Mapping of the binding landscape for a picomolar protein-protein complex through computation and experiment

Structure. 2014 Apr 8;22(4):636-45. doi: 10.1016/j.str.2014.01.012. Epub 2014 Mar 6.

Abstract

Our understanding of protein evolution would greatly benefit from mapping of binding landscapes, i.e., changes in protein-protein binding affinity due to all single mutations. However, experimental generation of such landscapes is a tedious task due to a large number of possible mutations. Here, we use a simple computational protocol to map the binding landscape for two homologous high-affinity complexes, involving a snake toxin fasciculin and acetylcholinesterase from two different species. To verify our computational predictions, we experimentally measure binding between 25 Fas mutants and the 2 enzymes. Both computational and experimental results demonstrate that the Fas sequence is close to the optimum when interacting with its targets, yet a few mutations could further improve Kd, kon, and koff. Our computational predictions agree well with experimental results and generate distributions similar to those observed in other high-affinity PPIs, demonstrating the potential of simple computational protocols in capturing realistic binding landscapes.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetylcholinesterase / chemistry*
  • Acetylcholinesterase / genetics
  • Amino Acid Sequence
  • Animals
  • Binding Sites
  • Cholinesterase Inhibitors / chemistry*
  • Elapid Venoms / chemistry*
  • Escherichia coli / genetics
  • Escherichia coli / metabolism
  • Gene Expression
  • Humans
  • Kinetics
  • Models, Molecular
  • Molecular Sequence Data
  • Mutation
  • Peptide Mapping / statistics & numerical data*
  • Protein Binding
  • Recombinant Proteins / chemistry
  • Recombinant Proteins / genetics
  • Thermodynamics
  • Torpedo

Substances

  • Cholinesterase Inhibitors
  • Elapid Venoms
  • Recombinant Proteins
  • fasciculin
  • Acetylcholinesterase