Article
KRAS inhibitors: resistance drivers and combinatorial strategies.
Trends in cancer - 1 Feb 2025
Isermann Tamara, Sers Christine, Der Channing J, Papke Bjoern
Abstract excerpt
In 1982, the RAS genes HRAS and KRAS were discovered as the first human cancer genes, with KRAS later identified as one of the most frequently mutated oncogenes. Yet, it took nearly 40 years to develop clinically effective inhibitors for RAS-mutant cancers. The discovery in 2013 by Shokat and colleagues of a druggable pocket in KRAS paved the way to FDA approval of the first covalently binding KRASG12C...
Topics
- Humans
- Drug Resistance, Neoplasm
- Proto-Oncogene Proteins p21(ras)
- Neoplasms
- Mutation
- Antineoplastic Combined Chemotherapy Protocols
- Molecular Targeted Therapy
- Piperazines
- Pyridines
- Pyrimidines