Small molecule alpha(v) integrin antagonists: novel anticancer agents

The members of the integrin family are targets that potentially provide bot h therapeutic and diagnostic opportunities. Advances in the understanding o f the signalling pathways, transcriptional regulation and the structure/fun ction relationships of the adhesion molecules to extracellular matrix prote ins have all contributed to these opportunities. The role of the integrins in pathological processes in both acute and chronic diseases, include ocula r, cancer (solid rumours and metastasis), cardiovascular (stroke and heart failure) and inflammatory (rheumatoid arthritis) conditions. Various therap eutic candidates, including antibodies, cyclic peptides and peptidomimetics , have been identified. This review will focus on the key role of the alpha (v) integrin (alpha(v)beta(5) and alpha(v)beta(5)) in angiogenic processes in tumours, including its potential use in cancer diagnostics and therapy.