A hierarchical model of HIV-1 protease drug resistance

Appl Bioinformatics. 2002;1(1):3-12.

Abstract

A hierarchical model of HIV-1 drug therapy may be used to evaluate new inhibitors and test new treatment strategies that address the problem of drug resistance. The model includes an atomic representation of drug-protease interaction, evaluation of viral fitness based on cleavage of polyprotein substrates during viral maturation, evolutionary modelling of drug resistance mutations in the face of selection pressures by drug and a mathematical description of viral population dynamics in infected individuals. These techniques have been used for the design of resistance-evading inhibitors by computational coevolution techniques and for the optimisation of existing protease inhibitors for improving their robustness in the face of resistance mutation.

Publication types

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

MeSH terms

  • Catalytic Domain / genetics
  • Computational Biology
  • Computer-Aided Design
  • Directed Molecular Evolution
  • Drug Design
  • Drug Resistance, Viral / genetics
  • HIV Infections / drug therapy
  • HIV Infections / virology
  • HIV Protease / chemistry
  • HIV Protease / drug effects*
  • HIV Protease / genetics
  • HIV Protease Inhibitors / pharmacology
  • HIV-1 / drug effects*
  • HIV-1 / enzymology
  • HIV-1 / genetics
  • Humans
  • Models, Biological*
  • Models, Molecular
  • Mutation

Substances

  • HIV Protease Inhibitors
  • HIV Protease