Design and Synthesis of an RGD Peptidomimetic-Paclitaxel Conjugate Targeting ?v?3 Integrin for Tumour-Directed Drug Delivery

A 1,2,3-triazole-based RGD peptidomimetic having nanomolar affinity for ?v?3 integrin was conjugated to the potent antimitotic paclitaxel via an oxime heterobifunctional linker. The resulting construct maintained nanomolar binding concentration to ?v?3 integrin and showed 11-fold selectivity in terms of cytotoxicity towards highly ?v?3 expressing U87MG cancer cells relative to non ?v?3 expressing MCF7 cells, indicating promising cancer cell targeting capacity.