Normal mode analysis as a prerequisite for drug design: application to matrix metalloproteinases inhibitors

FEBS Lett. 2006 Oct 2;580(22):5130-6. doi: 10.1016/j.febslet.2006.08.037. Epub 2006 Sep 1.

Abstract

We demonstrate the utility of normal mode analysis in correctly predicting the binding modes of inhibitors in the active sites of matrix metalloproteinases (MMPs). We show the accuracy in predicting the positions of MMP-3 inhibitors is strongly dependent on which structure is used as the target, especially when it has been energy minimized. This dependency can be overcome by using intermediate structures generated along one of the normal modes previously calculated for a given target. These results may be of prime importance for further in silico drug discovery.

MeSH terms

  • Drug Design*
  • Matrix Metalloproteinase 3 / chemistry*
  • Models, Chemical*
  • Models, Molecular*
  • Protease Inhibitors / chemistry*
  • Protein Structure, Tertiary
  • Software*
  • Structure-Activity Relationship

Substances

  • Protease Inhibitors
  • Matrix Metalloproteinase 3