Adrian Gill,
Kevan M Shokat,
Kevan M. Shokat
RAS Drug Discovery
Past, Present and Future
Paperback Engels 2024 9780443218613Levertijd ongeveer 9 werkdagen
Gratis verzonden
Samenvatting
KRAS Drug Discovery: Past, Present and Future is a comprehensive overview of the state-of-the-art medicinal chemistry approaches towards targeting the formerly undruggable oncogene, KRAS. It includes Seminal medicinal chemistry case histories of KRASG12C inhibitors such as Sotorosib, the first approved KRASG12C inhibitor for NSCLC, alongside the latest advances towards identification of in vivo tools and development candidates targeting KRAS G12D, KRAS G13C and other mutations. The book also provides the reader with a comprehensive overview of the in vitro assay systems, in vivo pharmacology xenograft models and chemical biology tools available to characterize small molecule inhibitors of KRAS.
Specificaties
Lezersrecensies
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Inhoudsopgave
<p>1. Introduction to KRAS Biology<br>2. Historical context and background to RAS drug discovery: the first 25 years of RAS targeting focused on FTase inhibitors<br>3. KRAS in vitro assays – biochem, biophysics and cell based<br>4. KRAS in vivo models and pharmacology<br>5. RAS Structural Biology: The Journey from Structures to Therapeutic Advances<br><br>Section 1: First generation KRAS G12C OFF inhibitors<br>6. ARS-1620 SAR journey<br>7. Sotorasib/AMG510 SAR journey<br>8. Adagrasib/MRTX849 SAR journey<br>9. Novartis SAR journey - JDQ 443<br>10. Jacobio SAR Journey – JAB-21822<br>11. KRAS degraders<br><br>Section 2: Second generation G12C inhibitors and new modalities<br>12. KRAS ON inhibitors using Tri-complex inhibitors – RMC-4998/6291 story<br><br>Section 3: Beyond KRAS G12C<br>13. Pan-KRAS inhibitors<br>14. RAS-multi – RMC-7977 story<br>15. G12S/R stories<br>16. G12D stories<br>17. MRTX1133 (small molecule)<br>18. RMC-9945 (G12D covalent inhibitor)<br>19. KRAS combinations (preclinical and clinical)<br>20. The immune-oncology potential of KRAS inhibitors<br>21. KRAS Competitive Intelligence/G12C, G12D, pan/multi-RAS Chapter<br>22. Conclusions and future of RAS Drug Discovery<br>23. LUMAKRAS® (sotorasib): SAR Journey & Path to the Clinic</p>
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