Specific inhbitor of ERK 1/2 AEZS-131: anticancer activity in models of human cancers with and without overactivation of ERK 1/2

Purpose: The RAS/RAF/MEK/ERK pathway is activated in more than 30% of human cancers, mostly via mutation in K-Ras oncogene and also via mutations in BRAF. Although various MEK-inhibitors have been developed, acquired resistance to MEK-inhibitors is a major problem. We investigate specific ERK inhibitor AEZS-131 in a panel of human cancers with and without mutations in the MAPK-pathway. Methods: The ability of AEZS 131 to selectively target cancer cell proliferation and survival is demonstrated in-vitro by MTT-assays and FACS based analysis. Furthermore the mechanism of cytotoxicity is analysed by FACS based assa…