Synthesis and characterization of Arg-Gly-Asp (RGD) peptidomimetics functionalized onto gold nanoparticles


One of the challenges for developing therapeutic nanoparticles involves attaching appropriate chemical moieties that will target cells that overexpress specific surface receptors. We have initiated a project to design and prepare functionalized gold nanoparticles (AuNPs) that selectively target cancer cells that overexpress the integrin ?v?3 receptors. We have devised a convergent strategy that uses novel, multivalent RGD peptidomimetics attached to the AuNP surface as a means for enhancing cellular selectivity, affinity and uptake. In this study, we describe the synthesis of a novel RGD peptidomimetic, its ligation to a Newkome-type dendron and its attachment to AuNPs. The characterization and evaluation of the functionalized AuNPs will be discussed.