Anti-angiogenesis activities of novel peptide complexes: Mitochondria-disruptive 9MER peptides conjugated with the integrin alpha v beta 3-homing cyclic RGD

Abstract

RGD peptides are popular drug delivery tools in treating integrin αVβ3-expressing malignant tumors and tumor vasculature cells. We investigated the specific delivery and pharmacological potential of enantiomeric mitochondria-disruptive peptides (RLYLRIGRR-NH2, RLRLRIGRR-NH 2, ALYLAIRRR-NH2, and RLLLRIGRRNH2) after conjugation with an integrin αVβ3-homing peptide, cyclic pentameric RGD peptide. The cyclic RGD-conjugated mitochondria-disruptive peptides exhibited specific internalization, apoptosis induction, and cytotoxicity against integrin αVβ3-high-expressing human umbilical vein endothelial cells. Our findings indicate that these novel peptide complexes might prove good anti-angiogenesis reagents.