Proteases Of Infectious Agents
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Proteases Of Infectious Agents
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Author : Ben Dunn
language : en
Publisher: Elsevier
Release Date : 1999-07-01
Proteases Of Infectious Agents written by Ben Dunn and has been published by Elsevier this book supported file pdf, txt, epub, kindle and other format this book has been release on 1999-07-01 with Science categories.
Proteases are enzymes that essentially "eat" protein. Without proteases, infectious organisms cannot properly mount an attack against a host. It is for this reason that proteases have become popular targets for drug discovery. Research has shown that if you can inhibit the protease, you can defend against the invading microbe. The defense against HIV, the virus that causes AIDS, is the best-documented case of the efficacy of protease inhibitors. Researchers are now trying to deploy this strategy against several infectious agents. This book gives information that is useful in that search. Proteases of Infectious Agents collects reviews from leading experts describing the latest information on the properties of key enzymes from a variety of viruses, fungi, and parasites. Each chapter provides the critical facts needed to initiate a drug discovery effort in that particular area. Includes information on the basic biology and function of proteases Provides global survey of current research efforts in protease inhibitors Illustrates how structure-based drug design targets effective and selective compounds Highlights important diseases that provide economically important targets Describes the role of proteases as important new targets for drug discovery
Protease Inhibitors In Aids Therapy
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Author : Richard C. Ogden
language : en
Publisher: CRC Press
Release Date : 2001-01-24
Protease Inhibitors In Aids Therapy written by Richard C. Ogden and has been published by CRC Press this book supported file pdf, txt, epub, kindle and other format this book has been release on 2001-01-24 with Medical categories.
Details the evolution of HIV protease inhibitors from molecular development through medical applications! Considering the latest class of revolutionary drugs fighting against HIV infection and AIDS, this comprehensive reference thoroughly examines the development and properties of HIV protease inhibitors from clinical and scientific perspectives, discussing how protease inhibitors changed the FDA approval process-enhancing the collaboration between regulatory authorities and drug developers. Spotlights protease inhibitors as the cornerstone drugs of the first HAART regimens-key components of long-term viral suppression and immune restoration, and in secondary and tertiary regimens! Evaluating protease inhibitors as therapeutic options and research tools, Protease Inhibitors in AIDS Therapy reviews the impact of advances in recombinant DNA technology for understanding and treating HIV and AIDS highlights a variety of strategies and techniques for drug discovery and development illustrated by success stories of pharmaceutical companies and biotechnology start-up firms summarizes the pharmacokinetics, metabolism, and drug interactions of protease inhibitors details preliminary clinical studies on oral bioavailability, pharmacokinetic profiling, efficacy, resistance, and tolerability describes available efficacy data for marketed inhibitors and those in clinical development reports on efforts to manage antiviral resistance in the clinic and improve patient adherence to complex drug therapy and more! Containing more than 600 helpful literature references, drawings, photographs, and tables, Protease Inhibitors in AIDS Therapy serves for an essential reference for infectious disease specialists, epidemiologists, virologists, immunologists, pharmacologists, medicinal chemists and biochemists, microbiologists, hematologists, hepatologists, and medical students in these disciplines.
Pseudomonas Aeruginosa As An Opportunistic Pathogen
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Author : Mario Campa
language : en
Publisher: Springer Science & Business Media
Release Date : 2012-12-06
Pseudomonas Aeruginosa As An Opportunistic Pathogen written by Mario Campa and has been published by Springer Science & Business Media this book supported file pdf, txt, epub, kindle and other format this book has been release on 2012-12-06 with Medical categories.
Assembling the latest research by an international group of contributors, this volume covers the epidemiology, pathogenesis, clinical features, and control measures of this elusive microorganism. It will provide a deeper understanding of the pathogen to physicians and surgeons caring for patients infected, or at risk of becoming infected, with Pseudomonas Aeruginosa.
Proteolytic Enzymes And Their Inhibitors In Infectious Pathogens
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Author : Theresa Coetzer
language : en
Publisher: Academic Press
Release Date : 2023-01-15
Proteolytic Enzymes And Their Inhibitors In Infectious Pathogens written by Theresa Coetzer and has been published by Academic Press this book supported file pdf, txt, epub, kindle and other format this book has been release on 2023-01-15 with Science categories.
