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Enhanced binding to and killing of hepatocellular carcinoma cells in vitro by melittin when linked with a novel targeting peptide screened from phage display.

Abstract
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.
AuthorsHonglei Zhao, Xin Feng, Wenyu Han, Yuwen Diao, Dong Han, Xiaofeng Tian, Yu Gao, Shanshan Liu, Seng Zhu, Cuimei Yao, Jingmin Gu, Changjiang Sun, Liancheng Lei
JournalJournal of peptide science : an official publication of the European Peptide Society (J Pept Sci) Vol. 19 Issue 10 Pg. 639-50 (Oct 2013) ISSN: 1099-1387 [Electronic] England
PMID24014474 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
CopyrightCopyright © 2013 European Peptide Society and John Wiley & Sons, Ltd.
Chemical References
  • Peptide Library
  • Peptides
  • Melitten
Topics
  • Amino Acid Sequence
  • Carcinoma, Hepatocellular (drug therapy, pathology)
  • Cell Line, Tumor
  • Enzyme-Linked Immunosorbent Assay
  • Flow Cytometry
  • Humans
  • Liver Neoplasms (drug therapy, pathology)
  • Melitten (administration & dosage)
  • Peptide Library
  • Peptides (administration & dosage, chemistry)
  • Protein Binding

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