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Aspartic acid proteases as therapeutic targets / / edited by Arun K. Ghosh
| Aspartic acid proteases as therapeutic targets / / edited by Arun K. Ghosh |
| Pubbl/distr/stampa | Weinheim, Germany : , : Wiley-VCH, , 2010 |
| Descrizione fisica | 1 online resource (641 p.) |
| Disciplina |
571.9/36
612.01516 |
| Collana | Methods and Principles in Medicinal Chemistry |
| Soggetto topico |
Aspartic proteinases
Aspartic proteinases - Inhibitors - Therapeutic use |
| Soggetto genere / forma | Electronic books. |
| ISBN |
1-282-77490-5
9786612774904 3-527-64162-9 3-527-63094-5 3-527-63095-3 |
| Formato | Materiale a stampa  |
| Livello bibliografico | Monografia |
| Lingua di pubblicazione | eng |
| Nota di contenuto |
Aspartic Acid Proteases as Therapeutic Targets; Contents; List of Contributors; Preface; A Personal Foreword; Part: One Overview of Aspartic Acid Proteases; 1 Introduction to the Aspartic Proteinase Family; 2 Aspartic Proteases: Structure, Function, and Inhibition; 3 Human Aspartic Proteinases; 4 Structure-Based Drug Design Strategies for Inhibition of Aspartic Proteinases; Part Two: HIV-1 Protease as Target for the Treatment of HIV/AIDS; 5 HIV-1 Protease: Role in Viral Replication, Protein-Ligand X-Ray Crystal Structures and Inhibitor Design
6 First-Generation HIV-1 Protease Inhibitors for the Treatment of HIV/AIDS7 Second-Generation Approved HIV Protease Inhibitors for the Treatment of HIV/AIDS; 8 Darunavir, a New PI with Dual Mechanism: From a Novel Drug Design Concept to New Hope Against Drug-Resistant HIV; 9 Development of HIV-1 Protease Inhibitors, Antiretroviral Resistance, and Current Challenges of HIV/AIDS Management; Part Three: Renin as Target for the Treatment of Hypertension; 10 Discovery and Development of Aliskiren, the First-in-Class Direct Renin Inhibitor for the Treatment of Hypertension 11 Evolution of Diverse Classes of Renin Inhibitors Through the YearsPart Four: ?-Secretase as Target for the Treatment of Alzheimer""s Disease; 12: ?-Secretase: An Unusual Enzyme with Many Possible Disease Targets, Including Alzheimer""s Disease; 13 ?-Secretase Inhibition: An Overview of Development of Inhibitors for the Treatment of Alzheimer's Disease; Part Five: ß-Secretase as Target for the Treatment of Alzheimer's Disease; 14 BACE: A (Almost) Perfect Target for Staving Off Alzheimer's Disease 15 The Discovery of ß-Secretase and Development Toward a Clinical Inhibitor for AD: An Exciting Academic Collaboration16 Peptidomimetic BACE1 Inhibitors for Treatment of Alzheimer.s Disease: Design and Evolution; 17 Nonpeptide BACE1 Inhibitors: Design and Synthesis; Part Six: Plasmepsins and Other Aspartic Proteases as Drug Targets; 18 The Plasmepsin Family as Antimalarial Drug Targets; 19 Plasmepsins Inhibitors as Potential Drugs Against Malaria: Starving the Parasite; 20 Fungal Aspartic Proteases as Possible Therapeutic Targets; Index |
| Record Nr. | UNINA-9910140801803321 |
| Weinheim, Germany : , : Wiley-VCH, , 2010 | ||
| Materiale a stampa | ||
| Lo trovi qui: Univ. Federico II | ||
| ||
Aspartic acid proteases as therapeutic targets / / edited by Arun K. Ghosh
| Aspartic acid proteases as therapeutic targets / / edited by Arun K. Ghosh |
| Pubbl/distr/stampa | Weinheim, Germany : , : Wiley-VCH, , 2010 |
| Descrizione fisica | 1 online resource (641 p.) |
| Disciplina |
571.9/36
612.01516 |
