Engineered humanized dimeric forms of IgG are more effective antibodies

J Exp Med. 1992 Oct 1;176(4):1191-5. doi: 10.1084/jem.176.4.1191.

Abstract

Humanized IgG1 M195 (HuG1-M195), a complementarity determining region-grafted recombinant monoclonal antibody, is reactive with CD33, an antigen expressed on myelogenous leukemia cells. M195 is in use in trials for the therapy of acute myelogenous leukemia. Since biological activity of IgG may depend, in part, on multimeric Fab and Fc clustering, homodimeric forms of HuG1-M195 were constructed by introducing a mutation in the gamma 1 chain CH3 region gene to change a serine to a cysteine, allowing interchain disulfide bond formation at the COOH terminal of the IgG. Despite similar avidity, the homodimeric IgG showed a dramatic improvement in the ability to internalize and retain radioisotope in target leukemia cells. Moreover, homodimers were 100-fold more potent at complement-mediated leukemia cell killing and antibody-dependent cellular cytotoxicity using human effectors. Therefore, genetically engineered multimeric constructs of IgG may have advantages relative to those forms that are found naturally.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Antibodies, Monoclonal / genetics
  • Antibodies, Monoclonal / immunology*
  • Antibodies, Monoclonal / metabolism
  • Antibody-Dependent Cell Cytotoxicity
  • Cell Line
  • Cell Membrane / immunology
  • Flow Cytometry
  • Humans
  • Immunoglobulin Constant Regions / genetics
  • Immunoglobulin Constant Regions / immunology
  • Immunoglobulin Fab Fragments / immunology
  • Immunoglobulin Fc Fragments / immunology
  • Immunoglobulin G / genetics
  • Immunoglobulin G / immunology*
  • Immunoglobulin G / metabolism
  • Leukemia, Promyelocytic, Acute
  • Lymphocytes / immunology*
  • Macromolecular Substances
  • Mutagenesis, Site-Directed
  • Protein Engineering
  • Recombinant Proteins / immunology
  • Recombinant Proteins / metabolism

Substances

  • Antibodies, Monoclonal
  • Immunoglobulin Constant Regions
  • Immunoglobulin Fab Fragments
  • Immunoglobulin Fc Fragments
  • Immunoglobulin G
  • Macromolecular Substances
  • Recombinant Proteins