Highly active and selective ligands for integrin avß6

The family of human heterodimeric integrin receptors consists of 24 members. Eight integrins of this superfamily (αvß1, αvß3, αvß5, avß6, αvß8, α5ß1, α8ß1 and αIIbß3) are able to recognize the RGD tripeptide fragment in natural and artificial ligands with various activity and selectivity. avß6 is usually undetectable in normal adults’ cells, but is highly upregulated in different types of cancer (including pancreatic, breast, skin, head and neck, lung (NSCLC) and ovarian cancer) and exclusively expressed on epithelial cells. Therefore, avß6 is an emerging target for therapy as well as imaging across several common tumor types.