A novel peptide isolated from a phage display peptide library with trastuzumab can mimic antigen epitope of HER-2

J Biol Chem. 2005 Feb 11;280(6):4656-62. doi: 10.1074/jbc.M411047200. Epub 2004 Nov 9.

Abstract

Trastuzumab, a humanized antibody to HER-2, has been shown to be effective in the treatment of breast cancer in which HER-2 overexpression and metastasis occurs. In our search for an effective mimic epitope of HER-2 binding with trastuzumab and to develop HER-2 peptide vaccine, we screened a phage display 12-mer peptide library with trastuzumab as the target. A mimetic peptide (mimotope) H98 (LLGPYELWELSH) that could specifically recognize trastuzumab was isolated. The DNA encoding peptide H98 was cloned and expressed as the fusion protein GST-H98 in Escherichia coli BL21. The purified GST-H98 could specifically bind to trastuzumab and block the binding of trastuzumab to HER-2 protein. Moreover, H98 could significantly block the function of trastuzumab inhibiting the growth of cancer cells. Mice that were immunized with GST-H98 made specific antibody to H98 as well as to HER-2. In addition, T-cell proliferation occurred in mice immunized with GST-H98. Although no sequence homology was found between H98 and HER-2, through the use of structure analysis we were able to determine that peptide H98 contributed to a conformational epitope of HER-2. Furthermore, we determined that the last two amino acids at the C terminus, and the third together with the fourth amino acid at the N terminus of peptide H98 are critical to the binding of H98 to trastuzumab. As a result, we conclude that peptide H98 has potential for being developed as a HER-2 vaccine for biotherapy of cancer with HER-2 overexpression.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antibodies, Monoclonal / pharmacology*
  • Antibodies, Monoclonal, Humanized
  • Antigens / chemistry
  • Antineoplastic Agents / pharmacology
  • Binding, Competitive
  • Blotting, Western
  • Cell Line, Tumor
  • Coloring Agents / pharmacology
  • DNA / metabolism
  • Dose-Response Relationship, Drug
  • Enzyme-Linked Immunosorbent Assay
  • Epitopes / chemistry
  • Escherichia coli / metabolism
  • Genetic Vectors
  • Glutathione Transferase / metabolism
  • Humans
  • Immunoglobulin G / chemistry
  • Mice
  • Mice, Inbred BALB C
  • Models, Molecular
  • Mutation
  • NIH 3T3 Cells
  • Neoplasms / therapy
  • Peptide Library
  • Peptides / chemistry
  • Protein Binding
  • Protein Conformation
  • Protein Structure, Tertiary
  • Receptor, ErbB-2 / chemistry*
  • Recombinant Fusion Proteins / metabolism
  • Recombinant Proteins / chemistry
  • Spleen / metabolism
  • T-Lymphocytes / metabolism
  • Tetrazolium Salts / pharmacology
  • Thiazoles / pharmacology
  • Trastuzumab

Substances

  • Antibodies, Monoclonal
  • Antibodies, Monoclonal, Humanized
  • Antigens
  • Antineoplastic Agents
  • Coloring Agents
  • Epitopes
  • Immunoglobulin G
  • Peptide Library
  • Peptides
  • Recombinant Fusion Proteins
  • Recombinant Proteins
  • Tetrazolium Salts
  • Thiazoles
  • DNA
  • Glutathione Transferase
  • Receptor, ErbB-2
  • thiazolyl blue
  • Trastuzumab

Associated data

  • PDB/1Y2N