Proteases Structure and Function

Author: Klaudia Brix
Publisher: Springer Science & Business Media
ISBN: 3709108853
Format: PDF, ePub, Mobi
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Proteolysis is an irreversible posttranslational modification affecting each and every protein from its biosynthesis to its degradation. Limited proteolysis regulates targeting and activity throughout the lifetime of proteins. Balancing proteolysis is therefore crucial for physiological homeostasis. Control mechanisms include proteolytic maturation of zymogens resulting in active proteases and the shut down of proteolysis by counteracting endogenous protease inhibitors. Beyond the protein level, proteolytic enzymes are involved in key decisions during development that determine life and death – from single cells to adult individuals. In particular, we are becoming aware of the subtle role that proteases play in signaling events within proteolysis networks, in which the enzymes act synergistically and form alliances in a web-like fashion. Proteases come in different flavors. At least five families of mechanistically distinct enzymes and even more inhibitor families are known to date, many family members are still to be studied in detail. We have learned a lot about the diversity of the about 600 proteases in the human genome and begin to understand their physiological roles in the degradome. However, there are still many open questions regarding their actions in pathophysiology. It is in this area where the development of small molecule inhibitors as therapeutic agents is extremely promising. Approaching proteolysis as the most important, irreversible post-translational protein modification essentially requires an integrated effort of complementary research disciplines. In fact, proteolytic enzymes seem as diverse as the scientists working with these intriguing proteins. This book reflects the efforts of many in this exciting field of research where team and network formations are essential to move ahead.

Acid Proteases Structure Function and Biology

Author: Jordan Tang
Publisher: Springer Science & Business Media
ISBN: 1475707193
Format: PDF, Docs
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In the past ten years, a number of proceedings of symposia on the structure and function of proteolytic enzymes have been pub lished. Their coverage of acid proteases has been limited, mainly due to the lack of significant new information on the structure of these enzymes. In the last four years, however, the primary and tertiary structures of a number of acid proteases have been deter mined, prompting the need to discuss the meanings of the old data and the possibilities for new experimentations. It was for this purpose that the "Conference on Acid Proteases: Structure, Function, and Biology" was organized. It took place at the University of Oklahoma on November 21-24, 1976. This book is a collection of the main lectures delivered at the Conference. Acid Proteases, by definition refers to a group of proteases having an optimal pH in acidic solutions. The classic examples are pepsin and chymosin. Some catalytic features are obviously shared by these proteases, most notably, their inhibition by pepstatin. The use of active center-directed inactivators such as diazoacetyl norleucine methyl ester and 1,2-epoxy-3-(p-nitrophenoxy)propane has shown that two catalytic aspartyl residues are present in most of these enzymes. These apparent cornmon features have prompted the suggestion by several investigators to name this group of enzymes "aspartyl proteases" or "carboxyl proteases".

Structure Function Relationships of Proteolytic Enzymes

Author: P. Desnuelle
Publisher: Elsevier
ISBN: 1483261174
Format: PDF
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Structure–Function Relationships of Proteolytic Enzymes provides information pertinent to the fundamental aspects of proteolytic enzymes. This book presents the historical role of proteolytic enzyme as a group in protein and enzyme chemistry. Organized into 23 chapters, this book begins with an overview of the results obtained from investigation on the chymotrypsinogens of porcine origin. This text then examines the differences of amino acid sequence between chymotrypsin, trypsin, and elastase that affect the substrate binding site, which reflect the specificity differences between these enzymes. Other chapters consider the kinetic parameters related to the trypsin-catalyzed hydrolysis of several model peptides. This book discusses as well the acetylation of trypsin, which result in functional consequences varying from complete inactivation to promotion of activity. The final chapter deals with the physical properties of stem bromelain in comparison with the data for three other sulfhydryl proteases of plant origin. This book is a valuable resource for enzymologists, microbiologists, and biochemists.

Mechanisms of Protease Action

Author: Laszlo Polgar
Publisher: CRC Press
ISBN: 9780849369018
Format: PDF, Kindle
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A uniform treatment of the four protease groups and a discussion of the differences and similarities in their action is presented in this important new publication. Serine, cysteine, aspartate, and zinc proteases are systematically discussed by nomenclature, evolution, specificity and their regulatory role. The chemistry of the peptide bond, including the catalysis of ester and peptide hydrolyses, is explained. For each protease group the emphasis is placed on the structure and function. Kinetics, enzyme modifications, isotope effects, subzero temperature investigations, nuclear magnetic resonance measurements, X-ray diffraction data, binding of transition-state analogs, zymogen activation, and site-specific mutagenesis are combined to rationalize the action of proteases. Both natural and synthetic inhibitors are considered because of their importance in mechanistic studies and drug design.

