This is a peptide with NGR (Asn-Gly-Arg) motif having a disulfide bridge connecting cys1 to cys5 known to elicit antimicrobial property in addition to the presence of KLA sequence. This peptide shows potent cytotoxicity and activity against tumor cells due to its binding to CD13 on tumor cells. This peptide shows dose-dependent antiproliferation against tumor cells and induces cell cylce arrest at G2/M phases and apoptosis of the tumor cells. NGR motif containing peptides are useful in delivering cytotoxic drugs, proapoptotic peptides and tumor necrosis factor (TNF) to tumor vasculature.
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)