Recombinant single-chain and disulfide-stabilized Fv-immunotoxins that cause complete regression of a human colon cancer xenograft in nude mice

Int J Cancer. 1996 Jul 3;67(1):113-23. doi: 10.1002/(SICI)1097-0215(19960703)67:1<113::AID-IJC19>3.0.CO;2-F.

Abstract

Monoclonal antibody (MAb) 55.1 specifically recognizes an antigen on the surface of human colon adenocarcinoma cells. We constructed recombinant immunotoxins composed of the heavy- and light-chain variable regions of MAb 55.1 fused to a recombinant form of Pseudomonas exotoxin (PE). The heavy- and light-chain variable regions are stabilized by 2 means. One is by a flexible peptide linker to form a single-chain antigen binding protein (scFv) and the second by an interchain disulfide bond engineered between structurally conserved framework regions. These are termed disulfide stabilized Fvs (dsFv). The 2 Fv forms are fused to truncated forms of PE lacking the cell binding domain. The recombinant scFv- and dsFv-immunotoxins were expressed in E. coli and purified to near homogeneity. The scFv- and dsFv-immunotoxins were shown to be specifically cytotoxic to human colon adenocarcinoma cell lines. The scFv-immunotoxin containing PE38KDEL was more active than the immunotoxin containing PE38 with the native carboxyl terminus (REDLK). However, the PE38KDEL immunotoxin is about 2-fold more toxic in mice, and therefore it does not appreciably increase the therapeutic window in mice. Intravenous administration of the scFv- and dsFv- recombinant immunotoxins caused complete regression of a human colon carcinoma (Colo205) growing subcutaneously in immunodeficient mice. The dsFv-immunotoxin has better antitumor activity compared with its scFv-immunotoxin counterpart.

MeSH terms

  • ADP Ribose Transferases*
  • Amino Acid Sequence
  • Animals
  • Antibodies, Monoclonal / therapeutic use
  • Bacterial Toxins*
  • Base Sequence
  • Colonic Neoplasms / therapy*
  • Exotoxins / therapeutic use*
  • Female
  • Humans
  • Immunoglobulin Fragments / therapeutic use*
  • Immunotoxins / therapeutic use*
  • Mice
  • Mice, Inbred BALB C
  • Mice, Nude
  • Molecular Sequence Data
  • Neoplasm Transplantation
  • Pseudomonas aeruginosa Exotoxin A
  • Recombinant Proteins / therapeutic use
  • Transplantation, Heterologous
  • Virulence Factors*

Substances

  • Antibodies, Monoclonal
  • Bacterial Toxins
  • Exotoxins
  • Immunoglobulin Fragments
  • Immunotoxins
  • Recombinant Proteins
  • Virulence Factors
  • immunoglobulin Fv
  • ADP Ribose Transferases