Transactivation of Raf signaling by BRAF inhibitors in Ras mutant melanoma.
Typically, NRAS mutant melanomas rely on CRAF-mediated MAPK activation, with BRAF locked into an inactive conformation.
BRAF inhibitors relieve the autoinhibition of BRAF leading to its recruitment to the plasma membrane. This then leads to the dimerization of BRAF and CRAF, leading to enhanced MAPK pathway signaling and proliferation. A full colour version of this figure is available at the Oncogene journal online.