Functionalized cyclic RGD peptidomimetics: conjugable ligands for αvβ3 receptor imaging

The α(v)β(3) integrin is an adhesion molecule involved in physiological and pathological angiogenesis as well as in tumor invasion and metastasis, and therefore, there is a strong interest in developing novel agents interacting with this molecule. We report the synthesis and characterization of fluorescent α(v)β(3) integrin probes and their use to visualize integrin α(v)β(3) expression on human normal and cancer cells. The fluorescent probes we describe here may be of use for noninvasive imaging of α(V)β(3) integrin expression also in vivo.