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.