Structural basis of IL-23 antagonism by an Alphabody protein scaffold

Nat Commun. 2014 Oct 30:5:5237. doi: 10.1038/ncomms6237.

Abstract

Protein scaffolds can provide a promising alternative to antibodies for various biomedical and biotechnological applications, including therapeutics. Here we describe the design and development of the Alphabody, a protein scaffold featuring a single-chain antiparallel triple-helix coiled-coil fold. We report affinity-matured Alphabodies with favourable physicochemical properties that can specifically neutralize human interleukin (IL)-23, a pivotal therapeutic target in autoimmune inflammatory diseases such as psoriasis and multiple sclerosis. The crystal structure of human IL-23 in complex with an affinity-matured Alphabody reveals how the variable interhelical groove of the scaffold uniquely targets a large epitope on the p19 subunit of IL-23 to harness fully the hydrophobic and hydrogen-bonding potential of tryptophan and tyrosine residues contributed by p19 and the Alphabody, respectively. Thus, Alphabodies are suitable for targeting protein-protein interfaces of therapeutic importance and can be tailored to interrogate desired design and binding-mode principles via efficient selection and affinity-maturation strategies.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Cell Line
  • Drug Evaluation, Preclinical
  • Humans
  • Interleukin-23 / antagonists & inhibitors*
  • Male
  • Mice
  • Mice, Inbred C57BL
  • Molecular Sequence Data
  • Peptides / chemistry*
  • Peptides / therapeutic use
  • Psoriasis / prevention & control

Substances

  • Interleukin-23
  • Peptides

Associated data

  • PDB/4OE8
  • PDB/4OG9