1. In melanoma tumours expressing the BRAFV600E oncogene RAF inhibitor treatment decreases ERK activation resulting in tumour regression and increased survival.
Figure 2 from M Holderfield
British Journal of Cancer (2014) 111, ; doi: /bjc
Several approaches exist to target Eph receptors. Kinase inactivating strategies include kinase inhibitors or blocking peptides or antibodies. Kinase activating strategies include ligand stimulation, activating antibodies or ligand peptide mimetics Strategies to deliver toxic payloads following receptor activation and internalisation include coupling of cytotoxic agents or radionuclides to Eph monoclonal antibodies.
© 2014 Cancer Research UK.