In one comprehensive volume, the editors, Dr. Rongshi Li and Dr. Jeffrey Stafford, present timely and important case studies of marketed kinase drugs and several of the most advanced kinase inhibitors in clinical trials. Kinase Inhibitor Drugs includes: Case studies from leading investigators and experts in the field that provide firsthand accounts of kinase inhibitor discovery Current thinking on kinase structure, biochemistry, and signal transduction pathways Information on state-of-the-art technologies and tools such as structure-based and fragment-based drug discovery A lineup of clinical-phase growth factor receptor inhibitors Inhibitors of cell cycle kinases The discovery of allosteric inhibitors of MEK kinase Information on pharmacogenomics and its application to kinase inhibitor clinical development

Targeting Protein Kinases for Cancer Therapy

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Publisher : John Wiley & Sons
ISBN 13 : 1118210778
Total Pages : 719 pages
Book Rating : 4.1/5 (182 download)

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Book Synopsis Targeting Protein Kinases for Cancer Therapy by : David J. Matthews

Download or read book Targeting Protein Kinases for Cancer Therapy written by David J. Matthews and published by John Wiley & Sons. This book was released on 2011-09-20 with total page 719 pages. Available in PDF, EPUB and Kindle. Book excerpt: An expert guide to targeting protein kinases in cancer therapy Research has shown that protein kinases can instigate the formation and spread of cancer when they transmit faulty signals inside cells. Because of this fact, pharmaceutical scientists have targeted kinases for intensive study, and have been working to develop medicinal roadblocks to sever their malignant means of communication. Complete with full-color presentations, Targeting Protein Kinases for Cancer Therapy defines the structural features of protein kinases and examines their cellular functions. Combining kinase biology with chemistry and pharmacology applications, this book enlists emerging data to drive the discovery of new cancer-fighting drugs. Valuable information includes: Comprehensive overviews of the major kinase families involved in oncology, integrating protein structure and function, and providing important tools to assist pharmaceutical researchers to understand and work in this dynamic area of cancer drug research Focus on small molecule inhibitors as well as other therapeutic modalities Discussion of kinase inhibitors that have entered clinical trials for the treatment of cancer, with an emphasis on molecules that have progressed to late stage clinical trials and, in a few cases, to market Providing a platform for further study, this important work reviews both the successes and challenges of kinase inhibitor therapy, and provides insight into future directions in the war against cancer.

Next Generation Kinase Inhibitors

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Publisher : Springer Nature
ISBN 13 : 3030482839
Total Pages : 224 pages
Book Rating : 4.0/5 (34 download)

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Book Synopsis Next Generation Kinase Inhibitors by : Paul Shapiro

Download or read book Next Generation Kinase Inhibitors written by Paul Shapiro and published by Springer Nature. This book was released on 2020-07-14 with total page 224 pages. Available in PDF, EPUB and Kindle. Book excerpt: Protein kinases are fascinating enzymes that maintain the proper function of nearly every task performed by the cells of the human body. By extracting a phosphate from the energy molecule ATP and linking it to another protein, protein kinases alter the structure and ultimate function of other proteins. In this way, protein kinases help monitor the extracellular environment and integrate signaling cues that, for the most part, are beneficial for human health and survival. However, protein kinases are often dysregulated and responsible for the initiation and progression of many types of cancers, inflammatory disorders, and other diseases. Thus, decades of research have revealed much about how protein kinases are regulated and approaches to inhibit these enzymes to treat disease. However, nearly 30 years since the identification of the first clinically beneficial small molecule protein kinase inhibitor, there are only a few examples where these drugs provide sustained and durable patient responses. The goal of this book is to provide biomedical scientists, graduate, and professional degree students insight into different approaches using small molecules to block specific protein kinase functions that promote disease.

Protein Kinases

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Publisher : BoD – Books on Demand
ISBN 13 : 1838809066
Total Pages : 164 pages
Book Rating : 4.8/5 (388 download)

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Book Synopsis Protein Kinases by :

Download or read book Protein Kinases written by and published by BoD – Books on Demand. This book was released on 2021-12-08 with total page 164 pages. Available in PDF, EPUB and Kindle. Book excerpt: For the past two decades, the protein kinase family has been an intense area of research for developing anticancer drugs. Despite tremendous advancements in kinase drug expansion, many kinases are still unexplored. As such, this book includes research and review articles from experts that focus on protein kinase signalling pathways as a molecular drug target. Chapters include illustrations and cover such topics as the mechanism of action and anticancer activity of protein kinase inhibitors on various cancer types. They also discuss new opportunities, challenges, and future perspectives in the field.

