Fine tuning of the specificity of an anti-progesterone antibody by first and second sphere residue engineering

J Biol Chem. 2005 Jul 1;280(26):24880-7. doi: 10.1074/jbc.M500048200. Epub 2005 May 4.

Abstract

The specificity of anti-progesterone P15G12C12G11 antibody was improved by combination of in vitro scanning saturation mutagenesis and error-prone PCR. The most evolved mutant is able to discriminate against 5beta- or 5alpha-dihydroprogesterone, 23 and 15 times better than the starting antibody, while maintaining the affinity for progesterone that remains in the picomolar range. The high level of homology with anti-progesterone monoclonal antibody DB3 allowed the construction of three-dimensional models of P15G12C12G11 based on the structures of DB3 in complex with various steroids. These models together with binding data, derived from site-directed mutagenesis, were used to build a phage library in which five first sphere positions in complementarity-determining regions 2H and 3L were varied. Variants selected by an initial screening in competition against a large excess of 5beta- or 5alpha-dihydroprogesterone were characterized by a convergent amino acid signature different from that of the wild-type antibody and had lower cross-reactivity. Binding properties of this first set of mutants were further improved by the addition of second sphere mutations selected independently from an error-prone library. The three-dimensional models of the best variant show changes in the antigen binding site that explain well the increase in selectivity. The improvements are partly linked to a change in the canonical class of the light chain third hypervariable loop.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 5-alpha-Dihydroprogesterone / chemistry
  • Amino Acid Sequence
  • Animals
  • Antibodies, Monoclonal / chemistry
  • Binding Sites
  • Binding, Competitive
  • Biosensing Techniques
  • Biotinylation
  • Cloning, Molecular
  • Dose-Response Relationship, Drug
  • Enzyme-Linked Immunosorbent Assay
  • Gene Library
  • Hybridomas / metabolism
  • Immunoglobulin Fc Fragments / chemistry
  • Inhibitory Concentration 50
  • Kinetics
  • Mice
  • Models, Molecular
  • Molecular Sequence Data
  • Mutagenesis
  • Mutagenesis, Site-Directed
  • Mutation
  • Peptide Library
  • Polymerase Chain Reaction
  • Progesterone / chemistry*
  • Protein Binding
  • Protein Engineering / methods*
  • Protein Structure, Tertiary
  • Sequence Homology, Amino Acid
  • Steroids / chemistry
  • Surface Plasmon Resonance

Substances

  • Antibodies, Monoclonal
  • Immunoglobulin Fc Fragments
  • Peptide Library
  • Steroids
  • Progesterone
  • 5-alpha-Dihydroprogesterone