Proteolytic enzymes are found in all life forms, where they catalyze peptide bond hydrolysis during essential biological processes. Proteases of various pathogens have also been shown to use endogenous protease inhibitors to regulate the activity of host proteolytic enzymes encountered during infection. Proteolytic Enzymes and their Inhibitors in Infectious Pathogens brings together key experts to provide a thorough discussion of proteolytic enzymes and their endogenous inhibitors found in parasites, bacteria, and viruses. The book focuses on the respective roles of the different catalytic classes of proteolytic enzymes and their protein-protease inhibitors at the host-infectious organism interface, and how this knowledge may inform drug and vaccine design. Following a foundational overview of proteases and macromolecular inhibitors of pathogenic organisms, authors discuss recent research on distinct classes of proteolytic enzymes in pathogens. Classes include aspartic proteases, cysteine proteases, metalloproteases, serine proteases, and threonine proteases with experts contributing chapters on distinct enzymes and inhibitors. New methods to identify protease substrates and inhibitors are also provided, with step-by-step protocols to advance new research and drive drug discovery. Discusses proteolytic enzymes of parasites, bacteria, and viruses arranged by peptide bond cleavage classes, for improved integration of information across the infectious organisms Includes information on the structure and interaction with proteases of macromolecular protease inhibitors, and how these structures can be engineered to provide more potent and specific protease inhibitors Provides instructions in methods and technologies to identify physiological protease substrates, their cleavage specificities, and inhibitors Features rich illustrations and diagrams of core concepts, including informative three-dimensional protein structures and molecular interactions
Proteases In Health And Disease
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Author : Sajal Chakraborti
language : en
Publisher: Springer Science & Business Media
Release Date : 2013-12-04
Proteases In Health And Disease written by Sajal Chakraborti and has been published by Springer Science & Business Media this book supported file pdf, txt, epub, kindle and other format this book has been release on 2013-12-04 with Science categories.
In view of rapidly growing research in the deregulation of proteases and their impact in human health and diseases, this book will highlight existing and emerging research in this exciting area. In-depth critical state-of-the-art reviews will be written by established investigators on proteases dysfunctions associated with pathogenesis of different diseases that are known to occur due to deregulation of proteolytic systems. Multidisciplinary approaches demonstrating biochemical and signal transduction mechanisms associated with deregulation of proteases leading to manifestation of the diseases will be discussed. The book highlights the roles of both intracellular and extracellular proteases in health and disease.
Viral Proteases And Antiviral Protease Inhibitor Therapy
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Author : Uwe Lendeckel
language : en
Publisher: Springer
Release Date : 2009-07-16
Viral Proteases And Antiviral Protease Inhibitor Therapy written by Uwe Lendeckel and has been published by Springer this book supported file pdf, txt, epub, kindle and other format this book has been release on 2009-07-16 with Medical categories.
The 8th volume in the Proteases in Biology and Disease series focuses on the role of proteases in virus function and their potential as anti-viral targets. Viral infections are still difficult to threat and some remained life-threatening diseases in spite of antiviral drug research over decades. Proteases are still regarded as an Achilles’ heel of the pathogens and, thus, protease inhibitors may help to handle the known and the emerging viral threads. The book discusses viral proteases of the most important pathogenic viruses, responsible for severe diseases: AIDS, SARS, Hepatitis, Cytomegalovirus, T-cell lymphotropic virus, Picornavirus. This book focuses specifically on the viral proteases, crucial prerequisites for viral entry into cells and viral replication. Viral proteases represent an important pharmaceutical target. The current stage of protease inhibitor development and therapy are summarised and discussed by experts in the field. This volume represents a timely and valuable continuation of the Proteases in Biology and Disease series. The reader will learn the potential for proteases as targets for effective anti-virals. This book will be a valuable source of information on viral proteases and provoke further research in this important field.
Encyclopedia Of Molecular Pharmacology
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Author : Stefan Offermanns
language : en
Publisher: Springer Science & Business Media
Release Date : 2008-08-14
Encyclopedia Of Molecular Pharmacology written by Stefan Offermanns and has been published by Springer Science & Business Media this book supported file pdf, txt, epub, kindle and other format this book has been release on 2008-08-14 with Medical categories.
An essential text, this is a fully updated second edition of a classic, now in two volumes. It provides rapid access to information on molecular pharmacology for research scientists, clinicians and advanced students. With the A-Z format of over 2,000 entries, around 350 authors provide a complete reference to the area of molecular pharmacology. The book combines the knowledge of classic pharmacology with the more recent approach of the precise analysis of the molecular mechanisms by which drugs exert their effects. Short keyword entries define common acronyms, terms and phrases. In addition, detailed essays provide in-depth information on drugs, cellular processes, molecular targets, techniques, molecular mechanisms, and general principles.
