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Updated: Apr 12, 2026
Peptide-based Identification of Functional Motifs and their Binding Partners
Published on: June 30, 2013
An antimicrobial peptide containing NGR motif has potent antitumor activity against CD13+ and CD13- tumor cells
Abstract:
Antimicrobial peptides (AMPs) with Asn-Gly-Arg (NGR) motif have potent cytotoxicity, preferably against tumor cells due to their binding to CD13 on tumor cells. However, the importance of αvβ3 expression for antitumor activity of AMPs containing NGR has not been clarified. This study was aimed at designing a new AMP containing NGR and testing their biological activity against different types of tumor cells with varying CD13 and αvβ3 expression. We first synthesized the new AMP containing NGR motif (CK21), which effectively entered into CD13+ HT-1080, but less into CD13- αvβ3+ MDA-MB-435 and further less into stable αvβ3-silencing MDA-MB-435 cells. Furthermore, CK21 displayed dose-dependent antiproliferation against these tumor cells and induced cell cycling arrest at G2/M phases and apoptosis of these tumor cells. In addition, CK21 inhibited the invasion of these tumor cells in vitro and inhibited the growth of implanted tumor cells in vivo. Particularly, the antitumor effect of CK21 in CD13+ HT-1080 was stronger than that of CD13- αvβ3+ MDA-MB-435 and much stronger than that of stable αvβ3-silencing MDA-MB-435. Our data indicated that the new AMPs containing NGR had potent antitumor activity against CD13+ or αvβ3+ tumor cells, preferably against CD13+ tumor cells, possibly through binding to CD13 or αvβ3 on tumor cells.
Insights
New antimicrobial peptides (AMPs) with an Asn-Gly-Arg (NGR) motif show potent antitumor activity, particularly against CD13+ tumor cells. This study highlights the dual targeting potential of NGR-AMPs against CD13 and αvβ3 receptors on cancer cells.
Area of Science:
- Biochemistry
- Molecular Biology
- Oncology
Background:
- Antimicrobial peptides (AMPs) with an Asn-Gly-Arg (NGR) motif exhibit cytotoxicity, targeting CD13 on tumor cells.
- The role of αvβ3 integrin expression in the antitumor activity of NGR-motif AMPs remains unclear.
Purpose of the Study:
- To design and synthesize a novel NGR-motif AMP.
- To evaluate the biological activity of the new AMP against tumor cells with varying CD13 and αvβ3 expression.
Main Methods:
- Synthesis of a new NGR-motif AMP (CK21).
- Assessment of cellular uptake in tumor cells with differential CD13 and αvβ3 expression.
- In vitro antiproliferation, cell cycle arrest, apoptosis, and invasion assays.
- In vivo tumor growth inhibition studies.
Main Results:
- CK21 demonstrated effective cellular entry into CD13+ HT-1080 cells, with reduced entry into αvβ3+ MDA-MB-435 cells and further reduced entry into αvβ3-silencing cells.
- CK21 induced dose-dependent antiproliferation, G2/M cell cycle arrest, and apoptosis in tested tumor cells.
- CK21 inhibited tumor cell invasion in vitro and suppressed tumor growth in vivo, with superior efficacy against CD13+ HT-1080 cells compared to αvβ3+ or αvβ3-silencing cells.
Conclusions:
- The novel NGR-motif AMP (CK21) possesses significant antitumor activity.
- Antitumor efficacy is associated with CD13 and αvβ3 expression, with a preference for CD13+ tumor cells.
- NGR-AMPs represent a promising therapeutic strategy targeting CD13 and/or αvβ3 on tumor cells.
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