Anti-Angiogenesis Activities of Novel Peptide Complexes: Mitochondria-Disruptive 9mer Peptides Conjugated with the Integrin alpha V beta 3-Homing Cyclic RGD Motif

作者：Iwasaki Takashi; Yamakawa Minoru; Asaoka Ai; Kawano Tsuyoshi; Ishibashi Jun^*

来源：Bioscience Biotechnology and Biochemistry, 2012, 76(11): 2044-2048.

DOI：10.1271/bbb.120397

• antimicrobial peptide
• cyclic RGD motif
• mitochondria
• integrin alpha V beta 3
• drug delivery system

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.

• 出版日期2012-11