A combined molecular docking-based and pharmacophore-based target prediction strategy with a probabilistic fusion method for target ranking

J Mol Graph Model. 2013 Jul:44:278-85. doi: 10.1016/j.jmgm.2013.07.005. Epub 2013 Jul 23.

Abstract

Herein, a combined molecular docking-based and pharmacophore-based target prediction strategy is presented, in which a probabilistic fusion method is suggested for target ranking. Establishment and validation of the combined strategy are described. A target database, termed TargetDB, was firstly constructed, which contains 1105 drug targets. Based on TargetDB, the molecular docking-based target prediction and pharmacophore-based target prediction protocols were established. A probabilistic fusion method was then developed by constructing probability assignment curves (PACs) against a set of selected targets. Finally the workflow for the combined molecular docking-based and pharmacophore-based target prediction strategy was established. Evaluations of the performance of the combined strategy were carried out against a set of structurally different single-target compounds and a well-known multi-target drug, 4H-tamoxifen, which results showed that the combined strategy consistently outperformed the sole use of docking-based and pharmacophore-based methods. Overall, this investigation provides a possible way for improving the accuracy of in silico target prediction and a method for target ranking.

Keywords: A probabilistic fusion method; Drug target prediction; Molecular docking; Pharmacophore.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Algorithms
  • Binding Sites
  • Cluster Analysis
  • Databases, Factual
  • Drug Design*
  • Estrogen Receptor alpha / chemistry
  • Estrogen Receptor alpha / metabolism
  • Humans
  • Molecular Conformation
  • Molecular Docking Simulation*
  • Molecular Dynamics Simulation
  • Quantitative Structure-Activity Relationship*
  • Tamoxifen / chemistry
  • Tamoxifen / metabolism

Substances

  • Estrogen Receptor alpha
  • Tamoxifen