The coming of age of MEK
Menés sur 97 et 206 patients atteints d'un mélanome, ces deux essais de phase I évaluent le trametinib, un inhibiteur de MEK
An important pathway in oncology is the MAPK signal cascade, incorporating the enzymes RAS, RAF, MEK, and ERK. After the discovery that genes encoding RAS and the RAF isoform BRAF were oncogenic, much effort has been made to target this pathway, to prove the hypothesis that cancer cells need oncogenes to grow and survive—so-called oncogene addiction. Findings of preclinical studies indicate that protein kinase activity of MEK is needed for RAS and BRAF to promote cell proliferation and survival and to induce a state of oncogene addiction. This area of cancer research is important, because activating mutations in RAS isoforms and BRAF are reported in up to 30% and 6—7% of human cancers, respectively. Therefore, successful inhibition of MEK could profoundly change the way patients with mutations in RAS or BRAF are managed...
The Lancet Oncology , commentaire, 2011