Viral Proteases And Their Inhibitors
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Author : Satya Prakash Gupta
language : en
Publisher: Academic Press
Release Date : 2017-07-03
Viral Proteases And Their Inhibitors written by Satya Prakash Gupta and has been published by Academic Press this book supported file pdf, txt, epub, kindle and other format this book has been release on 2017-07-03 with Science categories.
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 In Human Diseases
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Author : Sajal Chakraborti
language : en
Publisher: Springer
Release Date : 2017-07-13
Proteases In Human Diseases written by Sajal Chakraborti and has been published by Springer this book supported file pdf, txt, epub, kindle and other format this book has been release on 2017-07-13 with Medical categories.
This book bridges the gap between fundamental research and biomedical and pharmacological applications on proteases. It represents a comprehensive overview of the multifaceted field of proteases in cellular environment and highlights the recently elucidated functions of complex proteolytic systems in different diseases. Several established investigators have elucidated the crucial role of proteases in biological processes, including how proteolytic function and regulation can be combined to develop new strategies of therapeutic interventions. Proteases form one of the largest and most diverse families of enzymes known. It is now clear that proteases are involved in every aspect of life functions of an organism. Under physiological conditions, proteases are regulated by their endogenous inhibitors; however, when the activity of proteases is not regulated appropriately, disease processes can result in. So, there is absolute need for a stringent control of proteolytic activities in cells and tissues. Dysregulation of proteases may cause derangement of cellular signalling network resulting in different pathophysiological conditions such as vascular remodelling, atherosclerotic plaque progression, ulcer and rheumatoid arthritis, Alzheimer disease, cancer metastasis, tumor progression and inflammation. Additionally, many infective microorganisms require proteases for replication or use proteases as virulence factors, which have facilitated the development of protease-targeted therapies for a variety of parasitic diseases.
Discovery Of Covalent Allosteric Or Orthosteric Protease Inhibitors Of Infectious Viruses
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Author : Ittipat Meewan
language : en
Publisher:
Release Date : 2021
Discovery Of Covalent Allosteric Or Orthosteric Protease Inhibitors Of Infectious Viruses written by Ittipat Meewan and has been published by this book supported file pdf, txt, epub, kindle and other format this book has been release on 2021 with categories.
Over several centuries, infectious diseases caused by viruses have been a serious threat for human health globally. Even though the numbers new highly effective antiviral drugs or vaccines have been developed for the treatment rapidly, but there are plenty of newly emerge viruses that have no proper specific treatment. In addition, the reemergence of new drug resistance viral strain is a huge challenge for drug development. This dissertation presents studies the therapeutic approach of major infectious viral diseases by proper drug target selection, design of small molecules, and test the effectiveness of small molecules experimentally. In chapter 1, we discovered inhibitors containing thiuram disulfide or dithiobis-(thioformate) tested against three key proteases in The Severe Acute Respiratory Syndrome Coronavirus (SARS-CoV) replication including Main Protease (Mpro), SARS CoV-2 Papain Like Protease (PLpro), and human cathepsin L. The use of thiuram disulfide and dithiobis-(thioformate) covalent inhibitor warheads was inspired by disulfiram, a currently prescribed drug commonly used to treat chronic alcoholism that at the present time is in Phase 2 clinical trials against SARS-CoV-2. At the maximal allowed dose, disulfiram is associated with adverse effects. We found a few compounds that were more potent than disulfiram in the enzymatic assays against SARS-CoV-2 Mpro, SARS-CoV-2 PLpro, and human cathepsin L. The identified protease inhibitors in this series were also tested against SARS CoV-2 in a cell-based and toxicity assay and were shown to have similar or greater antiviral effect than Disulfiram. In chapter 2, we identified a novel transient deep and hydrophobic pocket of the "super-open" conformation of Zika virus (ZIKV) NS2B-NS3 protease and targeted it to overcome the limitations of the orthosteric inhibitors. We applied virtual docking screening of approximately 7 million compounds against the novel allosteric site and found seven candidates. Six out of seven top candidates selected by the docking screen inhibited ZIKV NS2B-NS3 protease proteolytic activity at low micromolar concentrations, as well as suppressing viral replication. In chapter 3, we discovered the novel class of small molecules based on a tryptophan derivative scaffold identified as hepatitis C (HCV) NS3/4A protease inhibitors that are active against both wild type and mutant form of the protease. We selected the compounds that the predicted binding poses not affected by the most frequent mutations in the active site. The top compounds had a comparable inhibition profile for the common mutant HCV GT1b D168A and the wild-type enzyme. The top three inhibitors were also tested against four human serine proteases and were shown to be specific to the viral protease. The fluorescence-based cell viability assay demonstrated a sufficient therapeutic range for the top three candidates.