Molecules engineered against oncogenic proteins and cancer : discovery, design, and development /: discovery, design, and development. (2023)

• Record Type: Book
• Further Information: Note: E.J. Corey, Yong-Jin Wu.
• Authors: Corey, E. J; Wu, Yong-Jin
• Contents: Preface vii Chapter 1. Introduction 1 1.1 Types of Protein Kinases 1 1.2 Protein Kinase Domains 1 1.3 ATP-Binding Site 2 1.4 Types of Kinase Inhibitors 3 1.5 Brief History of Smallmolecule Kinase Inhibitors 5 1.6 Peak 12-Month Sales for Leading Kinase Inhibitors 7 1.7 Approved Kinase Inhibitors 7 Chapter 2. BCR-ABL Inhibitors 18 2.1 Imatinib* (1) 19 2.2 Nilotinib* (2) 24 2.3 Dasatinib* (3) 27 2.4 Bosutinib* (4) 30 2.5 Ponatinib* (5) 33 2.6 Olvermbatinib** (6) 37 2.7 Asciminib* (7) 38 Chapter 3. BTK Inhibitors 43 3.1 Ibrutinib* (8) 45 3.2 Acalabrutinib* (9) 51 3.3 Zanubrutinib* (10) 54 3.4 Tirabrutinib** (11) 57 3.5 Orelabrutinib** (12) 58 Chapter 4. EGFR/HER Family Inhibitors 59 4.1 Gefitinib* (13) 61 4.2 Erlotinib * (14) 67 4.3 Icotinib** (15) 72 4.4 Afatinib* (16) 74 4.5 Dacomitinib* (17) 77 4.6 Osimertinib* (18) 80 4.7 Mobocertinib* (19) 86 4.8 Lapatinib* (20) 90 4.9 Tucatinib* (21) 93 4.10 Neratinib* (22) 95 Chapter 5. VEGFR/Multikinase Inhibitors 97 5.1 Sorafenib* (23) 99 5.2 Regorafenib* (24) 104 5.3 Sunitinib* (25) 106 5.4 Pazopanib* (26) 112 5.5 Axitinib* (27) 114 5.6 Nintedanib* (28) 117 5.7 Apatinib** (29) 121 5.8 Lenvatinib* (30) 122 5.9 Tovozanib* (31) 125 Chapter 6. CDK4/6 Inhibitors 127 6.1 Palbociclib* (32) 129 6.2 Ribociclib*(33) 136 6.3 Abemaciclib* (34) 139 6.4 Trilaciclib* (35) 142 Chapter 7. JAK Inhibitors 144 7.1 Tofacitinib* (36) 147 7.2 Baricitinib* (37) 151 7.3 Peficitinib** (38) 153 7.4 Upadacitinib* (39) 158 7.5 Delgocitinib** (40) 161 7.6 Filgotinib** (41) 163 7.7 Abrocitinib* (42) 166 7.8 Ruxolitinib* (43) 170 7.9 Fedratinib* (44) 173 7.10 Pacritinib* (45) 175 7.11 Ritlecitinib # (46) 177 7.12 Brepocitinib # (47) 181 7.13 Ropsacitinib # (48) 184 Chapter 8. Allosteric TYK2 Inhibitors 187 8.1 Deucravacitinib* (49) 189 Chapter 9. ALK/multikinase Inhibitors 195 9.1 Crizotinib* (50) 197 9.2 Ceritinib* (51) 202 9.3 Alectinib* (52) 205 9.4 Brigatinib* (53) 207 9.5 Lorlatinib* (54) 210 Chapter 10. BRAF/Multikinase Inhibitors 214 10.1 Vemurafenib* (55) 216 10.2 Dabrafenib* (56) 222 10.3 Encorafenib* (57) 225 Chapter 11. MEK Inhibitors 227 11.1 Trametinib* (58) 228 11.2 Cobimetinib* (59) 232 11.3 Binimetinib* (60) 235 11.4 Selumetinib* (61) 237 Chapter 12. RET/Multikinase Inhibitors 240 12.1 Vandetanib* (62) 242 12.2 Cabozantinib* (63) 245 12.3 Selpercatinib* (64) 247 12.4 Pralsetinib* (65) 251 Chapter 13. FGFR Inhibitors 253 13.1 Erdafitinib* (66) 255 13.2 Pemigatinib* (67) 260 13.3 Infigratinib* (68) 263 13.4 Futibatinib* (69) 