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 treatment of various disorders. Proteinase and Peptidase Inhibition presents updated progress reports on the characterization of a wide range of cellular proteinases whose inhibitors may hold the key to the development of new drugs. Introductory chapters deal with the broad enzyme classes, inhibitor types and regulatory mechanisms governing proteinase activity. The target enzymes themselves, together with all aspects of their inhibition and inhibitor design, are comprehensively described. The classification of target enzymes by structural similarity, rather than by pharmacological effects, provides a new and coherent platform for understanding how inhibition of different targets can lead to the same therapeutic outcomes. This is a valuable reference book that will appeal to both academic and industrial researchers in the fields of medicinal chemistry, drug design and development, pharmacology, biochemistry, and molecular and cell biology.
Enzyme Classes and Mechanisms. Regulatory Mechanisms for Proteinase Activity. Matrix Metalloproteinases (MMPs). Proteasomes. Cathepsins. Calpain. Human Neutrophil Elastase Inhibitors. Thrombin. Inhibitors of Factor VIIa, Factor IXa, and Factor Xa as Anticoagulants. The Urokinase-Type Plasminogen Activator (uPA) System: A New Target for Tumor Therapy. Proteinases Involved in Amyloid ß-Peptide (Aß) Production and Clearance. Herpes Virus and Cytomegalovirus Proteinase. Human Rhinovirus 3C Proteinase Inhibitors. Aminopeptidases. The Hepatitis C Virus NS3 Serine-Type Proteinase. Zinc Metallopeptidases. HIV Aspartate Proteinase: Resistance to Inhibitors. Proteases of Protozoan Parasites for Proteinase Activity.