Flexible docking and design

Annu Rev Biophys Biomol Struct. 1995:24:677-700. doi: 10.1146/annurev.bb.24.060195.003333.

Abstract

Docking and design are the major computational steps toward understanding and affecting receptor-ligand interactions. The flexibility of many ligands makes these calculations difficult and requires the development and use of special methods. The need for such tools is illustrated by two examples: the design of protease inhibitors and the analysis and design of peptide antigens binding to specific MHC receptors. We review the computational concepts that have been extended from rigid-body to flexible docking, as well as the following important strategies for flexible docking and design: (a) Monte Carlo/molecular dynamics docking, (b) in-site combinatorial search, (c) ligand build-up, and (d) site mapping and fragment assembly. The use of empirical free energy as a target function is discussed. Due to the rapid development of the methodology, most new methods have been tested on only a limited number of applications and are likely to improve results obtained by more traditional computational or graphic tools.

Publication types

  • Research Support, U.S. Gov't, Non-P.H.S.
  • Research Support, U.S. Gov't, P.H.S.
  • Review

MeSH terms

  • Algorithms
  • Computer Simulation*
  • Drug Design*
  • Histocompatibility Antigens / chemistry
  • Histocompatibility Antigens / metabolism
  • Models, Chemical*
  • Peptides / chemistry
  • Peptides / metabolism
  • Protease Inhibitors / chemistry
  • Protease Inhibitors / metabolism
  • Thermodynamics

Substances

  • Histocompatibility Antigens
  • Peptides
  • Protease Inhibitors