These authors contributed equally to this work.
Enhanced binding to and killing of hepatocellular carcinoma cells in vitro by melittin when linked with a novel targeting peptide screened from phage display
Article first published online: 26 AUG 2013
Copyright © 2013 European Peptide Society and John Wiley & Sons, Ltd.
Journal of Peptide Science
Volume 19, Issue 10, pages 639–650, October 2013
How to Cite
Zhao, H., Feng, X., Han, W., Diao, Y., Han, D., Tian, X., Gao, Y., Liu, S., Zhu, S., Yao, C., Gu, J., Sun, C. and Lei, L. (2013), Enhanced binding to and killing of hepatocellular carcinoma cells in vitro by melittin when linked with a novel targeting peptide screened from phage display. J. Peptide Sci., 19: 639–650. doi: 10.1002/psc.2542
- Issue published online: 6 SEP 2013
- Article first published online: 26 AUG 2013
- Manuscript Accepted: 29 JUN 2013
- Manuscript Revised: 10 JUN 2013
- Manuscript Received: 17 MAR 2013
- National Natural Science Foundation of China. Grant Number: 30901069
- State Key Program of National Natural Science of China. Grant Number: 31130052
- Ph.D.-12 phage peptide library;
- hepatocellular carcinoma cell;
- subtraction biopanning;
- tumor targeting
A random phage 12-mer peptide library and a whole-cell subtractive biopanning protocol against HepG2 cells were used to select a novel peptide-specific binding to hepatocellular carcinoma cells. As a result, peptide SLSLITMLKISR (AM-2) was screened as a novel homing peptide to hepatocellular carcinoma cells, tested by immunofluorescence and immunochemistry assays. Subsequently, peptide AM-2 was linked to melittin by A(EAAAK)2A, and the antitumor effect of this ligation product was detected by MTT assay, fluorescence-activated cell sorting, and scanning electron microscopy methods. Results of cell growth inhibition tests confirmed that the affinity of melittin was increased after being incorporated into AM-2, and AM-2-melittin specifically targeted and killed HepG2 cells in vitro. Thus, AM-2 is a valuable ligand for tumor targeting, which leads to increased binding and killing effect of hepatocellular carcinoma cells in vitro when ligated to melittin, and AM-2-melittin has a clinical potential application as target agents for the treatment of human hepatocellular carcinoma. Copyright © 2013 European Peptide Society and John Wiley & Sons, Ltd.