06502nam 22005173 450 991102008310332120230812060236.09781394207145139420714X97813942070911394207093(MiAaPQ)EBC30682641(Au-PeEL)EBL30682641(CKB)27962326400041(Exl-AI)30682641(Perlego)4208585(EXLCZ)992796232640004120230812d2023 uy 0engurcnu||||||||txtrdacontentcrdamediacrrdacarrierMolecules Engineered Against Oncogenic Proteins and Cancer Discovery, Design, and Development1st ed.Newark :John Wiley & Sons, Incorporated,2023.©2023.1 online resource (391 pages)Print version: Corey, E. J. Molecules Engineered Against Oncogenic Proteins and Cancer Newark : John Wiley & Sons, Incorporated,c2023 9781394207084 Cover -- Title Page -- Copyright -- Contents -- Preface -- Chapter 1. Introduction -- 1.1 Types of Protein Kinases -- 1.2 Protein Kinase Domains -- 1.3 ATP-Binding Site -- 1.4 Types of Kinase Inhibitors -- 1.5 Brief History of Small-molecule kinase Inhibitors -- 1.6 Peak 12-Month Sales for Leading Kinase Inhibitors -- 1.7 Approved Kinase Inhibitors -- Chapter 2. BCR-ABL Inhibitors -- 2.1 Imatinib* -- 2.2 Nilotinib* -- 2.3 Dasatinib* -- 2.4 Bosutinib* -- 2.5 Ponatinib* -- 2.6 Olvermbatinib** -- 2.7 Asciminib* -- Chapter 3. BTK Inhibitors -- 3.1 Ibrutinib* -- 3.2 Acalabrutinib* -- 3.3 Zanubrutinib* -- 3.4 Tirabrutinib** -- 3.5 Orelabrutinib** -- Chapter 4. EGFR/HER Family Inhibitors -- 4.1 Gefitinib* -- 4.2 Erlotinib * -- 4.3 Icotinib** -- 4.4 Afatinib* -- 4.5 Dacomitinib* -- 4.6 Osimertinib* -- 4.7 Mobocertinib* -- 4.8 Lapatinib* -- 4.9 Tucatinib* -- 4.10 Neratinib* -- Chapter 5. VEGFR/Multikinase Inhibitors -- 5.1 Sorafenib* -- 5.2 Regorafenib* -- 5.3 Sunitinib* -- 5.4 Pazopanib* -- 5.5 Axitinib* -- 5.6 Nintedanib* -- 5.7 Apatinib** -- 5.8 Lenvatinib* -- 5.9 Tovozanib* -- Chapter 6. CDK4/6 Inhibitors -- 6.1 Palbociclib* -- 6.2 Ribociclib* -- 6.3 Abemaciclib* -- 6.4 Trilaciclib* -- Chapter 7. JAK Inhibitors -- 7.1 Tofacitinib* -- 7.2 Baricitinib* -- 7.3 Peficitinib** -- 7.4 Upadacitinib* -- 7.5 Delgocitinib** -- 7.6 Filgotinib** -- 7.7 Abrocitinib* -- 7.8 Ruxolitinib* -- 7.9 Fedratinib* -- 7.10 Pacritinib* -- 7.11 Ritlecitinib# -- 7.12 Brepocitinib# -- 7.13 Ropsacitinib# -- Chapter 8. Allosteric TYK2 Inhibitors -- 8.1 Deucravacitinib* -- Chapter 9. ALK/multikinase Inhibitors -- 9.1 Crizotinib* -- 9.2 Ceritinib* -- 9.3 Alectinib* -- 9.4 Brigatinib* -- 9.5 Lorlatinib* -- Chapter 10. BRAF/Multikinase Inhibitors -- 10.1 Vemurafenib* -- 10.2 Dabrafenib* -- 10.3 Encorafenib* -- Chapter 11. MEK Inhibitors -- 11.1 Trametinib* -- 11.2 Cobimetinib*.11.3 Binimetinib* -- 11.4 Selumetinib* -- Chapter 12. RET/Multikinase Inhibitors -- 12.1 Vandetanib* -- 12.2 Cabozantinib* -- 12.3 Selpercatinib* -- 12.4 Pralsetinib* -- Chapter 13. FGFR Inhibitors -- 13.1 Erdafitinib* -- 13.2 Pemigatinib* -- 13.3 Infigratinib* -- 13.4 Futibatinib* -- Chapter 14. PI3K Inhibitors -- 14.1 Alpelisib* -- 14.2 Idelalisib* -- 14.3 Duvelisib* -- 14.4 Umbralisib* -- 14.5 