Article
Structure and RAF family kinase isoform selectivity of type II RAF inhibitors tovorafenib and naporafenib.
The Journal of biological chemistry - 1 May 2023
Tkacik Emre, Li Kunhua, Gonzalez-Del Pino Gonzalo, Ha Byung Hak, Vinals Javier, Park Eunyoung, Beyett Tyler S, Eck Michael J
Abstract excerpt
Upon activation by RAS, RAF family kinases initiate signaling through the MAP kinase cascade to control cell growth, proliferation, and differentiation. Among RAF isoforms (ARAF, BRAF, and CRAF), oncogenic mutations are by far most frequent in BRAF. The BRAFV600E mutation drives more than half of all malignant melanoma and is also found in many other cancers. Selective inhibitors of BRAFV600E (vemurafenib,...
Topics
- Humans
- Cell Line, Tumor
- Crystallography, X-Ray
- MAP Kinase Signaling System
- Melanoma
- Models, Molecular
- Molecular Structure
- Mutation
- Protein Isoforms
- Protein Kinase Inhibitors