| Collana | Methods and Principles in Medicinal Chemistry |
| Soggetto topico |
Aspartic proteinases
Aspartic proteinases - Inhibitors - Therapeutic use |
| ISBN |
1-282-77490-5
9786612774904 3-527-64162-9 3-527-63094-5 3-527-63095-3 |
| Formato | Materiale a stampa |
| Livello bibliografico | Monografia |
| Lingua di pubblicazione | eng |
| Nota di contenuto |
Aspartic Acid Proteases as Therapeutic Targets; Contents; List of Contributors; Preface; A Personal Foreword; Part: One Overview of Aspartic Acid Proteases; 1 Introduction to the Aspartic Proteinase Family; 2 Aspartic Proteases: Structure, Function, and Inhibition; 3 Human Aspartic Proteinases; 4 Structure-Based Drug Design Strategies for Inhibition of Aspartic Proteinases; Part Two: HIV-1 Protease as Target for the Treatment of HIV/AIDS; 5 HIV-1 Protease: Role in Viral Replication, Protein-Ligand X-Ray Crystal Structures and Inhibitor Design
6 First-Generation HIV-1 Protease Inhibitors for the Treatment of HIV/AIDS7 Second-Generation Approved HIV Protease Inhibitors for the Treatment of HIV/AIDS; 8 Darunavir, a New PI with Dual Mechanism: From a Novel Drug Design Concept to New Hope Against Drug-Resistant HIV; 9 Development of HIV-1 Protease Inhibitors, Antiretroviral Resistance, and Current Challenges of HIV/AIDS Management; Part Three: Renin as Target for the Treatment of Hypertension; 10 Discovery and Development of Aliskiren, the First-in-Class Direct Renin Inhibitor for the Treatment of Hypertension 11 Evolution of Diverse Classes of Renin Inhibitors Through the YearsPart Four: ?-Secretase as Target for the Treatment of Alzheimer""s Disease; 12: ?-Secretase: An Unusual Enzyme with Many Possible Disease Targets, Including Alzheimer""s Disease; 13 ?-Secretase Inhibition: An Overview of Development of Inhibitors for the Treatment of Alzheimer's Disease; Part Five: ß-Secretase as Target for the Treatment of Alzheimer's Disease; 14 BACE: A (Almost) Perfect Target for Staving Off Alzheimer's Disease 15 The Discovery of ß-Secretase and Development Toward a Clinical Inhibitor for AD: An Exciting Academic Collaboration16 Peptidomimetic BACE1 Inhibitors for Treatment of Alzheimer.s Disease: Design and Evolution; 17 Nonpeptide BACE1 Inhibitors: Design and Synthesis; Part Six: Plasmepsins and Other Aspartic Proteases as Drug Targets; 18 The Plasmepsin Family as Antimalarial Drug Targets; 19 Plasmepsins Inhibitors as Potential Drugs Against Malaria: Starving the Parasite; 20 Fungal Aspartic Proteases as Possible Therapeutic Targets; Index |
| Record Nr. | UNINA-9910829994603321 |
| Weinheim, Germany : , : Wiley-VCH, , 2010 | ||
| Materiale a stampa | ||
| Lo trovi qui: Univ. Federico II | ||
| ||
Aspartic acid proteases as therapeutic targets / / edited by Arun K. Ghosh
| Aspartic acid proteases as therapeutic targets / / edited by Arun K. Ghosh |
| Pubbl/distr/stampa | Weinheim, : Wiley-VCH, 2010 |
| Descrizione fisica | 1 online resource (641 p.) |
| Disciplina |
571.9/36
612.01516 |
| Altri autori (Persone) | GhoshArun K., Prof. Dr. |
| Collana | Methods and principles in medicinal chemistry |
| Soggetto topico |
Aspartic proteinases
Aspartic proteinases - Inhibitors - Therapeutic use |
| ISBN |
9786612774904
9781282774902 1282774905 9783527641628 3527641629 9783527630943 3527630945 9783527630950 3527630953 |
| Formato | Materiale a stampa |
| Livello bibliografico | Monografia |
