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

Autor: Jun Ishibashi, Ai Asaoka, Tsuyoshi Kawano, Minoru Yamakawa, Takashi Iwasaki
Rok vydání: 2012
Předmět:
Zdroj: Bioscience, Biotechnology, and Biochemistry. 76:2044-2048
ISSN: 1347-6947
0916-8451
DOI: 10.1271/bbb.120397
Popis: 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-NH(2), RLRLRIGRR-NH(2), ALYLAIRRR-NH(2), and RLLLRIGRR-NH(2)) 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.
Databáze: OpenAIRE