Subpocket analysis method for fragment-based drug discovery

J Chem Inf Model. 2013 Jan 28;53(1):131-41. doi: 10.1021/ci300523r. Epub 2013 Jan 17.

Abstract

Although two binding sites might be dissimilar overall, they might still bind the same fragments if they share suitable subpockets. Information about shared subpockets can be therefore used in fragment-based drug design to suggest new fragments or to replace existing fragments within an already known compound. A novel computational method called SubCav is described which allows the similarity searching and alignment of subpockets from a PDB-wide database against a user-defined query. The method is based on pharmacophoric fingerprints combined with a subpocket alignment algorithm. SubCav was shown to be effective in producing reasonable alignments for subpockets with low sequence similarity and be able to retrieve relevant subpockets from a large database of structures including those with different folds. It can also be used to analyze subpockets inside a protein family to facilitate drug design and to rationalize compound selectivity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Binding Sites
  • Data Mining
  • Databases, Pharmaceutical
  • Databases, Protein
  • Drug Design
  • Drug Discovery / methods*
  • HSP90 Heat-Shock Proteins / chemistry
  • HSP90 Heat-Shock Proteins / metabolism
  • Histone Methyltransferases
  • Histone-Lysine N-Methyltransferase / chemistry
  • Histone-Lysine N-Methyltransferase / metabolism
  • Humans
  • Models, Molecular
  • Organophosphonates / chemistry
  • Organophosphonates / metabolism
  • Protein Conformation
  • Reproducibility of Results
  • Software

Substances

  • HSP90 Heat-Shock Proteins
  • Organophosphonates
  • Histone Methyltransferases
  • Histone-Lysine N-Methyltransferase