Introduction to biological and small molecule drug research and development : theory and case studies /

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The fundamental concept of the book is to provide, for the first time, an introduction to understand the science behind successful pharmaceutical research and development programs. As well as explaining the basic principles, the book compares and contrasts approaches to both biopharmaceuticals (prot...

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Detalles Bibliográficos
Clasificación:Libro Electrónico
Otros Autores: Ganellin, C. R. (C. Robin) (Editor ), Roberts, Stanley (Chemist) (Editor ), Jefferis, Roy (Editor )
Formato: Electrónico eBook
Idioma:Inglés
Publicado: Waltham, MA : Academic Press, 2013.
Temas:
Drugs > Research.
Drug Discovery
Biopharmaceutics > methods
Small Molecule Libraries
Médicaments > Recherche.
MEDICAL > Drug Guides.
MEDICAL > Nursing > Pharmacology.
MEDICAL > Pharmacology.
MEDICAL > Pharmacy.
Drugs > Research
Internet Resources.
Charts.
Plates.
Acceso en línea:Texto completo
Tabla de Contenidos:
  • Note continued: References
  • 13.1. Introduction
  • 13.2. The Target Enzyme: HIV-1 Aspartic Acid Protease
  • 13.3. Advent of Protease Inhibitors, HAART, and Structural Insights from S aquinavir
  • 13.4. Cyclic Ethers to Mimic Peptide Bonds: Inspiration from Natural Products
  • 13.5. Design of Conceptually New Cyclic Ether-derived Ligands and Corresponding Protease Inhibitors
  • 13.5.1. Exploration of ligands from cyclic ethers to cyclic sulfones
  • 13.5.2. Design and development of bicyclic bis-tetrahydrofuran (bis-THF) ligand
  • 13.6. Design Strategy to Combat Drug Resistance by Targeting Protein Backbone: 'Backbone Binding Concept'
  • 13.7. Design of PIs Promoting Strong Backbone Interactions from S2 to S2 Subsites
  • 13.8. The 'Backbone Binding Concept' and Its Relevance to Combat Drug Resistance
  • 13.9. Selection of Darunavir as a Promising Drug Candidate
  • 13.9.1. Thermodynamic and kinetic effects behind darunavir's high binding affinity for the protease
  • 13.9.2. Darunavir inhibits HIV-1 protease dimerization: a unique dual mode of action
  • 13.10. Convenient Syntheses of the bis-THF Ligand
  • 13.11. Clinical Use of Darunavir in the Management of HIV-1 Infection
  • 13.12. Design of Potent Inhibitors Targeting the Protease Backbone
  • 13.13. Conclusion
  • References
  • 14.1. The Story of anti-TNF: From Septic Shock to Inflammatory Diseases
  • 14.2. From a Clinically Validated Target to the Design of anti-TNF Biopharmaceuticals
  • 14.2.1. Development of anti-TNF-cc mAbs
  • 14.2.2. Development of soluble receptors
  • 14.3. Marketing Approvals and Post-Marketing Clinical Experience
  • 14.3.1. Efficacy (biomarkers and sequential treatment)
  • 14.3.2. Tolerance
  • 14.4. Structure-Clinical Activities Relationships Drawn from the Clinical Experience
  • 14.4.1. Immunogenicity
  • 14.4.2.mAbs, granulomas, and membrane TNF
  • 14.5. Conclusions
  • References
  • 15.1. Introduction
  • 15.2. Past Approaches to Lowering Levels of Circulating Cholesterol
  • 15.2.1. Bile acid sequestrants
  • 15.2.2. Hypocholesterolaemic drugs
  • 15.2.3. Inhibition of cholesterol absorption by fibrates: inhibitors of ACAT
  • 15.2.4. Statins: inhibitors of HMG-CoA reductase
  • 15.2.5. Inhibition of cholesterol absorption by saponins
  • 15.3. Further Work on ACAT Inhibitors
  • 15.4. Inhibition of a Novel Mechanism for Cholesterol Uptake and the Discovery of SCH 48461
  • 15.5. Design of Ezetimibe (SCH 58235)
  • 15.6. Ezetimibe in Human Studies
  • 15.7. Identification of a New Mechanism for Cholesterol Uptake
  • 15.8. Conclusion
  • References.

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