Protein-Protein Interactions in Drug Discovery

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Publisher : John Wiley & Sons
ISBN 13 : 3527648224
Total Pages : 493 pages
Book Rating : 4.5/5 (276 download)

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Book Synopsis Protein-Protein Interactions in Drug Discovery by : Alexander Dömling

Download or read book Protein-Protein Interactions in Drug Discovery written by Alexander Dömling and published by John Wiley & Sons. This book was released on 2013-01-02 with total page 493 pages. Available in PDF, EPUB and Kindle. Book excerpt: Treating protein-protein interactions as a novel and highly promising class of drug targets, this volume introduces the underlying strategies step by step, from the biology of PPIs to biophysical and computational methods for their investigation. The main part of the book describes examples of protein targets for which small molecule modulators have been developed, covering such diverse fields as cancer, autoimmune disorders and infectious diseases. Tailor-made for the practicing medicinal chemist, this ready reference includes a wide selection of case studies taken straight from the development pipeline of major pharmaceutical companies to illustrate the power and potential of this approach. From the contents: * Prediction of intra- and inter-species protein-protein interactions facilitating systems biology studies * Modulators of protein-protein interactions: The importance of Three-Dimensionality * Interactive technologies for leveraging the known chemistry of anchor residues * SH3 Domains as Drug Targets * P53 MDM2 Antagonists: Towards Non Genotoxic Anticancer Treatments * Inhibition of LFA-1/ICAM interaction for treatment of autoimmune diseases * The PIF-binding pocket of AGC kinases * Peptidic inhibitors of protein-protein interactions for cell adhesion receptors * The REPLACE Strategy for generating Non-ATP competitive Inhibitors of Cell-Cycle Protein Kinases and more

Protein Kinase Inhibitors in Research and Medicine

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Publisher : Academic Press
ISBN 13 : 0123984629
Total Pages : 252 pages
Book Rating : 4.1/5 (239 download)

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Book Synopsis Protein Kinase Inhibitors in Research and Medicine by :

Download or read book Protein Kinase Inhibitors in Research and Medicine written by and published by Academic Press. This book was released on 2013-07-01 with total page 252 pages. Available in PDF, EPUB and Kindle. Book excerpt: This new volume of Methods in Enzymology continues the legacy of this premier serial with quality chapters authored by leaders in the field. This volume covers protein kinase inhibitors in research and medicine, and includes chapters on such topics as fragment-based screening, broad kinome profiling of kinase inhibitors, and designing drug-resistant kinase alleles. Continues the legacy of this premier serial with quality chapters authored by leaders in the field Covers research methods in biomineralization science Contains sections focusing on protein kinase inhibitors in research and medicine

Protein Crystallography in Drug Discovery

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Publisher : John Wiley & Sons
ISBN 13 : 3527606351
Total Pages : 278 pages
Book Rating : 4.5/5 (276 download)

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

Download or read book Protein Crystallography in Drug Discovery written by Robert E. Babine and published by John Wiley & Sons. This book was released on 2008-07-15 with total page 278 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.

Proteinkinase Inhibitors

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Publisher : Springer Nature
ISBN 13 : 3030681807
Total Pages : 256 pages
Book Rating : 4.0/5 (36 download)

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Book Synopsis Proteinkinase Inhibitors by : Stefan Laufer

Download or read book Proteinkinase Inhibitors written by Stefan Laufer and published by Springer Nature. This book was released on 2021-03-23 with total page 256 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book reviews the principles of design and examples of successful implementation of proteinkinase inhibitors (PKI), and offers a comprehensive and authoritative overview of the history and latest developments in the field. Chapters written by experts from industry and academia cover the function, structure and topology of Proteinkinases, molecular modelling, disclose how to achieve high level of selectivity for kinase inhibitors, and exploit kinase inhibitors for cancer treatment. Particular attention is given to Inhibitors of c-Jun N-terminal kinase 3, and to covalent Janus Kinase 3 Inhibitors. A case study on Receptor Tyrosine Kinases EGFR, VEGFR, PDGFR is also presented in this book. Given its breath, this book will appeal to medicinal chemists, students, researchers and professionals alike.

Protein Kinases

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Publisher :
ISBN 13 : 9781579362645
Total Pages : pages
Book Rating : 4.3/5 (626 download)

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Book Synopsis Protein Kinases by : Sreten Bogdanovic

Download or read book Protein Kinases written by Sreten Bogdanovic and published by . This book was released on 2003-01-01 with total page pages. Available in PDF, EPUB and Kindle. Book excerpt:

Structural Biology in Drug Discovery

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Publisher : John Wiley & Sons
ISBN 13 : 1118900502
Total Pages : 1367 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 1367 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

Protein Allostery in Drug Discovery

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Publisher : Springer Nature
ISBN 13 : 9811387192
Total Pages : 384 pages
Book Rating : 4.8/5 (113 download)

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Book Synopsis Protein Allostery in Drug Discovery by : Jian Zhang

Download or read book Protein Allostery in Drug Discovery written by Jian Zhang and published by Springer Nature. This book was released on 2019-11-09 with total page 384 pages. Available in PDF, EPUB and Kindle. Book excerpt: The book focuses on protein allostery in drug discovery. Allosteric regulation, ʹthe second secret of lifeʹ, fine-tunes virtually most biological processes and controls physiological activities. Allostery can both cause human diseases and contribute to development of new therapeutics. Allosteric drugs exhibit unparalleled advantages compared to conventional orthosteric drugs, rendering the development of allosteric modulators as an appealing strategy to improve selectivity and pharmacodynamic properties in drug leads. The Series delineates the immense significance of protein allostery—as demonstrated by recent advances in the repertoires of the concept, its mechanistic mechanisms, and networks, characteristics of allosteric proteins, modulators, and sites, development of computational and experimental methods to predict allosteric sites, small-molecule allosteric modulators of protein kinases and G-protein coupled receptors, engineering allostery, and the underlying role of allostery in precise medicine. Comprehensive understanding of protein allostery is expected to guide the rational design of allosteric drugs for the treatment of human diseases. The book would be useful for scientists and students in the field of protein science and Pharmacology etc.