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Successful drug discovery. Volume 5 [electronic resource] / edited by Janos Fischer, Christian Klein, Wayne E. Childers.

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Bibliographic Details
Online Access: Full Text (via Wiley)
Other Authors: Fischer, János (Editor), Klein, Christian (Editor), Childers, Wayne E. (Editor)
Format: Electronic eBook
Language:English
Published: Weinheim : Wiley-VCH, 2021.
Subjects:
Drug development > History > 21st century.
Drug development.
History.
Table of Contents:
  • Cover
  • Title Page
  • Copyright
  • Contents
  • Advisory Board Members
  • Preface
  • Part I General Aspects
  • Chapter 1 Drug Discovery in Academia
  • 1.1 Introduction
  • 1.2 Repurposing Drugs
  • 1.2.1 Thalidomide Derivatives
  • 1.2.2 Chemotherapy: Nitrogen Mustards
  • 1.3 Pregabalin
  • 1.4 Natural Product-Derived Drug Discovery
  • 1.4.1 Antibiotics
  • 1.4.2 Anticancer Drugs
  • 1.4.2.1 Camptothecin
  • 1.4.2.2 Taxol
  • 1.4.2.3 Epothilones
  • 1.4.2.4 Eribulin
  • 1.4.3 Artemisinin and Artemether
  • 1.4.4 Carfilzomib
  • 1.5 Biologic Drugs
  • 1.5.1 Insulin
  • 1.5.2 Rituximab
  • 1.5.3 Alglucerase.
  • 1.6 Conceptionally New Small Molecule Drugs
  • 1.6.1 Histone Deacetylase Inhibitors
  • 1.6.2 Acyclic Nucleoside Phosphonates
  • 1.6.3 Darunavir
  • 1.6.4 Sunitinib
  • 1.7 Sweet Spot for Academic Drug Discovery
  • List of Abbreviations
  • References
  • Biography
  • Chapter 2 From Degraders to Molecular Glues: New Ways of Breaking Down Disease-Associated Proteins
  • 2.1 Introduction
  • 2.2 Definition and Historical Development of Degraders
  • 2.3 The Ubiquitin-Proteasome System and Considerations of E3 Ligases
  • 2.4 General Design Aspects.
  • 2.5 Differentiation of the Degrader Technology to Traditional Approaches
  • 2.5.1 The Ability to Expand the Druggable Proteome
  • 2.5.2 Overcoming the Accumulation of Target Protein
  • 2.5.3 Abrogating Scaffolding Functions
  • 2.5.4 Creating Target Specificity
  • 2.5.5 Catalytic Mode of Action
  • 2.5.6 Event-Driven Pharmacology and Prolonged PD Effect
  • 2.6 Potential Disadvantages and Limitations of Degraders
  • 2.7 Molecular Glue-like Degraders and Monovalent Degraders
  • 2.7.1 Definitions and Historical Perspective
  • 2.7.2 State of the Art
  • 2.8 Future Directions (Status Q3 2020)
  • 2.9 Summary and Conclusions
  • Acknowledgments
  • List of Abbreviations
  • References
  • Biographies
  • Part II Drug Class Studies
  • Chapter 3 GLP-1 Receptor Agonists for the Treatment of Type 2 Diabetes and Obesity
  • 3.1 Introduction
  • 3.2 GLP-1 Biology
  • 3.2.1 GLP-1 Receptor Binding and Activation
  • 3.2.2 GLP-1 Pharmaceutical Developments
  • 3.3 Ex4-Based Analogues
  • 3.3.1 Exenatide
  • 3.3.2 Exenatide LAR
  • 3.3.3 Lixisenatide
  • 3.3.4 Efpeglenatide
  • 3.3.5 Pegylated Loxenatide
  • 3.4 GLP-1 Based Analogues
  • 3.4.1 Liraglutide
  • 3.4.2 Semaglutide
  • 3.4.3 Taspoglutide.
  • 3.4.4 Albiglutide and Albenatide
  • 3.4.5 Dulaglutide
  • 3.5 Co-agonists
  • 3.5.1 GLP-1/GIP Co-agonists
  • 3.5.2 GLP-1/Glucagon Co-agonists
  • 3.5.2.1 Other GLP-1R Agonists
  • 3.6 Summary
  • List of Abbreviations
  • References
  • Biographies
  • Chapter 4 Recent Advances on SGLT2 Inhibitors: Synthetic Approaches, Therapeutic Benefits, and Adverse Events
  • 4.1 Introduction
  • 4.2 The Mechanism of Action of SGLT2 Inhibitors
  • 4.3 Synthetic Approaches to Gliflozins
  • 4.3.1 Dapagliflozin
  • 4.3.2 Sotagliflozin
  • 4.3.3 Empagliflozin
  • 4.3.4 Bexagliflozin
  • 4.3.5 Luseogliflozin.
  • 4.3.6 Tofogliflozin.

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