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Record Nr. |
UNINA9910829994603321 |
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Titolo |
Aspartic acid proteases as therapeutic targets / / edited by Arun K. Ghosh |
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Pubbl/distr/stampa |
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Weinheim, Germany : , : Wiley-VCH, , 2010 |
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©2010 |
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ISBN |
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1-282-77490-5 |
9786612774904 |
3-527-64162-9 |
3-527-63094-5 |
3-527-63095-3 |
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Descrizione fisica |
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1 online resource (641 p.) |
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Collana |
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Methods and Principles in Medicinal Chemistry ; ; Volume 45 |
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Disciplina |
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Soggetti |
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Aspartic proteinases |
Aspartic proteinases - Inhibitors - Therapeutic use |
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Lingua di pubblicazione |
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Formato |
Materiale a stampa |
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Livello bibliografico |
Monografia |
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Note generali |
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Description based upon print version of record. |
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Nota di bibliografia |
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Includes bibliographical references at the end of each chapters and index. |
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Nota di contenuto |
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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 |
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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 |
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Sommario/riassunto |
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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 |
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