Identification of protease exosite-interacting peptides that enhance substrate cleavage kinetics

Biol Chem. 2012 Sep;393(9):933-41. doi: 10.1515/hsz-2012-0162.

Abstract

Many peptidases are thought to require non-active site interaction surfaces, or exosites, to recognize and cleave physiological substrates with high specificity and catalytic efficiency. However, the existence and function of protease exosites remain obscure owing to a lack of effective methods to identify and characterize exosite-interacting substrates. To address this need, we modified the cellular libraries of peptide substrates (CLiPS) methodology to enable the discovery of exosite-interacting peptide ligands. Invariant cleavage motifs recognized by the active sites of thrombin and caspase-7 were displayed on the outer surface of bacteria adjacent to a candidate exosite-interacting peptide. Exosite peptide libraries were then screened for ligands that accelerate cleavage of the active site recognition motif using two-color flow cytometry. Exosite CLiPS (eCLiPS) identified exosite-binding peptides for thrombin that were highly similar to a critical exosite interaction motif in the thrombin substrate, protease-activated receptor 1. Protease activity probes incorporating exosite-binding peptides were cleaved ten-fold faster than substrates without exosite ligands, increasing their sensitivity to thrombin activity in vitro. For comparison, screening with caspase-7 yielded peptides that modestly enhanced (two-fold) substrate cleavage rates. The eCLiPS method provides a new tool to profile the ligand specificity of protease exosites and to develop improved substrates.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Amino Acid Sequence
  • Caspase 7 / chemistry
  • Caspase 7 / metabolism
  • Catalytic Domain
  • Humans
  • Kinetics
  • Ligands
  • Models, Molecular
  • Molecular Sequence Data
  • Peptides / chemistry*
  • Peptides / metabolism*
  • Receptor, PAR-1 / chemistry
  • Receptor, PAR-1 / metabolism
  • Substrate Specificity
  • Thrombin / chemistry*
  • Thrombin / metabolism*

Substances

  • Ligands
  • Peptides
  • Receptor, PAR-1
  • Thrombin
  • Caspase 7