Design of peptide affinity ligands for S-protein: a comparison of combinatorial and de novo design strategies

Mol Divers. 2013 May;17(2):357-69. doi: 10.1007/s11030-013-9436-z. Epub 2013 Mar 27.

Abstract

Design of peptide affinity ligands against biological targets is important for a broad range of applications. Here, we report on de novo and combinatorial strategies for the design of high-affinity and high-specificity peptides against S-protein as a target. The peptide libraries employed in this study contain (1) consensus motif (CM) sequences identified from high-throughput phage combinatorial screening, (2) point mutations of CM sequences, and (3) de novo sequences rationally designed based on stereo-chemical information of the complex between S-protein and its natural ligand, S-peptide. In general, point mutations to CM allowed for modulating peptide affinity and specificity over a broad range. This is particularly useful in designing peptides with varying affinities and specificities for the target. De novo sequences, especially those based on the S-protein binding pocket, on average bound with higher affinities within a narrow range (10-100 nM) as compared to point mutations to CM (1 nM-2 μM). As such, the approaches described here serve as a general guide for optimizing the design of peptide affinity ligands for a wide range of target proteins or applications.

MeSH terms

  • Affinity Labels / chemical synthesis*
  • Affinity Labels / chemistry
  • Animals
  • Cattle
  • Combinatorial Chemistry Techniques
  • Consensus Sequence
  • Crystallography, X-Ray
  • Ligands
  • Molecular Docking Simulation
  • Molecular Sequence Data
  • Peptide Fragments / chemistry*
  • Peptide Fragments / genetics
  • Peptide Library
  • Peptides / chemical synthesis*
  • Peptides / chemistry
  • Point Mutation
  • Protein Interaction Domains and Motifs
  • Protein Structure, Tertiary
  • Ribonucleases / chemistry*
  • Ribonucleases / genetics

Substances

  • Affinity Labels
  • Ligands
  • Peptide Fragments
  • Peptide Library
  • Peptides
  • ribonuclease S-peptide
  • Ribonucleases