A highly stable polyethylene glycol-conjugated human single-chain antibody neutralizing granulocyte-macrophage colony stimulating factor at low nanomolar concentration

Protein Eng Des Sel. 2006 Oct;19(10):461-70. doi: 10.1093/protein/gzl031. Epub 2006 Jul 25.

Abstract

GM-CSF (granulocyte-macrophage colony stimulating factor) plays a central role in inflammatory processes. Treatment with antibodies neutralizing murine GM-CSF showed significant therapeutic effects in mouse models of inflammatory diseases. We constructed by phage display technology a human scFv, which could potently neutralize human GM-CSF. At first, a human V(L) repertoire was combined with the V(H) domain of a parental GM-CSF-neutralizing rat antibody. One dominant rat/human scFv clone was selected, neutralizing human GM-CSF with an IC50 of 7.3 nM. The human V(L) of this clone was then combined with a human V(H) repertoire. The latter preserved the CDR 3 of the parental rat V(H) domain to retain binding specificity. Several human scFvs were selected, which neutralized human GM-CSF at low nanomolar concentrations (IC50 > or = 2.6 nM). To increase serum half-life, a branched 40 kDa PEG-polymer was coupled to the most potent GM-CSF-neutralizing scFv (3077) via an additional C-terminal cysteine. PEG conjugation had a negligible effect on the in vitro neutralizing potential of the scFv, although it caused a significant drop in binding affinity owing to a reduced on-rate. It also significantly increased the stability of the scFv at elevated temperatures. In mouse experiments, the PEGylated scFv 3077 showed a significantly prolonged elimination half-life of 59 h as compared with 2 h for the unconjugated scFv version. PEGylated scFv 3077 is a potential candidate for development of a novel antibody therapy to treat pro-inflammatory human diseases.

MeSH terms

  • Animals
  • Dose-Response Relationship, Drug
  • Granulocyte-Macrophage Colony-Stimulating Factor / chemistry*
  • Hot Temperature
  • Humans
  • Immunoglobulin Fragments / chemistry*
  • Immunoglobulin Variable Region / chemistry*
  • Kinetics
  • Mice
  • Peptide Library
  • Polyethylene Glycols / chemistry*
  • Protein Engineering / methods
  • Protein Structure, Tertiary
  • Rats
  • Sequence Analysis, DNA

Substances

  • Immunoglobulin Fragments
  • Immunoglobulin Variable Region
  • Peptide Library
  • Polyethylene Glycols
  • Granulocyte-Macrophage Colony-Stimulating Factor