Kinase Targets and Drug Discovery covers the critical role of kinases as regulators of cellular functions and their implications in a range of diseases, from cancers to cardiovascular disorders and inflammatory conditions. Readers will explore foundational concepts on the functions of kinases, the role of kinase inhibitors in disease therapy, and challenges faced. The second section focuses on innovative strategies in kinase drug discovery, covering screening and computational approaches, along with the development of covalent, macrocyclic, allosteric inhibitors, and kinase degraders. Final sections examine clinical applications, detailing how kinase inhibition can be harnessed for cancer therapies, non-oncologic diseases, and even non-catalytic functions.
This book will serve as an indispensable resource for pharmacologists, medicinal chemists, and researchers in both academia and industry. By bridging the gap between foundational research and clinical application, it equips professionals with the latest insights and practical approaches to advance their understanding to contribute meaningfully to the evolving landscape of drug discovery.
1. Chapter 1. Introduction to kinases and their functions - p. 3 2. Chapter 2. Kinase inhibitors in diseases therapy - p. 31 3. Chapter 3. Challenges in kinase inhibitors discovery - p. 59 4. Part II: Strategies in kinase drug discovery - p. P77 5. Chapter 4. Screening approaches for kinases - p. 79 6. Chapter 5. Computational approaches for kinase inhibitors - p. 107 7. Chapter 6. Covalent inhibitors of kinases - p. 133 8. Chapter 7. Small macrocyclic inhibitors of kinase - p. 163 9. Chapter 8. Allosteric targeting of protein kinases: mechanisms and computational design strategies - p. 191 10. Chapter 9. Kinase degrader: a new era of drug development - p. 225 11. Chapter 10. Small-molecule kinase activators - p. 251 12. Part III: Clinical indications for kinase inhibitors - p. P275 13. Chapter 11. Kinase inhibitors as anticancer drugs - p. 277 14. Chapter 12. Kinase inhibition for nononcologic diseases - p. 305 15. Chapter 13. Kinase inhibition for noncatalytic function - p. 335 16. Index - p. 351
Kinase Targets and Drug Discovery covers the critical role of kinases as regulators of cellular functions and their implications in a range of diseases, from cancers to cardiovascular disorders and inflammatory conditions. Readers will explore foundational concepts on the functions of kinases, the role of kinase inhibitors in disease therapy, and challenges faced. The second section focuses on innovative strategies in kinase drug discovery, covering screening and computational approaches, along with the development of covalent, macrocyclic, allosteric inhibitors, and kinase degraders. Final sections examine clinical applications, detailing how kinase inhibition can be harnessed for cancer therapies, non-oncologic diseases, and even non-catalytic functions.
This book will serve as an indispensable resource for pharmacologists, medicinal chemists, and researchers in both academia and industry. By bridging the gap between foundational research and clinical application, it equips professionals with the latest insights and practical approaches to advance their understanding to contribute meaningfully to the evolving landscape of drug discovery.
1. Chapter 1. Introduction to kinases and their functions - p. 3 2. Chapter 2. Kinase inhibitors in diseases therapy - p. 31 3. Chapter 3. Challenges in kinase inhibitors discovery - p. 59 4. Part II: Strategies in kinase drug discovery - p. P77 5. Chapter 4. Screening approaches for kinases - p. 79 6. Chapter 5. Computational approaches for kinase inhibitors - p. 107 7. Chapter 6. Covalent inhibitors of kinases - p. 133 8. Chapter 7. Small macrocyclic inhibitors of kinase - p. 163 9. Chapter 8. Allosteric targeting of protein kinases: mechanisms and computational design strategies - p. 191 10. Chapter 9. Kinase degrader: a new era of drug development - p. 225 11. Chapter 10. Small-molecule kinase activators - p. 251 12. Part III: Clinical indications for kinase inhibitors - p. P275 13. Chapter 11. Kinase inhibitors as anticancer drugs - p. 277 14. Chapter 12. Kinase inhibition for nononcologic diseases - p. 305 15. Chapter 13. Kinase inhibition for noncatalytic function - p. 335 16. Index - p. 351
