This is a peptide with an NGR (Asn-Gly-Arg) motif and a disulfide bridge connecting cys1 and cys5. It is known to have antibacterial properties in addition to the KLA sequence. This peptide shows strong cytotoxicity and activity against tumor cells due to its binding to CD13 on tumor cells. The peptide has a dose-dependent anti-proliferation effect on tumor cells, induces cell cycle arrest in G2/M phase, and induces tumor cell apoptosis. Peptides containing NGR motifs can be used to deliver cytotoxic drugs, pro-apoptotic peptides and tumor necrosis factor (TNF) to tumor blood vessels.
1, Ellerby, HM. et al. Nat Med. 5, 1032 (1999) 2, Colombo, G. et al. J. Biol. Chem. 277, 47891 (2002) 3, Van Hensbergen, Y. et al. Biochem. Pharmacol. 63, 897 (2002) 4, Plesniak, L. et al. Protein Sci. 13, 1988 (2004) 5, Zhang Z. et al. Tum Biol. 36(10), 8167-8175 (2015).
Sequence (One-Letter Code)
CNGRCGGklaklakklaklak-NH2 (Disulfide bridge: 1-5)
Sequence (Three-Letter Code)
H - Cys - Asn - Gly - Arg - Cys - Gly - Gly - D - Lys - D - Leu - D - Ala - D - Lys - D - Leu - D - Ala - D - Lys - D - Lys - D - Leu - D - Ala - D - Lys - D - Leu - D - Ala - D - Lys - NH2 (Disulfide bridge: 1 - 5)