Successful drug discovery. Volume 5

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Title:

Author:

Fischer, János, editor.

ISBN:

9783527826872

9783527826858

9783527826865

Publication Information:

Weinheim : Wiley-VCH, 2021.

Physical Description:

1 online resource (317 pages)

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.

Abstract:

In the fifth volume of Successful Drug Discovery, the inventors and primary developers of drugs that made it to the market tell the story of the drug's discovery and development. Case studies of drugs from different therapeutic fields reveal the all-too-often unpredictable path from the first drug candidate molecule to the successfully marketed drug. In addition, this new volume addresses overarching topics for drug discovery, such as drug discovery in academia, and discusses currently important classes of small molecule as well as biological drugs. Comprehensive in scope, the book's nine chapters provide a representative cross-section of the present-day drug development effort.

Local Note:

John Wiley and Sons

Subject Term:

Drug development -- History -- 21st century.

Médicaments -- Développement -- Histoire -- 21e siècle.

Genre:

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