| Lingua di pubblicazione | eng |
| Nota di contenuto |
Aspartic Acid Proteases as Therapeutic Targets; Contents; List of Contributors; Preface; A Personal Foreword; Part: One Overview of Aspartic Acid Proteases; 1 Introduction to the Aspartic Proteinase Family; 2 Aspartic Proteases: Structure, Function, and Inhibition; 3 Human Aspartic Proteinases; 4 Structure-Based Drug Design Strategies for Inhibition of Aspartic Proteinases; Part Two: HIV-1 Protease as Target for the Treatment of HIV/AIDS; 5 HIV-1 Protease: Role in Viral Replication, Protein-Ligand X-Ray Crystal Structures and Inhibitor Design
6 First-Generation HIV-1 Protease Inhibitors for the Treatment of HIV/AIDS7 Second-Generation Approved HIV Protease Inhibitors for the Treatment of HIV/AIDS; 8 Darunavir, a New PI with Dual Mechanism: From a Novel Drug Design Concept to New Hope Against Drug-Resistant HIV; 9 Development of HIV-1 Protease Inhibitors, Antiretroviral Resistance, and Current Challenges of HIV/AIDS Management; Part Three: Renin as Target for the Treatment of Hypertension; 10 Discovery and Development of Aliskiren, the First-in-Class Direct Renin Inhibitor for the Treatment of Hypertension 11 Evolution of Diverse Classes of Renin Inhibitors Through the YearsPart Four: ?-Secretase as Target for the Treatment of Alzheimer""s Disease; 12: ?-Secretase: An Unusual Enzyme with Many Possible Disease Targets, Including Alzheimer""s Disease; 13 ?-Secretase Inhibition: An Overview of Development of Inhibitors for the Treatment of Alzheimer's Disease; Part Five: ß-Secretase as Target for the Treatment of Alzheimer's Disease; 14 BACE: A (Almost) Perfect Target for Staving Off Alzheimer's Disease 15 The Discovery of ß-Secretase and Development Toward a Clinical Inhibitor for AD: An Exciting Academic Collaboration16 Peptidomimetic BACE1 Inhibitors for Treatment of Alzheimer.s Disease: Design and Evolution; 17 Nonpeptide BACE1 Inhibitors: Design and Synthesis; Part Six: Plasmepsins and Other Aspartic Proteases as Drug Targets; 18 The Plasmepsin Family as Antimalarial Drug Targets; 19 Plasmepsins Inhibitors as Potential Drugs Against Malaria: Starving the Parasite; 20 Fungal Aspartic Proteases as Possible Therapeutic Targets; Index |
| Record Nr. | UNINA-9911018822903321 |
| Weinheim, : Wiley-VCH, 2010 | ||
| Materiale a stampa | ||
| Lo trovi qui: Univ. Federico II | ||
| ||
BACE [[electronic resource] ] : lead target for orchestrated therapy of Alzheimer's disease / / edited by Varghese John
| BACE [[electronic resource] ] : lead target for orchestrated therapy of Alzheimer's disease / / edited by Varghese John |
| Pubbl/distr/stampa | Hoboken, NJ, : John Wiley & Sons, c2010 |
| Descrizione fisica | 1 online resource (284 p.) |
| Disciplina | 618.976831 |
| Altri autori (Persone) | JohnVarghese <1958-> |
| Soggetto topico |
Alzheimer's disease - Chemotherapy
Aspartic proteinases - Inhibitors - Therapeutic use Amyloid beta-protein precursor |
| ISBN |
1-282-49175-X
9786612491757 0-470-59408-X 0-470-59407-1 |
| Formato | Materiale a stampa |
| Livello bibliografico | Monografia |
| Lingua di pubblicazione | eng |
| Nota di contenuto |
