Novel antibody hinge regions for efficient production of CH2 domain-deleted antibodies

J Biol Chem. 2005 Dec 16;280(50):41494-503. doi: 10.1074/jbc.M508739200. Epub 2005 Oct 12.

Abstract

HuCC49 deltaCH2 is a heavy chain constant domain 2 domain-deleted antibody under development as a radioimmunotherapeutic for treating carcinomas overexpressing the TAG-72 tumor antigen. Mammalian cell culture biosynthesis of HuCC49 deltaCH2 produces two isoforms (form A and form B) in an approximate 1:1 ratio, and consequently separation and purification of the desired form A isoform adversely impact process and yield. A protein engineering strategy was used to develop a panel of hinge-engineered HuCC49 deltaCH2 antibodies to identify hinge sequences to optimize production of the form A isoform. We found that adding a single proline residue at Kabat position 243, immediately adjacent to the carboxyl end of the core middle hinge CPPC domain, resulted in an increase from 39 to 51% form A isoform relative to the parent HuCC49 deltaCH2 antibody. Insertion of the amino acids proline-alanine-proline (PAP) at positions 243-245 enhanced production of the form A isoform to 72%. Insertion of a cysteine-rich 15-amino acid IgG3 hinge motif (CPEPKSCDTPPPCPR) in both of these mutant antibodies resulted in secretion of predominantly form A isoform with little or no detectable form B. Yields exceeding 98% of the form A isoform have been realized. Preliminary peptide mapping and mass spectrometry analysis suggest that at least two, and as many as five, inter-heavy chain disulfide linkages may be present.

MeSH terms

  • Amino Acid Motifs
  • Animals
  • Antibodies / chemistry
  • Antibodies, Monoclonal / chemistry
  • Antibodies, Neoplasm / chemistry
  • Binding, Competitive
  • Blotting, Western
  • CHO Cells
  • Cattle
  • Cricetinae
  • Disulfides / chemistry
  • Electrophoresis, Polyacrylamide Gel
  • Genetic Vectors
  • Hypoxia
  • Immunohistochemistry
  • Mass Spectrometry
  • Models, Biological
  • Models, Molecular
  • Mucins / chemistry
  • Mutation
  • Oligonucleotides / chemistry
  • Peptide Mapping
  • Peptides / chemistry
  • Plasmids / metabolism
  • Protein Binding
  • Protein Conformation
  • Protein Engineering / methods*
  • Protein Isoforms
  • Protein Structure, Tertiary
  • Radioimmunotherapy / methods*
  • Spectrometry, Fluorescence
  • Time Factors

Substances

  • Antibodies
  • Antibodies, Monoclonal
  • Antibodies, Neoplasm
  • Disulfides
  • Mucins
  • Oligonucleotides
  • Peptides
  • Protein Isoforms