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Record Nr. |
UNINA9910132190803321 |
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Autore |
Ghosh Arun K. |
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Titolo |
Structure-based design of drugs and other bioactive molecules : tools and strategies / / Arun K. Ghosh and Sandra Gemma |
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Pubbl/distr/stampa |
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Weinheim, Germany : , : Wiley-VCH, , 2014 |
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©2014 |
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ISBN |
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3-527-66523-4 |
3-527-66521-8 |
3-527-66524-2 |
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Descrizione fisica |
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1 online resource (476 p.) |
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Disciplina |
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Soggetti |
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Drug development - Data processing |
Bioactive compounds - Analysis |
Biopolymers |
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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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Structure-based Design of Drugs and Other Bioactive Molecules: Tools and Strategies; Contents; Preface; 1 From Traditional Medicine to Modern Drugs: Historical Perspective of Structure-Based Drug Design; 1.1 Introduction; 1.2 Drug Discovery During 1928-1980; 1.3 The Beginning of Structure-Based Drug Design; 1.4 Conclusions; References; Part One: Concepts, Tools, Ligands, and Scaffolds for Structure-Based Design of Inhibitors; 2 Design of Inhibitors of Aspartic Acid Proteases; 2.1 Introduction; 2.2 Design of Peptidomimetic Inhibitors of Aspartic Acid Proteases |
2.3 Design of Statine-Based Inhibitors2.4 Design of Hydroxyethylene Isostere-Based Inhibitors; 2.5 Design of Inhibitors with Hydroxyethylamine Isosteres; 2.5.1 Synthesis of Optically Active α-Aminoalkyl Epoxide; 2.6 Design of (Hydroxyethyl)urea-Based Inhibitors; 2.7 (Hydroxyethyl)sulfonamide-Based Inhibitors; 2.8 Design of Heterocyclic/Nonpeptidomimetic Aspartic Acid Protease Inhibitors; 2.8.1 Hydroxycoumarin- and Hydroxypyrone-Based Inhibitors; 2.8.2 Design of Substituted Piperidine-Based Inhibitors; 2.8.3 Design of |
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Diaminopyrimidine-Based Inhibitors |
2.8.4 Design of Acyl Guanidine-Based Inhibitors2.8.5 Design of Aminopyridine-Based Inhibitors; 2.8.6 Design of Aminoimidazole- and Aminohydantoin-Based Inhibitors; 2.9 Conclusions; References; 3 Design of Serine Protease Inhibitors; 3.1 Introduction; 3.2 Catalytic Mechanism of Serine Protease; 3.3 Types of Serine Protease Inhibitors; 3.4 Halomethyl Ketone-Based Inhibitors; 3.5 Diphenyl Phosphonate-Based Inhibitors; 3.6 Trifluoromethyl Ketone Based Inhibitors; 3.6.1 Synthesis of Trifluoromethyl Ketones; 3.7 Peptidyl Boronic Acid-Based Inhibitors |
3.7.1 Synthesis of α-Aminoalkyl Boronic Acid Derivatives3.8 Peptidyl α-Ketoamide- and α-Ketoheterocycle-Based Inhibitors; 3.8.1 Synthesis of α-Ketoamide and α-Ketoheterocyclic Templates; 3.9 Design of Serine Protease Inhibitors Based Upon Heterocycles; 3.9.1 Isocoumarin-Derived Irreversible Inhibitors; 3.9.2 β-Lactam-Derived Irreversible Inhibitors; 3.10 Reversible/Noncovalent Inhibitors; 3.11 Conclusions; References; 4 Design of Proteasome Inhibitors; 4.1 Introduction; 4.2 Catalytic Mechanism of 20S Proteasome; 4.3 Proteasome Inhibitors; 4.3.1 Development of Boronate Proteasome Inhibitors |
4.3.2 Development of β-Lactone Natural Product-Based Proteasome Inhibitors4.3.3 Development of Epoxy Ketone-Derived Inhibitors; 4.3.4 Noncovalent Proteasome Inhibitors; 4.4 Synthesis of β-Lactone Scaffold; 4.5 Synthesis of Epoxy Ketone Scaffold; 4.6 Conclusions; References; 5 Design of Cysteine Protease Inhibitors; 5.1 Introduction; 5.2 Development of Cysteine Protease Inhibitors with Michael Acceptors; 5.3 Design of Noncovalent Cysteine Protease Inhibitors; 5.4 Conclusions; References; 6 Design of Metalloprotease Inhibitors; 6.1 Introduction; 6.2 Design of Matrix Metalloprotease Inhibitors |
6.3 Design of Inhibitors of Tumor Necrosis Factor-α-Converting Enzymes |
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Sommario/riassunto |
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In contrast to previous texts focusing on either computational, structural or synthetic methods, this one-of-a-kind guide integrates all three skill sets for a complete picture of contemporary structure-based design.As a result, this practical book demonstrates how to develop a high-affinity ligand with drug-like properties for any given drug target for which a high-resolution structure exists. The authors, both of whom have successfully designed drug-like molecules that were later developed into marketed drugs, use numerous examples of recently developed drugs to present best practice in |
