Using molecular docking, 3D-QSAR, and cluster analysis for screening structurally diverse data sets of pharmacological interest

J Chem Inf Model. 2008 Oct;48(10):2054-65. doi: 10.1021/ci8001952. Epub 2008 Sep 24.

Abstract

In this study, we propose a drug design approach which includes docking, molecular fingerprints based cluster analysis, and 'induced' descriptors based receptor-dependent 3D-QSAR. The method was shown to be very useful for screening and modeling structurally diverse data sets of pharmacological interest. Different from other receptor-dependent 3D-QSAR, no ambiguous alignments are required for the construction of the models, and the computational cost is relatively lower. Moreover, 'induced' descriptors were shown to be very powerful in "capturing" ligand-receptor intermolecular interactions. The methodology was validated for eight data sets sampled from the literature and from public databases: human sex hormone-binding globulin, human corticosteroid-binding globulin, anthrax lethal factor, HIV-1 reverse transcriptase, neuraminidase A, thrombin, trypsin, and Pneumocystis carinii dihydrofolate reductase data sets. The resulting models were interpretable; the constructed QSAR equations have high statistical significance and predictive strength; and the drug design solutions were shown to be useful for guiding ligand modification for the development of new inhibitors for a broad range of molecular targets.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Algorithms
  • Cluster Analysis
  • Databases, Factual*
  • Drug Evaluation, Preclinical / methods*
  • Genetics / statistics & numerical data
  • Ligands
  • Models, Molecular
  • Peptide Mapping
  • Protein Binding*
  • Protein Conformation
  • Quantitative Structure-Activity Relationship*
  • Receptors, Drug / chemistry

Substances

  • Ligands
  • Receptors, Drug