| Description |
1 online resource (viii, 381 pages) : color illustrations |
| Contents |
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* |
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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* |
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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* |
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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* |
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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# |
| Summary |
Featuring 91 total small molecule kinase/KRAS inhibitors, 80 of which are FDA-approved, Molecules Engineered Against Oncogenic Proteins and Cancer documents the recent scientific advances that have transformed one of medicine's most challenging areas - cancer treatment. Most of these inhibitors specifically block oncogene-induced carcinogenic proteins with results that have dramatically advanced the treatment of cancer. In addition, the structural formulas of more than 100 kinase/KRAS inhibitors in clinical trials are presented. Molecules Engineered Against Oncogenic Proteins and Cancer includes information on: Each molecule's structure, function of the kinase target and relevance to cancer, the drug discovery process, and molecular details of drug action; Mutated protein kinases as oncoproteins and targets for inhibition, along with the details of discovery for each antitumor antikinase agent; History of oncoprotein inhibitors and their role in advancing the treatment and understanding of cancer; and The discovery process as a whole, effective strategies for innovation, ongoing challenges, and a glimpse of the future of the field |
| Bibliography |
Includes bibliographical references and index |
| Notes |
Chapter 22. An Overview of the Discovery Process for Medically Useful Inhibitors of Oncogenic Protein Kinases |
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Description based on online resource; title from digital title page (viewed on September 21, 2023) |
| Subject |
Protein-tyrosine kinase -- Inhibitors -- Therapeutic use
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Carcinogenesis -- Molecular aspects.
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Cancer -- Treatment.
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| Form |
Electronic book
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| Author |
Wu, Yong-Jin, author
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| ISBN |
9781394207145 |
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139420714X |
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9781394207091 |
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1394207093 |
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9781394207107 |
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1394207107 |
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