Proteases of Infectious Agents
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Table of contents
- Cover
- Contentsvii
- Contributorsxiii
- Prefacexv
- Chapter 1. HIV Protease as a Target for the Design of Antiviral Agents for AIDS1
- I. Introduction1
- II. Retroviruses, HIV, and AIDS2
- III. HIV Protease: Biology, Biochemistry, and Structure5
- IV. Design of HIV Protease Inhibitors11
- V. Drug Resistance36
- VI. Future Challenges in HIV Protease Inhibitor Design41
- VII. Summary and Conclusions43
- References44
- Chapter 2. Proteases of the Hepatitis C Virus61
- I. Introduction61
- II. Genomic Organization63
- III. The NS2–NS3 Protease65
- IV. The NS3 Protease68
- V. Conclusions83
- References83
- Chapter 3. Human Herpesvirus Proteases93
- I. Introduction93
- II. Role of the Protease in the Virus Life Cycle96
- III. Primary Structures97
- IV. Enzymatic Activity99
- V. Three-Dimensional Structures102
- VI. Substrate Specificity105
- VII. Mechanism of Action106
- VIII. Inhibitors108
- IX. Ligand Binding112
- References113
- Chapter 4. The Secreted Proteinases from Candida: Challenges for Structure-Aided Drug Design117
- I. Introduction117
- II. Pathogenic Spectrum and Current Therapies118
- III. Secreted Aspartic Acid Proteases as Virulence Factors119
- IV. Secreted Aspartic Acid Protease Substrates and Early Inhibitors122
- V. Structural Characterization124
- VI. Candida Genomics133
- VII. Summary and Conclusions133
- VIII. Methods134
- References135
- Chapter 5. Proteolytic Enzymes of the Viruses of the Family Picornaviridae139
- I. Picornaviridae139
- II. Viral Replication and Polyprotein Processing140
- III. Picornaviral Proteinases146
- IV. Conclusions and Implications for Antiviral Strategies157
- References158
- Chapter 6. Proteases as Drug Targets for the Treatment of Malaria165
- I. Introduction165
- II. Proteases in Malaria Parasites167
- III. Current Antimalarial Agents with Effects on Parasite Proteolytic Enzymes184
- IV. Concluding Remarks185
- References185
- Chapter 7. Chagas Disease189
- I. Introduction189
- II. The Proteinases of Trypanosoma cruzi191
- III. Prospects for Novel Drugs Taking Trypanosoma cruzi Proteinases as Targets199
- References199
- Chapter 8. Cellular Proteinases and Viral Infection: Influenza Virus, Sendai Virus, and HIV-1205
- I. Introduction205
- II. Tryptase Clara in the Airway Epithelium Proteolytically Triggers the Infectivity of the Influenz206
- III. Human T-Cell Proteinase, Tryptase TL2, Binds to HIV-1 Envelope Glycoprotein gp120 Following Lim211
- References214
- Chapter 9. Bacterial Type I Signal Peptidases219
- I. Introduction219
- II. Biology, Biochemistry, Genetics, and Structure220
- III. Known Inhibitors226
- IV. Prospects for Novel Drugs227
- References229
- Chapter 10. Proteinases Involved in Plant Virus Genome Expression233
- I. Introduction233
- II. Picornalike Supergroup235
- III. Alphalike Supergroup249
- IV. Sobemolike Supergroup253
- V. Plant Pararetroviruses255
- VI. Concluding Remarks and Perspectives255
- References256
- Index265
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.
Key Features
* 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
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.
Key Features
* 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