Adrian Gill,
Adrian (SVP Discovery Chemistry, Revolution Medicines Inc., USA) Gill,
Kevan M. Shokat,
Kevan M. (Department of Cellular and Molecular Pharmacology at UCSF; Professor of Chemistry at UC Berkeley; Howard Hughes Medical Institute investigator, USA) Shokat
e.a.
RAS Drug Discovery
Past, Present and Future
Paperback Engels 2024 9780443218613Levertijd ongeveer 9 werkdagen
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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
Wees de eerste die een lezersrecensie schrijft!
Inhoudsopgave
1. Introduction to KRAS Biology
2. Historical context and background to RAS drug discovery: the first 25 years of RAS targeting focused on FTase inhibitors
3. KRAS in vitro assays – biochem, biophysics and cell based
4. KRAS in vivo models and pharmacology
5. RAS Structural Biology: The Journey from Structures to Therapeutic Advances
Section 1: First generation KRAS G12C OFF inhibitors
6. ARS-1620 SAR journey
7. Sotorasib/AMG510 SAR journey
8. Adagrasib/MRTX849 SAR journey
9. Novartis SAR journey - JDQ 443
10. Jacobio SAR Journey – JAB-21822
11. KRAS degraders
Section 2: Second generation G12C inhibitors and new modalities
12. KRAS ON inhibitors using Tri-complex inhibitors – RMC-4998/6291 story
Section 3: Beyond KRAS G12C
13. Pan-KRAS inhibitors
14. RAS-multi – RMC-7977 story
15. G12S/R stories
16. G12D stories
17. MRTX1133 (small molecule)
18. RMC-9945 (G12D covalent inhibitor)
19. KRAS combinations (preclinical and clinical)
20. The immune-oncology potential of KRAS inhibitors
21. KRAS Competitive Intelligence/G12C, G12D, pan/multi-RAS Chapter
22. Conclusions and future of RAS Drug Discovery
23. LUMAKRAS® (sotorasib): SAR Journey & Path to the Clinic
2. Historical context and background to RAS drug discovery: the first 25 years of RAS targeting focused on FTase inhibitors
3. KRAS in vitro assays – biochem, biophysics and cell based
4. KRAS in vivo models and pharmacology
5. RAS Structural Biology: The Journey from Structures to Therapeutic Advances
Section 1: First generation KRAS G12C OFF inhibitors
6. ARS-1620 SAR journey
7. Sotorasib/AMG510 SAR journey
8. Adagrasib/MRTX849 SAR journey
9. Novartis SAR journey - JDQ 443
10. Jacobio SAR Journey – JAB-21822
11. KRAS degraders
Section 2: Second generation G12C inhibitors and new modalities
12. KRAS ON inhibitors using Tri-complex inhibitors – RMC-4998/6291 story
Section 3: Beyond KRAS G12C
13. Pan-KRAS inhibitors
14. RAS-multi – RMC-7977 story
15. G12S/R stories
16. G12D stories
17. MRTX1133 (small molecule)
18. RMC-9945 (G12D covalent inhibitor)
19. KRAS combinations (preclinical and clinical)
20. The immune-oncology potential of KRAS inhibitors
21. KRAS Competitive Intelligence/G12C, G12D, pan/multi-RAS Chapter
22. Conclusions and future of RAS Drug Discovery
23. LUMAKRAS® (sotorasib): SAR Journey & Path to the Clinic
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