Article
The Discovery of Exarafenib (KIN-2787): Overcoming the Challenges of Pan-RAF Kinase Inhibition.
Journal of medicinal chemistry - 8 Feb 2024
Chen Young K, Kanouni Toufike, Arnold Lee D, Cox Jason M, Gardiner Elisabeth, Grandinetti Kathryn, Jiang Ping, Kaldor Stephen W, Lee Catherine, Li Chun, Martin Eric S, Miller Nichol, Murphy Eric A, Timple Noel, Tyhonas John S, Vassar Angie, Wang Tim S, Williams Richard, Yuan Ding, Kania Robert S
Abstract excerpt
RAF, a core signaling component of the MAPK kinase cascade, is often mutated in various cancers, including melanoma, lung, and colorectal cancers. The approved inhibitors were focused on targeting the BRAFV600E mutation that results in constitutive activation of kinase signaling through the monom...
Topics
- Humans
- Proto-Oncogene Proteins B-raf
- Protein Kinase Inhibitors
- Cell Line, Tumor
- Melanoma
- MAP Kinase Signaling System
- Mutation