Contribution of antibody heavy chain CDR1 to digoxin binding analyzed by random mutagenesis of phage-displayed Fab 26-10

J Biol Chem. 1995 Dec 1;270(48):28541-50. doi: 10.1074/jbc.270.48.28541.

Abstract

We constructed a bacteriophage-displayed library containing randomized mutations at H chain residues 30-35 of the anti-digoxin antibody 26-10 Fab to investigate sequence constraints necessary for high affinity binding in an antibody of known crystal structure. Phage were selected by panning against digoxin and three C-16-substituted analogues. All antigen-positive mutants selected using other analogues also bound digoxin. Among 73 antigen-positive clones, 26 different nucleotide sequences were found. The majority of Fabs had high affinity for digoxin (Ka 3.4 x 10(9) M-1) despite wide sequence diversity. Two mutants displayed affinities 2- and 4-fold higher than the parental antibody. Analysis of the statistical distribution of sequences showed that highest affinity binding occurred with a restricted set of amino acid substitutions at positions H33-35. All clones save two retained the parental Asn-H35, which contacts hapten and hydrogen bonds to other binding site residues in the parental structure. Positions H30-32 display remarkable diversity, with 10-14 different substitutions for each residue, consistent with high affinity binding. Thus complementarity can be retained and even improved despite diversity in the conformation of the N-terminal portion of the H-CDR1 loop.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Antibodies / immunology
  • Antibodies / metabolism
  • Bacteriophages / genetics*
  • Base Sequence
  • Binding Sites
  • Cell Line
  • Cloning, Molecular
  • DNA Primers / chemistry
  • Digoxin / immunology
  • Digoxin / metabolism*
  • Immunoglobulin Fab Fragments / genetics*
  • Immunoglobulin Variable Region / physiology*
  • Mice
  • Molecular Sequence Data
  • Mutagenesis

Substances

  • Antibodies
  • DNA Primers
  • Immunoglobulin Fab Fragments
  • Immunoglobulin Variable Region
  • Digoxin