Proteases as Targets for Therapy, Выпуск 146

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Klaus von der Helm, Bruce D. Korant, John Chris Dion Cheronis
Springer Science & Business Media, 2000 - Всего страниц: 410
Section I. Human Immunodeficiency Virus Protease Inhibitors.- 1 The Road to Fortovase. A History of Saquinavir, the First Human Immunodeficiency Virus Protease Inhibitor.- 2 Clinical Experience with Human Immunodeficiency Virus Protease Inhibitors: Antiretroviral Results, Questions and Future Strategies.- 3 The Nature of Resistance to Human Immunodeficiency Virus Type-1 Protease Inhibitors.- 4 The Next Generation of Human Immunodeficiency Virus Protease Inhibitors: Targeting Viral Resistance.- Section II. Other Viral (Non-HIV) Protease Inhibitors.- 5 The Proteinases Encoded by Hepatitis C Virus as Therapeutic Targets.- 6 The Human Herpes-Virus Proteases.- 7 The 3C Proteinases of Picornaviruses and Other Positive-Sense, Single-Stranded RNA Viruses.- 8 Adenovirus Proteinase-Antiviral Target for Triple-Combination Therapy on a Single Enzyme: Potential Inhibitor-Binding Sites.- 9 Proteinases as Virulence Factors in Bacterial Diseases and as Potential Targets for Therapeutic Intervention with Proteinase Inhibitors.- 10 Parasite Proteases as Targets for Therapy.- Section III. (Non-Viral) Proteases Involved in Diseases.- 11 Host Proteinases as Targets for Therapeutic Intervention.- 12 The Role of Metalloprotease Inhibitors in Cancer and Chronic Inflammatory Diseases.- 13 The Tumor Necrosis Factor-? Converting Enzyme.- 14 Serine Elastases in Inflammatory and Vascular Diseases.- 15 Inhibitors of Thrombin and Factor Xa.- 16 Inhibitors of Papain-Like Cysteine Peptidases in Cancer.- 17 Caspases and Their Natural Inhibitors as Therapeutic Targets for Regulating Apoptosis.- 18 Proteasome and Apoptosis.- 19 Proteolytic Processing of the Amyloid Precursor Protein of Alzheimer's Disease.- 20 Presenilins and ?-Amyloid Precursor Protein-Proteolytically Processed Proteins Involved in the Generation of Alzheimer's Amyloid ? Peptide.

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TANAKA K The Tokyo Metropolitan Institute of Medical Science
3
Early Clinical Studies
13
3333
20
Clinical Experience with Human Immunodeficiency Virus Protease
23
CHAPTER 3
33
Different Classes of Resistance Mutations in the Protease
39
CHAPTER 4
49
Suggestions for Future Therapeutic Strategies
66
General Considerations in the Development of MMPIS
224
G Conclusions
231
Inhibitors of TACE and TNFa Secretion
245
CHAPTER 14
259
B Serine Elastases and Inflammation
262
Potential Clinical Targets for SerineElastase Inhibition
268
82
273
CHAPTER 15
277

CHAPTER 5
75
The NS23 Proteinase
87
CHAPTER 6
95
78
101
E CellBased Activity of Protease Inhibitors
108
CHAPTER 7
117
E The 3C Proteinases
125
F Inhibition of 3C Proteinases
132
CHAPTER 8
145
Potential InhibitorBinding Sites
152
E Summary and Prospects
155
80
165
E Paradigms for Testing Proteinase Inhibitors as Therapeutic
173
F Bacterial Proteinases to the Rescue
179
CHAPTER 10
189
Serine Proteases
198
CHAPTER 11
207
Section Overview
213
81
218
CHAPTER 12
221
FactorXa Inhibitors
289
83
295
118
297
CHAPTER 16
301
Cystatins in Cancer
310
Potential Transcriptional Regulation
316
84
324
CHAPTER 17
329
G Potential for Caspase Inhibitor Therapy
335
CHAPTER 18
341
Regulatory Control of Ub and the Proteasome in Apoptosis
346
F The UbProteasome System and Cancer Therapy
353
CHAPTER 19
359
87
370
Role of Mutant Presenilins in Amyloid Generation
378
E Proteolytic Degradation of PSs
384
New Targets for AntiAmyloidogenic Drugs?
390
Subject Index
403
119
404
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