A synthetic mimic of a discontinuous binding site on interleukin-10

Nat Biotechnol. 1999 Mar;17(3):271-5. doi: 10.1038/7018.

Abstract

We synthetically reconstructed a discontinuous binding site on interleukin-10 (IL-10) that recognizes the neutralizing anti-IL-10 antibody CB/RS/1. To design the 32-mer IL-10 mimic, a discontinuous interaction site on IL-10 was mapped, and binding studies with epitope-derived peptides led to specific replacement of several amino acids. Both parts of the interaction site were combined by addition of a linker molecule. Systematic analoging of the combined molecule then led to introduction of several additional substitutions in both regions and the linker. All possible disulfide bridge-containing variants of the 32-mer were tested by binding studies. Parallel syntheses were performed on continuous cellulose membranes by spot synthesis. As a result, a conformationally stabilized IL-10-derived molecule was obtained that both binds to and neutralizes the biological activity of CB/RS/1 in the low nanomolar range. This synthetic approach is a powerful alternative to phage display methods for the design of protein mimics.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Substitution
  • Binding Sites / physiology*
  • Binding, Competitive
  • Dose-Response Relationship, Drug
  • Enzyme-Linked Immunosorbent Assay
  • Epitopes
  • Humans
  • Interleukin-10 / chemistry*
  • Kinetics
  • Leukocytes, Mononuclear / metabolism
  • Lipopolysaccharides / metabolism
  • Peptide Biosynthesis
  • Peptide Mapping
  • Tumor Necrosis Factor-alpha / metabolism

Substances

  • Epitopes
  • Lipopolysaccharides
  • Tumor Necrosis Factor-alpha
  • Interleukin-10