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 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...

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Bibliographic Details
Published in:Bioscience, biotechnology, and biochemistry biotechnology, and biochemistry, 2012, Vol.76 (11), p.2044-2048
Main Authors: IWASAKI, Takashi, YAMAKAWA, Minoru, ASAOKA, Ai, KAWANO, Tsuyoshi, ISHIBASHI, Jun
Format: Article
Language:English
Subjects:
Amino Acid Motifs
Amino Acid Sequence
Angiogenesis Inhibitors - chemistry
Angiogenesis Inhibitors - metabolism
Angiogenesis Inhibitors - pharmacology
Angiogenesis Inhibitors - toxicity
Animals
antimicrobial peptide
Apoptosis
Apoptosis - drug effects
Biological and medical sciences
Cell Line, Tumor
Cercopithecus aethiops
COS Cells
cyclic RGD motif
Drug Carriers - metabolism
drug delivery system
Fundamental and applied biological sciences. Psychology
Gene Expression Regulation - drug effects
Humans
Integrin alphaVbeta3 - metabolism
integrin αVβ3
Membrane Potential, Mitochondrial - drug effects
mitochondria
Mitochondria - drug effects
Mitochondria - metabolism
Oligopeptides - chemistry
Oligopeptides - metabolism
Oligopeptides - pharmacology
Oligopeptides - toxicity
Peptides, Cyclic - metabolism
Protein Transport
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Summary: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.
ISSN:0916-8451
1347-6947
DOI:10.1271/bbb.120397