Reviews: 2020 Medicinal Chemistry Reviews

1. Where it All Began
2. Organic Chemistry or Bust
3. Ah, Research!
4. Off to Graduate School, Part I
5. Uncle Sam Wanted Me
6. Off to Graduate School, Part II
7. Change in Career Path
8. Where the New Career Began
9. Research Projects Pursued
10. Epilogue

1. The Early Days
2. Becoming a Researcher
3. Becoming a Drug Hunter
4. The Power of Human Genetics
5. Becoming a Leader
6. Collaboration, Proactivity, and its Consequences
7. The Challenge of Global Leadership
8. Can I Make the Transition?
9. Helping to Make a Biotech: Science, Pipeline, and Culture
10. Closing Thoughts

1. Introduction
2. Inflammosome Biology
3. The Role of Kinases in Neuroinflammation
4. Medicinal Chemistry of Specific Targets
5. Summary and Outlook

1. Introduction
2. Therapeutic Areas for Intervention
3. Biased Opioid Signaling
4. Recent Advances in KOR and MOR Ligands
5. PET Tracers
6. Conclusion

1. Introduction
2. Existing Models for Cardiac Safety Assessment
3. Design Considerations
4. Cell Source
5. Assembly
6. Testing Capabilities
7. Emerging Technologies
8. Limitations
9. Conclusion

1. Introduction
2. Small-Molecule, Heme-Dependent Stimulators of sGC in Cardiovascular Diseases (Heart Failure and Pulmonary Hypertension)
3. Small-Molecule, Heme-Independent Activators of sGC in
4. Conclusion

1. Introduction
2. CP-456,773 and Other Sulfonylureas
3. Next-Generation Inhibitors
4. Clinical Progress
5. Conclusions

1. Introduction
2. Discovery and Development of Clinical Non-Covalent BTK Inhibitors for Autoimmune Diseases
3. Discovery and Development of Clinical Covalent BTK Inhibitors for Autoimmune Diseases
4. BTK Inhibitors in Early Development for Autoimmune Diseases
5. Conclusion

1. Introduction
2. Oligodeoxyribonucleotides (ODNs)
3. Oligoribonucleotides (ORNs)
4. Small-Molecule Antagonists
5. Conclusion

1. Introduction
2. Screening Approaches to Identify Covalent Inhibitor Leads
3. Clinical Candidates, Preclinical Programs, and Patent Disclosures
4. Emerging Approaches
5. Clinical Findings
6. Conclusions

1. Introduction: SHP2 in Cancer Biology
2. Drug Discovery Strategies for SHP2
3. Patent and Clinical Disclosures
4. Conclusions

1. Introduction
2. Structure and Function
3. Trk Biology in Cancer
4. Trk Inhibitors in Cancer
5. Approved Trk Inhibitors and Outlook on Next-Generation Molecules
6. Future Directions

1. Introduction
2. Recent Advances in the Discovery of Small-Molecule Catalytic Inhibitors of EZH2
3. EED Ligands
4. Other Modes of Targeting EZH2 and/or EED
5. Clinical Compounds
6. Conclusions

1. Introduction
2. Selected Clinically Relevant Polymicrobial Communities
3. Modulation of Quorum Signaling and Therapeutic Potential in Polymicrobial Settings
4. Conclusions

1. Introduction
2. Kinetic Selectivity
3. The Post-Antibiotic Effect and In Vivo PD of Current Antibiotic Classes
4. Conclusion

1. Introduction and Historical Perspective
2. Practical Considerations
3. Long-Acting Injectables by Indication
4. Conclusion

1. Introduction
2. Nuclear Transport Mechanisms
3. Nuclear Export Inhibitors (NEIs)
4. Conclusions

1. Introduction to Proteasome Activation
2. Modes of Action for Proteasome Activation
3. Case Studies
4. Conclusions and Future Outlook

1. Introduction to RNA Epigenetics
2. RNA Modifications
3. RNA-Modifying Enzymes and Links to Disease
4. Methods of Detection and Quantification
5. General Features of RNA-Modifying Enzymes
6. Families of RNA-Modifying Enzymes and their Inhibitors
7. Future Outlook
8. Late-Breaking News

