LEADER 06502nam 22005173 450 001 9911020083103321 005 20230812060236.0 010 $a9781394207145 010 $a139420714X 010 $a9781394207091 010 $a1394207093 035 $a(MiAaPQ)EBC30682641 035 $a(Au-PeEL)EBL30682641 035 $a(CKB)27962326400041 035 $a(Exl-AI)30682641 035 $a(Perlego)4208585 035 $a(EXLCZ)9927962326400041 100 $a20230812d2023 uy 0 101 0 $aeng 135 $aurcnu|||||||| 181 $ctxt$2rdacontent 182 $cc$2rdamedia 183 $acr$2rdacarrier 200 10$aMolecules Engineered Against Oncogenic Proteins and Cancer $eDiscovery, Design, and Development 205 $a1st ed. 210 1$aNewark :$cJohn Wiley & Sons, Incorporated,$d2023. 210 4$dİ2023. 215 $a1 online resource (391 pages) 311 08$aPrint version: Corey, E. J. Molecules Engineered Against Oncogenic Proteins and Cancer Newark : John Wiley & Sons, Incorporated,c2023 9781394207084 327 $aCover -- 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*. 327 $a11.3 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. 327 $aAppendix 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 & -- A Transactions Driven by Oncology-focused Kinase and KRAS Inhibitors -- Appendix 5. Alphabetic List of Oncogenic Protein Inhibitors -- EULA. 330 $aThis 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.$7Generated by AI. 606 $aProtein kinases$xInhibitors$7Generated by AI 606 $aOncogenes$7Generated by AI 615 0$aProtein kinases$xInhibitors 615 0$aOncogenes 700 $aCorey$b E. J$020674 701 $aWu$b Yong-Jin$01838661 801 0$bMiAaPQ 801 1$bMiAaPQ 801 2$bMiAaPQ 906 $aBOOK 912 $a9911020083103321 996 $aMolecules Engineered Against Oncogenic Proteins and Cancer$94417695 997 $aUNINA