Sortase A-mediated cyclization of novel polycyclic RGD peptides for ανβ3 integrin targeting

Cyclic arginine-glycine-aspartic (RGD) peptides that specifically bind to integrin ανβ3 have been developed for drug delivery, tracers, and imaging for tumor diagnosis and treatment. Herein, a series of polycyclic RGD peptides containing dual, tri, and tetra rings were designed and synthesized through sortase A-mediated ligation. An in vitro test on cell adhesion inhibition indicated that the RGD peptide containing tricylic structure exhibited outstanding potency and selectivity for ανβ3 integrin.