1. Introduction
2. Therapeutic Potential of TBK1/IKKε Inhibition
3. Inhibitors of TBK1/IKKε
4. Drug Development in the Field of TBK1/IKKε Inhibition
5 Conclusions and Future Perspective

1. Introduction
2. Strategies for Achieving Selectivity for Bruton’s Tyrosine Kinase
3. Second-Generation Irreversible Covalent Inhibitors Approved and in Development
4. Conclusion

1. Introduction
2. Ubiquitin-Proteasome System (UPS) and Protein Degradation
3. PROteolysis TArgeting Chimeras (PROTACs) Targeting Protein Kinases
4. Conclusions

1. Introduction
2. Practical Aspects of Affinity DEL Screening
3. Lessons from Published Examples of Optimized DEL Hit Molecules
4. One-Bead-One-Compound DELs and Activity-Based Screening
5. Conclusions

1. Introduction
2. Smallpox Disease
3. Discovery of Tecovirimat
4. CMC and Safety Pharmacology
5. Early Clinical Studies
6. Registrational Studies under the “Animal Efficacy Rule”
7. Conclusion

1. Introduction
2. Pathophysiology of Atopic Dermatitis and the Role of PDE4
3. Medicinal Chemistry Efforts Leading to the Discovery of Crisaborole
4. Preclinical Pharmacological Characterization of Crisaborole
5. Clinical Data on Eucrisa®
6. Conclusions

1. Afamelanotide (erythropoietic protoporphyria)
2. Alpelisib (anticancer)
3. Bremelanotide (hypoactive sexual desire)
4. Brexanolone (postpartum depression)
5. Cefiderocol (antibacterial)
6. Cenobamate (anticonvulsant)
7. Darolutamide (anticancer)
8. Elexacaftor (cystic fibrosis)
9. Entrectinib (anticancer)
10. Erdafitinib (anticancer)
11. Esaxerenone (hypertension)
12. Fedratinib (anticancer)
13. Fexinidazole (antiparasitic)
14. Flumatinib (anticancer)
15. Lascufloxacin (antibacterial)
16. Lasmiditan (migraine)
17. Lefamulin (antibacterial)
18. Lemborexant (insomnia)
19. Lumateperone (schizophrenia)
20. Mirogabalin (neuropathic pain)
21. Pexidartinib (anticancer)
22. Pretomanid (antibacterial)
23. Quizartinib (anticancer)
24. Relebactam (antibacterial)
25. Relugolix (uterine fibroids)
26. Remimazolam (anesthetic)
27. Remogliflozin etabonate (diabetes)
28. Selinexor (anticancer)
29. Siponimod (multiple sclerosis)
30. Solriamfetol (narcolepsy)
31. Sotagliflozin (diabetes)
32. Tapinarof (psoriasis)
33. Tenapanor (irritable bowel syndrome)
34. Triclabendazole (antiparasitic)
35. Trifarotene (acne)
36. Ubrogepant (migraine)
37. Upadacitinib (rheumatoid arthritis)
38. Voxelotor (sickle cell disease)
39. Zanubrutinib (anticancer)

1. Brolucizumab (ophthalmology; wet macular degeneration)
2. Camrelizumab (anticancer; Hodgkin’s lymphoma)
3. Crizanlizumab (genetic diseases; sickle cell disease)
4. Enfortumab Vedotin (anticancer; urothelial cancer)
5. Fam-Trastuzumab Deruxtecan (anticancer; breast cancer)
6. Givosiran (genetic diseases; acute hepatic porphyria)
7. Golodirsen (genetic diseases; Duchenne muscular dystrophy)
8. Netakimab (immunology and inflammation; plaque psoriasis)
9. Polatuzumab Vedotin (anticancer; diffuse large B-cell lymphoma)
10. Rabimabs (infectious disease; rabies post-exposure prophylaxis)
11. Risankizumab (immunology and inflammation; plaque psoriasis)
12. Romosozumab (musculoskeletal disease; osteoporosis)
13. Sintilimab (anticancer; Hodgkin’s lymphoma)
14. Tislelizumab (anticancer; Hodgkin’s lymphoma)
15. Toripalimab (anticancer; melanoma)
16. Volanesorsen (genetic diseases; familial chylomicronemia syndrome)