BACE; CONTENTS; PREFACE; ACKNOWLEDGMENTS; CONTRIBUTORS; CHAPTER 1 BACE, APP PROCESSING, AND SIGNAL TRANSDUCTION IN ALZHEIMER'S DISEASE; 1.1 Introduction; 1.2 BACE Cleavage of APP as a Molecular Switching Mechanism; 1.3 AD: An Imbalance in Cellular Dependence?; 1.4 BACE Cleavage, Caspase Cleavage, and Neuronal Trophic Dependence; 1.5 BACE Cleavage of APP, Dependence Receptors, and Alzheimer Pathology; 1.6 Key Mutations Proximal of APP Processing to Aβ; 1.7 Final Remarks; CHAPTER 2 IDENTIFICATION OF BACE AS A TARGET IN ALZHEIMER'S DISEASE; 2.1 Introduction; 2.2 The Search for β-Secretase
2.3 Validation of the BACE Target 2.4 Final Remarks; CHAPTER 3 BACE BIOLOGICAL ASSAYS; 3.1 Introduction; 3.2 Clinical and Physiological Hallmarks of Alzheimer's Disease (AD); 3.3 APP Processing; 3.4 Aspartyl Protease Classification; 3.5 BACE Structure; 3.6 Mechanism, Kinetics, Inhibition, and Specificity; 3.7 Assay Strategies for Inhibitor Finding and Development; 3.8 Common Assays Used to Identify and Study Inhibitors; 3.9 BACE Assays; 3.10 Final Remarks; CHAPTER 4 PEPTIDIC, PEPTIDOMIMETIC, AND HTS-DERIVED BACE INHIBITORS; 4.1 Introduction; 4.2 Elan/Pharmacia (Pfizer) 4.3 Oklahoma Medical Research Foundation (OMRF)/Multiple Collaborators 4.4 Eli Lilly; 4.5 Merck; 4.6 GlaxoSmithKline; 4.7 Schering Plough; 4.8 Bristol-Myers Squibb; 4.9 Novartis; 4.10 Amgen; 4.11 Wyeth; 4.12 Final Remarks; CHAPTER 5 FRAGMENT-BASED APPROACHES FOR IDENTIFICATION OF BACE INHIBITORS; 5.1 Introduction; 5.2 Biophysical Methods Applied to BACE Fragment Screens; 5.3 BACE Inhibitors Identified by Fragment Screening; 5.4 Final Remarks; CHAPTER 6 STRUCTURE-BASED DESIGN OF BACE INHIBITORS: TECHNICAL AND PRACTICAL ASPECTS OF PREPARATION, 3-DIMENSIONAL STRUCTURE, AND COMPUTATIONAL ANALYSIS 6.1 Introduction 6.2 Preparation of BACE for Structural Studies; 6.3 Crystallographic Studies of BACE; 6.4 Structural Studies with BACE Inhibitors: Peptidomimetics and Nonpeptidomimetics; 6.5 Computational Approaches; 6.6 Final Remarks; CHAPTER 7 PHARMACOLOGICAL MODELS FOR PRECLINICAL TESTING: FROM MOUSE TO DOG TO NONHUMAN PRIMATES; 7.1 Introduction; 7.2 BACE 1 and Mouse Models of AD; 7.3 Testing BACE Inhibitors in the Canine Model of Human Aging and AD; 7.4 BACE Inhibitors and Nonhuman Primates; 7.5 Final Remarks CHAPTER 8 ADSORPTION, DISTRIBUTION, METABOLISM, EXCRETION (ADME), EFFICACY, AND TOXICOLOGY FOR BACE INHIBITORS 8.1 Introduction; 8.2 Development of BACE Inhibitors with Optimized ADME Properties; 8.3 In Vivo Efficacy of BACE Inhibitors; 8.4 Toxicology of BACE Inhibitors; 8.5 Final Remarks; CHAPTER 9 CLINICAL TRIALS FOR DISEASE-MODIFYING DRUGS SUCH AS BACE INHIBITORS; 9.1 Introduction; 9.2 Update on Beta-Amyloid Therapies in Clinical Development; 9.3 Clinical Development of BACE Inhibitors and Other Disease-Modifying Drugs; 9.4 Final Remarks CHAPTER 10 FUTURE STRATEGIES FOR DEVELOPMENT OF NOVEL BACE INHIBITORS: ANTI-APP β-SITE ANTIBODY AND APP BINDING SMALL MOLECULE APPROACHES FOR ALZHEIMER'S DISEASE |
| Record Nr. | UNINA-9910140616703321 |
| Hoboken, NJ, : John Wiley & Sons, c2010 | ||
| Materiale a stampa | ||
| Lo trovi qui: Univ. Federico II | ||
| ||
BACE : lead target for orchestrated therapy of Alzheimer's disease / / edited by Varghese John
| BACE : lead target for orchestrated therapy of Alzheimer's disease / / edited by Varghese John |
| Edizione | [1st ed.] |
| Pubbl/distr/stampa | Hoboken, NJ, : John Wiley & Sons, c2010 |
| Descrizione fisica | 1 online resource (284 p.) |
| Disciplina | 618.976831 |
| Altri autori (Persone) | JohnVarghese <1958-> |
| Soggetto topico |
Alzheimer's disease - Chemotherapy
Aspartic proteinases - Inhibitors - Therapeutic use Amyloid beta-protein precursor |
