Tautomerism in computer-aided drug design

J Recept Signal Transduct Res. 2003;23(4):361-71. doi: 10.1081/rrs-120026975.

Abstract

Tautomers are often disregarded in computer-aided molecular modeling applications. Little is known about the different tautomeric states of a molecule and they are rarely registered in chemical databases. Tautomeric forms of a molecule differ in shape, functional groups, surface, and hydrogen-bonding pattern. Calculation of physical-chemical properties and molecular descriptors differ from one tautomeric state to the other as it is demonstrated with an example of the log P calculation, similarity index, and the complementarity pattern to the targeted protein. Considering tautomery in ligand-protein interactions therefore has a significant impact on the prediction of the ligand binding using various docking techniques. This article points on hitherto unaddressed issue of tautomerism in computer-aided drug design.

Publication types

  • Review

MeSH terms

  • Binding Sites
  • Computer Simulation*
  • Databases as Topic
  • Drug Design*
  • Hydrogen Bonding
  • Hydrogen-Ion Concentration
  • Kinetics
  • Ligands
  • Models, Chemical
  • Models, Molecular
  • Molecular Conformation
  • Software

Substances

  • Ligands