Copanlisib* -- Chapter 15. TRK/Multikinase Inhibitors -- 15.1 Larotrectinib* -- 15.2 Entrectinib* -- 15.3 Repotrectinib# -- Chapter 16. MET Inhibitors -- 16.1 Capmatinib* -- 16.2 Tepotinib* -- Chapter 17. KIT/PDGFR/Multkinase Inhibitors -- 17.1 Avapritinib* -- 17.2 Ripretinib* -- Chapter 18. FLT3 Inhibitors -- 18.1 Midostaurin* -- 18.2 Gilteritinib* -- Chapter 19. mTOR Inhibitors -- 19.1 Sirolimus* and Analogs -- Chapter 20. Other Kinase Inhibitors -- 20.1 Netarsudil* -- 20.2 Belumosudil* -- 20.3 Fostamatinib* -- 20.4 Pexidartinib* -- Chapter 21. KRAS Inhibitors -- 21.1 Sotorasib* -- 21.2 Adagrasib* -- 21.3 JDQ443# -- Chapter 22. An Overview of the Discovery Process for Medically Useful Inhibitors of Oncogenic Protein Kinases -- 22.1 High-quality Leads -- 22.2 Integrating Substructures from Different High Quality Leads or Established Inhibitors -- 22.3 Variation of Hinge-binding Nucleus -- 22.4 Macrocyclization -- 22.5 Fragment-based Approach -- 22.6 Covalent Inhibitors -- 22.7 Strategic Structural Modification of Prior Drugs -- 22.8 Exploiting Specific Kinase Pocket to Optimize Selectivity -- 22.9 Solvent-exposed Appendages to Enhance Solubility and PK Properties -- Chapter 23. Targeted Molecular Anticancer Therapies - Successes and Challenges -- 23.1 The Beginning -- 23.2 Further Developments -- 23.3 Biomarker-driven Drug Development -- 23.4 Mitigation of Drug Resistance -- 23.5 Miscellaneous Approaches -- 23.6 Discovery Chemistry.Appendix 1. First FDA Approvals by Year -- Appendix 2. Kinase/KRAS Inhibitors in Development -- Appendix 3. Visualization of Differentially Expressed Kinases in Cancer -- Appendix 4. M &amp -- A Transactions Driven by Oncology-focused Kinase and KRAS Inhibitors -- Appendix 5. Alphabetic List of Oncogenic Protein Inhibitors -- EULA.This book provides a comprehensive examination of recent scientific advancements in cancer treatment, focusing on the development of molecular therapies targeting oncogenic proteins. Authored by E. J. Corey and Yong-Jin Wu, it explores the transformation in cancer therapy over the last 30 years through the introduction of nearly 80 FDA-approved synthetic compounds. These compounds specifically target mutated biomolecules responsible for cancer, differing significantly from older cytotoxic agents. The book discusses the role of protein kinases, a class of enzymes integral to cell growth regulation, in cancer proliferation, and highlights the pivotal scientific research enabling these breakthroughs. It is intended for researchers, medical professionals, and students interested in oncology, molecular biology, and drug development.Generated by AI.Protein kinasesInhibitorsGenerated by AIOncogenesGenerated by AIProtein kinasesInhibitorsOncogenesCorey E. J20674Wu Yong-Jin1838661MiAaPQMiAaPQMiAaPQBOOK9911020083103321Molecules Engineered Against Oncogenic Proteins and Cancer4417695UNINA