Aspartic Acid Proteases as Therapeutic Targets

Author: Arun K. Ghosh
Publisher: John Wiley & Sons
ISBN: 3527641629
Format: PDF, ePub, Mobi
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In this ground-breaking practical reference, the family of aspartic acid proteases is described from a drug developer's perspective. The first part provides a general introduction to the family of aspartic acid proteases, their physiological functions, molecular structure and inhibition. Parts two to five present various case studies of successful protease inhibitor drug design and development, as well as current and potential uses of such inhibitors in pharmaceutical medicine, covering the major therapeutic targets HIV-1 protease, renin, beta-secretase, gamma-secretase,plasmepsins and fungal proteases. A ready reference aimed primarily at professionals in the pharmaceutical industry, as well as for anyone studying proteases and their function.

PROTEASES Potential Role in Health and Disease

Author: Walter H. Horl
Publisher: Springer Science & Business Media
ISBN: 1461593557
Format: PDF, Docs
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We are pleased to present to our readers the Proceedings of the International Symposium "Proteases: Potential Role in Health and Disease" which was held in WUrzburg (FRG) during October 17-20, 1982. The topics discussed included those dealing with the physi ology and pathophysiology of proteases and their inhibitors, the interactions of proteases and hormones, the kallikrein-kinin system, complement and the coagulation system, the function of proteases in the kidney and the intestinal tract as well as the role of proteases in lung diseases, pancreatitis, arthritis and hypercatabolic states (multiple trauma, septicemia, acute renal failure). The papers presented answered many questions, but raised many more concerning the significance of proteases and their inhibitors in clinical medicine. It was unfortunately impossible in this volume to in clude the extended, lively and extremely stimulating discussions which were enjoyed by the participants during the conference. The meeting has provided a unique framework for close inter action between scientists from various disciplines, including bio chemistry, physiology, surgery, anaesthesiology, endocrinology, hematology, pulmonology and nephrology. We would like to express our thanks and appreciation for all those who have stimulated, encouraged and supported us to hold this symposium in WUrzburg. This endeavor could not have been possible without the generous financial support of the Paul-Martini Foundation (Mainz), Bayer AG (Leverkusen), Beiersdorf AG (Hamburg).

Viral Proteases and Their Inhibitors

Author: Satya Prakash Gupta
Publisher: Academic Press
ISBN: 0128096829
Format: PDF, Mobi
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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

Cysteine Proteases of Pathogenic Organisms

Author: Mark W. Robinson
Publisher: Springer Science & Business Media
ISBN: 9781441984142
Format: PDF, Mobi
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Cysteine proteases expressed by pathogenic organisms play key roles in virulence including host entry, feeding and suppression of host immune responses. This book gives comprehensive coverage to all aspects of pathogen cysteine proteases and brings together numerous scientific advances which have been made over many years. Thus, the biochemistry, molecular biology and structure‐function relationships of these important pathogen enzymes are covered in detail. Written by leading researchers from Europe, Australia and North America, this book is essential reading for students and professionals interested in human medicine and infectious disease research.

Proteases

Author: Vito Turk
Publisher: Springer Science & Business Media
ISBN: 9783764357894
Format: PDF, ePub, Docs
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This book provides an account of the recent advances in our understanding of the role of proteases under physiological and pathological conditions. It reviews the contributions that have been made in the fields of biochemistry, molecular biology, medicine, agriculture and ecology. In addition there is an account of the growing number of practical applications in biotechnology, reflecting the fact that peptidases are major targets for medical and agricultural purposes. The book shows how the numerous protease structures are essential for drug design. The contributions place special emphasis on cysteine, aspartic and metalloproteases and their role in physiological and certain pathological states. Another focus is the classification and nomenclature of peptidases and a review of those proteases currently under the most intensive investigation. The book provides an informative introduction for teachers and newcomers to the field, such as graduate students, while providing a valuable source of material and ideas for the academic and industrial researcher in areas including biochemistry, medicine, agriculture and biotechnology.

Retroviral Proteases

Author: Lawrence C. Kuo
Publisher: Gulf Professional Publishing
ISBN: 9780121821425
Format: PDF, Docs
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Methods included in this volume apply to the expression and characterization of retroviral proteases and their inhibitor/substrate design.