The Application of Ligand-Mapping Molecular Dynamics Simulations to the Rational Design of Peptidic Modulators of Protein-Protein Interactions

J Chem Theory Comput. 2015 Jul 14;11(7):3199-210. doi: 10.1021/ct5010577. Epub 2015 Jun 22.

Abstract

A computational ligand-mapping approach to detect protein surface pockets that interact with hydrophobic moieties is presented. In this method, we incorporated benzene molecules into explicit solvent molecular dynamics simulations of various protein targets. The benzene molecules successfully identified the binding locations of hydrophobic hot-spot residues and all-hydrocarbon cross-links from known peptidic ligands. They also unveiled cryptic binding sites that are occluded by side chains and the protein backbone. Our results demonstrate that ligand-mapping molecular dynamics simulations hold immense promise to guide the rational design of peptidic modulators of protein-protein interactions, including that of stapled peptides, which show promise as an exciting new class of cell-penetrating therapeutic molecules.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aurora Kinase A / antagonists & inhibitors
  • Aurora Kinase A / chemistry*
  • Benzene / chemistry
  • Humans
  • Hydrophobic and Hydrophilic Interactions
  • Ligands
  • Molecular Dynamics Simulation*
  • Peptides / chemical synthesis
  • Peptides / chemistry*
  • Peptides / pharmacology
  • Protein Binding / drug effects
  • Solvents / chemistry
  • Water / chemistry

Substances

  • Ligands
  • Peptides
  • Solvents
  • Water
  • Aurora Kinase A
  • Benzene