Computational allosteric ligand binding site identification on Ras proteins

Acta Biochim Biophys Sin (Shanghai). 2016 Jan;48(1):3-10. doi: 10.1093/abbs/gmv100. Epub 2015 Oct 19.

Abstract

A number of computational techniques have been proposed to expedite the process of allosteric ligand binding site identification in inherently flexible and hence challenging drug targets. Some of these techniques have been instrumental in the discovery of allosteric ligand binding sites on Ras proteins, a group of elusive anticancer drug targets. This review provides an overview of these techniques and their application to Ras proteins. A summary of molecular docking and binding site identification is provided first, followed by a more detailed discussion of two specific techniques for binding site identification in ensembles of Ras conformations generated by molecular simulations.

Keywords: Ras proteins; binding site identification; molecular dynamics; probe-based simulation.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Allosteric Site
  • Antineoplastic Agents / chemistry*
  • Binding Sites
  • Catalytic Domain
  • Computational Biology
  • Computer Simulation
  • Drug Discovery
  • GTP Phosphohydrolases / chemistry
  • Guanosine Triphosphate / chemistry
  • Humans
  • Ligands
  • Lipids / chemistry
  • Molecular Docking Simulation
  • Molecular Dynamics Simulation
  • Protein Binding
  • Protein Conformation
  • Software
  • ras Proteins / chemistry*

Substances

  • Antineoplastic Agents
  • Ligands
  • Lipids
  • Guanosine Triphosphate
  • GTP Phosphohydrolases
  • ras Proteins