href="#ulink_4bcad8b0-7427-5d85-bf17-3f7a6b97591f">9.1 Introduction 9.2 G Protein‐Coupled Receptor Structure‐Based Drug Discovery 9.3 The Beginning of the Family B GPCR Structural Biology Revolution 9.4 Lessons Learned from the Corticotropin‐Releasing Factor Receptor Type 1 Crystal Structure 9.5 Structural Understanding of Glucagon and GLP1 Receptor Activation 9.6 Hyperinsulinemic Hypoglycemia 9.7 GLP1 Receptor Negative Allosteric Modulator Lead Identification 9.8 GLP1 Receptor Negative Allosteric Modulator Lead Optimization 9.9 Conclusion References
15 10 Discovery and Potential Application of [11 C]MK‐6884 10.1 Introduction 10.2 Discovery of a Selective PET Tracer for M4 PAM 10.3 A PET Tracer that Images M4 in Rat 10.4 Characterization of [11C]10 as a PET Tracer Preclinical Candidate for Human Use 10.5 Development of [11C]MK‐6884 Acknowledgement References
16 11 Targeted Protein Degradation by Proteolysis Targeting Chimeras: A Revolution in Small Molecule Drug Discovery 11.1 The Concept of Targeted Protein Degradation 11.2 Advances with PROTACs 11.3 Pharmacokinetics and Oral Absorption Challenge 11.4 PROTACs in Clinical Development 11.5 Challenges and Perspectives Acknowledgement References
17 12 Entrepreneurial Drug Hunter 12.1 Introduction 12.2 Macrocyclic Peptide Modalities in Retrospect 12.3 Receptor and Extracellularly Targeted Macrocyclic Peptides 12.4 Intracellular Protein–Protein Interaction Targeted Macrocyclic Peptides 12.5 Macrocyclic Peptide Advancement to Clinical Development and FDA Approval 12.6 Macrocyclic Peptide Drug Discovery Paradigm and Future Directions Acknowledgements References
18 13 Application of Pyrrolobenzodiazepines in Antibody Drug Conjugates 13.1 Introduction 13.2 Antibody Drug Conjugating with Pyrrolobenzodiazepine Payloads 13.3 Small Molecule Drug Conjugates with Pro‐Pyrrolobenzodiazepine Payloads 13.4 Discussion 13.5 Conclusion References
19 14 Combination Therapy Case Studies in Anticancer and Anti‐Infectious Disease Drug Discovery and Development 14.1 Introduction 14.2 Case Study of Olaparib (Lynparza®) and Bevacizumab (Avastin®) Combination in the Treatment of Advanced Ovarian Cancer 14.3 Case Study of Ceftazidime and Avibactam Combination (Avycaz®) in the Treatment of Complicated Urinary Tract Infections and Intra‐abdominal Infections 14.4 Combination Therapy Future Perspectives References
20 15 Accelerating Drug Discovery and Development 15.1 Introduction to Translational Medicine 15.2 From Bench to Bedside: Translating Basic Research into Desirable Clinical Outcomes for COVID‐19 Treatments 15.3 From Bedside to Bench: Accelerating Drug Discovery and Development in Treating COVID‐19 15.4 Translational Medicine Summary References
21 Appendix A: Appendix AMonoclonal Antibody Drug Discovery and Development Paradigm
22 Appendix B: Appendix BGlossary
23 Appendix C: Appendix CAbbreviations
24 Index
List of Tables
1 Chapter 3Table 3.1 Hemodynamic changes and QoL at 16 weeks in patients with high vs ...Table 3.2 Properties of the N‐substituted methyl carbamates 1, 3–9.Table 3.3 Properties of the