Bisphosphonate-functionalized cyclic Arg-Gly-Asp peptidomimetics

We report the synthesis of three new conjugates between a cRGD integrin ligand and alendronic acid as a bisphosphonate anchor. The selected ligand is an RGD peptidomimetic, carrying the conformationally constrained RGD sequence on an azabicycloalkane scaffold and endowed with high affinity for integrin ???3. Since integrin ???3 is involved in the adhesion of osteoprogenitor cells and of osteoblasts, these constructs could prove useful as new tools for biofunctionalization of materials in biomedical application and for development of modern implants