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2. |
Record Nr. |
UNINA9910778627103321 |
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Titolo |
The role of small satellites in NASA and NOAA earth observation programs [[electronic resource] /] / Committee on Earth Studies, Space Studies Board, Commission on Physical Sciences, Mathematics, and Applications, National Research Council |
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Pubbl/distr/stampa |
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Washington, D.C., : National Academy Press, c2000 |
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ISBN |
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0-309-18370-7 |
1-280-18552-X |
9786610185528 |
0-309-59409-X |
0-585-25489-3 |
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Descrizione fisica |
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1 online resource (104 p.) |
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Disciplina |
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Soggetti |
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Microspacecraft - United States |
Artificial satellites in earth sciences - United States |
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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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"Support for this project was provided by Contract NASW 96013 between the National Academy of Sciences and the National Aeronautics and Space Administration"--T.p. verso. |
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Nota di bibliografia |
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Includes bibliographical references. |
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Nota di contenuto |
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""THE ROLE OF SMALL SATELLITES IN NASA AND NOAA EARTH OBSERVATION PROGRAMS""; ""Copyright""; ""Foreword""; ""Acknowledgment of Reviewers""; ""Contents""; ""Executive Summary""; ""SMALL SATELLITES VERSUS SMALL MISSIONS""; ""MEETING CORE OBSERVATIONAL NEEDS""; ""CAPABILITY OF SMALL SATELLITES TO PERFORM EARTH OBSERVATION MISSIONS""; ""FLEXIBILITY AND NEW OPPORTUNITIES PROVIDED BY SMALL SATELLITES""; ""AVAILABILITY OF RELIABLE LAUNCH VEHICLES""; ""COST OF SMALL SATELLITE MISSIONS""; ""SENSOR DEVELOPMENT""; ""MISSION ARCHITECTURE""; ""MANAGEMENT OF SMALL SATELLITE PROGRAMS""; ""MISSION PLANNING"" |
""CONCLUSION""""1 Introduction ""; ""REFERENCES""; ""2 Core Observational Needs ""; ""REQUIRED MEASUREMENTS""; ""Measurements in Support of Climate and Global Change Research""; ""Measurements in Support of Operational Applications""; ""CHARACTERIZATION, |
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CALIBRATION, AND VALIDATION""; ""Prelaunch Sensor Characterization""; ""Calibration""; ""Validation""; ""DATA CONTINUITY""; ""Operational Data Continuity""; ""Data Continuity in Research""; ""SIMULTANEITY""; ""SAMPLING ERRORS""; ""SUMMARY""; ""REFERENCES""; ""3 Payload Sensor Characteristics "" |
""PAYLOAD DESIGN AND ACCOMMODATION REQUIREMENTS""""CURRENTLY PLANNED SENSORS""; ""SENSOR COSTS""; ""FUTURE SENSOR DESIGNS: IMPLICATIONS OF ADVANCED TECHNOLOGIES""; ""Size and Design Constraints""; ""Fundamental Limits on Size""; ""Technological Limits on Size""; ""Measurement Strategies and Mission Architectures""; ""SUMMARY""; ""4 Small Satellite Buses ""; ""CAPABILITIES OF SMALL SATELLITE BUSES""; ""SPACECRAFT BUS COSTS""; ""UTILITY OF ""COMMERCIAL"" SPACECRAFT""; ""SPACECRAFT CAPABILITY AS A PAYLOAD DESIGN PARAMETER""; ""PRINCIPAL INVESTIGATOR-LED PROJECTS""; ""FUTURE TRENDS""; ""SUMMARY"" |
""REFERENCES""""5 Small Launch Vehicles""; ""SMALL LAUNCH VEHICLES FOR EOS AND NPOESS""; ""SUMMARY""; ""6 Small Satellites and Mission Architectures ""; ""OPTIONS FOR DISTRIBUTING SENSORS""; ""Single-Sensor Platforms""; ""Multisensor Platforms""; ""Clusters""; ""Constellations""; ""COST-EFFECTIVENESS OF SMALL SATELLITE ARCHITECTURES""; ""Maintenance""; ""NPOESS""; ""EOS""; ""SUMMARY""; ""REFERENCES""; ""7 Opportunities and Challenges in Managing Small Satellite Systems ""; ""PROGRAMMATIC APPROACHES TO TECHNICAL ISSUES""; ""RISKS""; ""Programmatic Risks""; ""Management of Programmatic Risks"" |
""Hidden Programmatic Costs""""Scientific Risks""; ""Management of Scientific Risks""; ""Hidden Scientific Costs""; ""SUMMARY""; ""REFERENCES""; ""8 Findings and Recommendations ""; ""MISSION COSTS""; ""MEETING MISSION GOALS: OPPORTUNITIES WITH SMALL SATELLITES""; ""OPERATIONAL AND RESEARCH EARTH OBSERVATIONS""; ""PAYLOADS""; ""SATELLITE BUSES""; ""LAUNCH VEHICLES""; ""MISSION ARCHITECTURES""; ""SYSTEM MANAGEMENT""; ""SUMMARY""; ""Appendixes""; ""A Statement of Task ""; ""ANALYSIS OF SMALL SATELLITE CAPABILITIES IN LIGHT OF SCIENCE REQUIREMENTS FOR CORE OBSERVATIONAL NEE..."" |
""B Effects of Technology on Sensor Size and Design "" |
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