Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity

davidd submitted, created time 10 months 1 week (www.pnas.org)

B-RAF is the most frequent oncogenic protein kinase mutation known. Furthermore, inhibitors targeting "active" protein kinases have demonstrated significant utility in the therapeutic repertoire against cancer. The article represents the entire discovery process of a selective inhibitor , from initial identification through structural and biological studies in animal models to a promising therapeutic for testing in cancer patients bearing B-RafV600E-driven tumors.

Keywords: melanoma phosphorylation protein kinases B-RAF cell signaling cancer