Stephen Hiscox1, Robert I Nicholson. 1. RCUK Academic Fellow Cardiff University, Welsh School of Pharmacy, Redwood Building, King Edward VII Avenue, Cardiff, CF10 3XF, UK. HiscoxSE1@cf.ac.uk
Abstract
BACKGROUND: Recent evidence has established the non receptor tyrosine kinase, Src, as a critical component of multiple signalling pathways that regulate proliferation, survival, angiogenesis and metastasis. Increased levels of Src protein and activity are widely reported in human cancers including breast cancer, and its important role in oncogenic processes makes it a potential target for therapeutic intervention. OBJECTIVE: To review the role of Src kinase in breast cancer and discuss its potential as a therapeutic target. METHODS: Literature citing preclinical and clinical studies with Src inhibitors was reviewed. CONCLUSION: Experimental data with small-molecule inhibitors of Src kinase in breast cancer are encouraging, demonstrating effective suppression in vitro of tumour growth and invasion and inhibition of disease spread in preclinical models in vivo. Recently several Src inhibitors have been tested in Phase I clinical trials where they are well tolerated and demonstrate low toxicity. Overall, these findings suggest that Src inhibitors present a future therapeutic option in the treatment of breast cancer growth and progression.
BACKGROUND: Recent evidence has established the non receptor tyrosine kinase, Src, as a critical component of multiple signalling pathways that regulate proliferation, survival, angiogenesis and metastasis. Increased levels of Src protein and activity are widely reported in humancancers including breast cancer, and its important role in oncogenic processes makes it a potential target for therapeutic intervention. OBJECTIVE: To review the role of Src kinase in breast cancer and discuss its potential as a therapeutic target. METHODS: Literature citing preclinical and clinical studies with Src inhibitors was reviewed. CONCLUSION: Experimental data with small-molecule inhibitors of Src kinase in breast cancer are encouraging, demonstrating effective suppression in vitro of tumour growth and invasion and inhibition of disease spread in preclinical models in vivo. Recently several Src inhibitors have been tested in Phase I clinical trials where they are well tolerated and demonstrate low toxicity. Overall, these findings suggest that Src inhibitors present a future therapeutic option in the treatment of breast cancer growth and progression.