| ISBN |
9786612491757
9781282491755 128249175X 9780470594087 047059408X 9780470594070 0470594071 |
| Formato | Materiale a stampa |
| Livello bibliografico | Monografia |
| Lingua di pubblicazione | eng |
| Nota di contenuto |
BACE; CONTENTS; PREFACE; ACKNOWLEDGMENTS; CONTRIBUTORS; CHAPTER 1 BACE, APP PROCESSING, AND SIGNAL TRANSDUCTION IN ALZHEIMER'S DISEASE; 1.1 Introduction; 1.2 BACE Cleavage of APP as a Molecular Switching Mechanism; 1.3 AD: An Imbalance in Cellular Dependence?; 1.4 BACE Cleavage, Caspase Cleavage, and Neuronal Trophic Dependence; 1.5 BACE Cleavage of APP, Dependence Receptors, and Alzheimer Pathology; 1.6 Key Mutations Proximal of APP Processing to Aβ; 1.7 Final Remarks; CHAPTER 2 IDENTIFICATION OF BACE AS A TARGET IN ALZHEIMER'S DISEASE; 2.1 Introduction; 2.2 The Search for β-Secretase
2.3 Validation of the BACE Target 2.4 Final Remarks; CHAPTER 3 BACE BIOLOGICAL ASSAYS; 3.1 Introduction; 3.2 Clinical and Physiological Hallmarks of Alzheimer's Disease (AD); 3.3 APP Processing; 3.4 Aspartyl Protease Classification; 3.5 BACE Structure; 3.6 Mechanism, Kinetics, Inhibition, and Specificity; 3.7 Assay Strategies for Inhibitor Finding and Development; 3.8 Common Assays Used to Identify and Study Inhibitors; 3.9 BACE Assays; 3.10 Final Remarks; CHAPTER 4 PEPTIDIC, PEPTIDOMIMETIC, AND HTS-DERIVED BACE INHIBITORS; 4.1 Introduction; 4.2 Elan/Pharmacia (Pfizer) 4.3 Oklahoma Medical Research Foundation (OMRF)/Multiple Collaborators 4.4 Eli Lilly; 4.5 Merck; 4.6 GlaxoSmithKline; 4.7 Schering Plough; 4.8 Bristol-Myers Squibb; 4.9 Novartis; 4.10 Amgen; 4.11 Wyeth; 4.12 Final Remarks; CHAPTER 5 FRAGMENT-BASED APPROACHES FOR IDENTIFICATION OF BACE INHIBITORS; 5.1 Introduction; 5.2 Biophysical Methods Applied to BACE Fragment Screens; 5.3 BACE Inhibitors Identified by Fragment Screening; 5.4 Final Remarks; CHAPTER 6 STRUCTURE-BASED DESIGN OF BACE INHIBITORS: TECHNICAL AND PRACTICAL ASPECTS OF PREPARATION, 3-DIMENSIONAL STRUCTURE, AND COMPUTATIONAL ANALYSIS 6.1 Introduction 6.2 Preparation of BACE for Structural Studies; 6.3 Crystallographic Studies of BACE; 6.4 Structural Studies with BACE Inhibitors: Peptidomimetics and Nonpeptidomimetics; 6.5 Computational Approaches; 6.6 Final Remarks; CHAPTER 7 PHARMACOLOGICAL MODELS FOR PRECLINICAL TESTING: FROM MOUSE TO DOG TO NONHUMAN PRIMATES; 7.1 Introduction; 7.2 BACE 1 and Mouse Models of AD; 7.3 Testing BACE Inhibitors in the Canine Model of Human Aging and AD; 7.4 BACE Inhibitors and Nonhuman Primates; 7.5 Final Remarks CHAPTER 8 ADSORPTION, DISTRIBUTION, METABOLISM, EXCRETION (ADME), EFFICACY, AND TOXICOLOGY FOR BACE INHIBITORS 8.1 Introduction; 8.2 Development of BACE Inhibitors with Optimized ADME Properties; 8.3 In Vivo Efficacy of BACE Inhibitors; 8.4 Toxicology of BACE Inhibitors; 8.5 Final Remarks; CHAPTER 9 CLINICAL TRIALS FOR DISEASE-MODIFYING DRUGS SUCH AS BACE INHIBITORS; 9.1 Introduction; 9.2 Update on Beta-Amyloid Therapies in Clinical Development; 9.3 Clinical Development of BACE Inhibitors and Other Disease-Modifying Drugs; 9.4 Final Remarks CHAPTER 10 FUTURE STRATEGIES FOR DEVELOPMENT OF NOVEL BACE INHIBITORS: ANTI-APP β-SITE ANTIBODY AND APP BINDING SMALL MOLECULE APPROACHES FOR ALZHEIMER'S DISEASE |
| Record Nr. | UNINA-9910810075403321 |
| Hoboken, NJ, : John Wiley & Sons, c2010 | ||
| Materiale a stampa | ||
| Lo trovi qui: Univ. Federico II | ||
| ||
