title: 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.
authors.affiliation: College of Animal Science and Veterinary Medicine, Jilin University, Changchun, 130062, China.
authors.forename: Honglei
authors.initials: H
authors.lastname: Zhao
authors.forename: Xin
authors.initials: X
authors.lastname: Feng
authors.forename: Wenyu
authors.initials: W
authors.lastname: Han
authors.forename: Yuwen
authors.initials: Y
authors.lastname: Diao
authors.forename: Dong
authors.initials: D
authors.lastname: Han
authors.forename: Xiaofeng
authors.initials: X
authors.lastname: Tian
authors.forename: Yu
authors.initials: Y
authors.lastname: Gao
authors.forename: Shanshan
authors.initials: S
authors.lastname: Liu
authors.forename: Seng
authors.initials: S
authors.lastname: Zhu
authors.forename: Cuimei
authors.initials: C
authors.lastname: Yao
authors.forename: Jingmin
authors.initials: J
authors.lastname: Gu
authors.forename: Changjiang
authors.initials: C
authors.lastname: Sun
authors.forename: Liancheng
authors.initials: L
authors.lastname: Lei
mesh_terms: D000595:Amino Acid Sequence; D006528:Carcinoma, Hepatocellular / Q000188:drug therapy* / Q000473:pathology; D045744:Cell Line, Tumor; D004797:Enzyme-Linked Immunosorbent Assay; D005434:Flow Cytometry; D006801:Humans; D008113:Liver Neoplasms / Q000188:drug therapy* / Q000473:pathology; D008555:Melitten / Q000008:administration & dosage*; D019151:Peptide Library; D010455:Peptides / Q000008:administration & dosage* / Q000737:chemistry; D011485:Protein Binding
chemical_list: D019151:Peptide Library; D010455:Peptides; D008555:Melitten
keywords: Ph.D.-12 phage peptide library; hepatocellular carcinoma cell; melittin; subtraction biopanning; tumor targeting