Current antitumor therapies targeting the RAS-ERK pathway have been mostly aimed at inhibiting the activity of the kinases that populate the route. A small-molecule inhibitor of ERK dimerization effectively prevents the progression of tumors harboring oncogenic RAS and BRAF, demonstrating that targeting regulatory protein-protein interactions can be a valid strategy for treating RAS-ERK pathway-driven neoplasia.
Keywords: Antitumor therapy; dimerization inhibitor; ERK.