Cancer therapy using potent molecules targeting tumor angiogenesis: radiochemistry and preliminary biodistribution studies

Tumor angiogenesis, the sprouting of new blood vessels around proliferating cells, plays a significant during tumor growth and metastasis. The overexpression of integrin a α_vβ₃ in the neovasculature during tumor growth presents an interesting molecular target for both early detection and treatment of rapidly growing solid tumors. Integrin α_vβ₃ functions as a receptor for the extracellular matrix proteins with the exposed arginine(R)-glycine(G)-aspartic acid(D) tripeptide sequence. Considering the enhanced tumor targeting capability of cyclic RGD peptide dimer, an attempt has been made to prepare ⁹⁰Y- and ¹⁷⁷Lu-labeled DOTA-E(c(RGDfK)₂ (E = Glutamic acid, f = phenyl alanine, K = lysine) as a potential agents for targeted tumor therapy