Single-chain Fv with manifold N-glycans as bifunctional scaffolds for immunomolecules

Protein Eng. 1998 Dec;11(12):1277-83. doi: 10.1093/protein/11.12.1277.

Abstract

Unlike natural antibodies, single-chain Fv (sFv) proteins normally lack asparagine-linked glycosylation. Many designed immunoconjugates and other therapeutics currently employ the advantageous conjugation chemistry or targeting properties provided by the glycoprotein oligosaccharide domain. sFv proteins with engineered N-glycan designs were evaluated in Pichia pastoris for glycosylation efficiency, expression level, oligosaccharide chain length and composition, and affinity. In contrast to nearly all natural glycoproteins, the engineered attachment of N-glycans conveniently near the polypeptide C-terminus was found to produce the optimal results. Furthermore, the percentage modification and chain length of the attached mannose chains were controllable by the use of tandem and overlapping Asn-X-Thr tripeptide sites. The glycosylated sFv mannose chains could be effectively conjugated to polyethylene glycol and the resulting conjugate displayed a 10-fold increased circulating life in mice. The potential to control polymer:sFv or drug:sFv molar ratios by site-specific conjugation may substantially improve the therapeutic efficacy of these minimal antigen-binding molecules.

MeSH terms

  • Animals
  • Antibodies / chemistry*
  • Antibodies / genetics
  • Carbohydrate Conformation
  • Carbohydrate Sequence
  • Female
  • Gene Expression
  • Glycosylation
  • Immunoconjugates / chemistry*
  • Immunoglobulin G / chemistry
  • Immunoglobulin Variable Region / chemistry*
  • Immunoglobulin Variable Region / genetics
  • Mannose / chemistry
  • Mice
  • Molecular Sequence Data
  • Mutagenesis, Site-Directed
  • Pichia / genetics
  • Polyethylene Glycols
  • Polysaccharides / chemistry*

Substances

  • Antibodies
  • Immunoconjugates
  • Immunoglobulin G
  • Immunoglobulin Variable Region
  • Polysaccharides
  • Polyethylene Glycols
  • Mannose