265 Chapter 14. PI3K Inhibitors 267 14.1 Alpelisib* (70) 269 14.2 Idelalisib* (71) 273 14.3 Duvelisib* (72) 277 14.4 Umbralisib* (73) 279 14.5 Copanlisib* (74) 281 Chapter 15. TRK/Multikinase Inhibitors 284 15.1 Larotrectinib* (75) 285 15.2 Entrectinib* (76) 288 15.3 Repotrectinib # (77) 291 Chapter 16. MET Inhibitors 294 16.1 Capmatinib* (78) 295 16.2 Tepotinib* (79) 297 Chapter 17. KIT/PDGFR/Multkinase Inhibitors 299 17.1 Avapritinib* (80) 301 17.2 Ripretinib* (81) 304 Chapter 18. FLT3 Inhibitors 306 18.1 Midostaurin* (82) 308 18.2 Gilteritinib* (83) 313 Chapter 19. mTOR Inhibitors 315 19.1 Sirolimus* and Analogs (84) 317 Chapter 20. Other Kinase Inhibitors 322 20.1 Netarsudil* (85) 324 20.2 Belumosudil* (86) 326 20.3 Fostamatinib* (87) 328 20.4 Pexidartinib* (88) 331 Chapter 21. KRAS Inhibitors 335 21.1 Sotorasib* (89) 337 21.2 Adagrasib* (90) 346 21.3 Jdq443 # (91) 350 Chapter 22. An Overview of the Discovery Process for Medically Useful Inhibitors of Oncogenic Protein Kinases 353 22.1 High-quality Leads 353 22.2 Integrating Substructures from Different High Quality Leads or Established Inhibitors 355 22.3 Variation of Hinge-binding Nucleus 357 22.4 Macrocyclization 359 22.5 Fragment-based Approach 360 22.6 Covalent Inhibitors 361 22.7 Strategic Structural Modification of Prior Drugs 362 22.8 Exploiting a Specific Kinase Pocket to Optimize Selectivity 364 22.9 Solvent-exposed Appendages to Enhance Solubility and PK Properties 367 Chapter 23. Targeted Molecular Anticancer Therapies – Successes and Challenges 368 23.1 The Beginning 368 23.2 Further Developments 368 23.3 Biomarker-driven Drug Development 369 23.4 Mitigation of Drug Resistance 370 23.5 Miscellaneous Approaches 371 23.6 Discovery Chemistry 373 Appendix 1. First FDA Approvals by Year 374 Appendix 2. Kinase/KRAS Inhibitors in Development 375 Appendix 3. Visualization of Differentially Expressed Kinases in Cancer 378 Appendix 4. M & A Transactions Driven by Oncology-focused Kinase and KRAS Inhibitors 379 Appendix 5. Alphabetic List of Oncogenic Protein Inhibitors 380
• Edition: 1st
• Publisher Details: Hoboken : John Wiley & Sons, Inc
• Publication Date: 2023
• Extent: 1 online resource (400 pages)
• Subjects: 616.994071; Carcinogenesis -- Molecular aspects; Carcinogens; Proteins
• Languages: English
• ISBNs: 9781394207107
• Notes: Note: Description based on CIP data; resource not viewed.
• Access Rights: Legal Deposit; Only available on premises controlled by the deposit library and to one user at any one time; The Legal Deposit Libraries (Non-Print Works) Regulations (UK).
• Access Usage: Restricted: Printing from this resource is governed by The Legal Deposit Libraries (Non-Print Works) Regulations (UK) and UK copyright law currently in force.