Fab chains as an efficient heterodimerization scaffold for the production of recombinant bispecific and trispecific antibody derivatives

J Immunol. 2000 Dec 15;165(12):7050-7. doi: 10.4049/jimmunol.165.12.7050.

Abstract

Due to their multispecificity and versatility, bispecific Abs (BsAbs) are promising therapeutic tools in tomorrow's medicine. Especially intermediate-sized BsAbs that combine body retention with tissue penetration are valuable for therapy but necessitate expression systems that favor heterodimerization of the binding sites for large-scale application. To identify heterodimerization domains to which single-chain variable fragments (scFv) can be fused, we compared the efficiency of heterodimerization of CL and CH1 constant domains with complete L and Fd chains in mammalian cells. We found that the isolated CL:CH1 domain interaction was inefficient for secretion of heterodimers. However, when the complete L and Fd chains were used, secretion of L:Fd heterodimers was highly successful. Because these Fab chains contribute a binding moiety, C-terminal fusion of a scFv molecule to the L and/or Fd chains generated BsAbs or trispecific Abs (TsAbs) of intermediate size (75-100 kDa). These disulfide-stabilized bispecific Fab-scFv ("bibody") and trispecific Fab-(scFv)(2) ("tribody") heterodimers represent up to 90% of all secreted Ab fragments in the mammalian expression system and possess fully functional binding moieties. Furthermore, both molecules recruit and activate T cells in a tumor cell-dependent way, whereby the trispecific derivative can exert this activity to two different tumor cells. Thus we propose the use of the disulfide-stabilized L:Fd heterodimer as an efficient platform for production of intermediate-sized BsAbs and TsAbs in mammalian expression systems.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adjuvants, Immunologic / chemical synthesis
  • Adjuvants, Immunologic / genetics
  • Adjuvants, Immunologic / metabolism
  • Adjuvants, Immunologic / pharmacology
  • Animals
  • Antibodies, Bispecific / biosynthesis*
  • Antibodies, Bispecific / genetics
  • Antibodies, Bispecific / pharmacology
  • Binding Sites, Antibody / genetics
  • Cell Line
  • Cytotoxicity, Immunologic / genetics
  • Dimerization
  • Drug Stability
  • Humans
  • Immunoglobulin Constant Regions / genetics
  • Immunoglobulin Constant Regions / metabolism
  • Immunoglobulin Fab Fragments / genetics
  • Immunoglobulin Fab Fragments / metabolism*
  • Immunoglobulin Variable Region / genetics
  • Immunoglobulin Variable Region / metabolism
  • Lymphocyte Activation / genetics
  • Mice
  • Mice, Inbred BALB C
  • Mice, Inbred C3H
  • Protein Structure, Tertiary / genetics
  • Recombinant Fusion Proteins / biosynthesis*
  • Recombinant Fusion Proteins / immunology
  • Recombinant Fusion Proteins / pharmacology
  • T-Lymphocytes / immunology
  • Tumor Cells, Cultured

Substances

  • Adjuvants, Immunologic
  • Antibodies, Bispecific
  • Immunoglobulin Constant Regions
  • Immunoglobulin Fab Fragments
  • Immunoglobulin Variable Region
  • Recombinant Fusion Proteins