Anti-Angiogenesis Activities Of Novel Peptide Complexes: Mitochondria-Disruptive 9mer Peptides Conjugated With The Integrin Alpha V Beta 3-Homing Cyclic Rgd Motif

RGD peptides are popular drug delivery tools in treating integrin alpha V beta 3-expressing malignant tumors and tumor vasculature cells. We investigated the specific delivery and pharmacological potential of enantiomeric mitochondria-disruptive peptides (RLYLRIGRR-NH2, RLRLRIGRR-NH2, ALYLAIRRR-NH2, and RILLRIGRR-NH2) after conjugation with an integrin alpha V beta 3-homing peptide, cyclic pentameric RGD peptide. The cyclic RGD-conjugated mitochondria-disruptive peptides exhibited specific internalization, apoptosis induction, and cytotoxicity against integrin alpha V beta 3-high-expressing human umbilical vein endothelial cells. Our findings indicate that these novel peptide complexes might prove good anti-angiogenesis reagents.