Coevolutionary analysis of resistance-evading peptidomimetic inhibitors of HIV-1 protease

Proc Natl Acad Sci U S A. 1999 Feb 16;96(4):1369-74. doi: 10.1073/pnas.96.4.1369.

Abstract

We have developed a coevolutionary method for the computational design of HIV-1 protease inhibitors selected for their ability to retain efficacy in the face of protease mutation. For HIV-1 protease, typical drug design techniques are shown to be ineffective for the design of resistance-evading inhibitors: An inhibitor that is a direct analogue of one of the natural substrates will be susceptible to resistance mutation, as will inhibitors designed to fill the active site of the wild-type or a mutant enzyme. Two design principles are demonstrated: (i) For enzymes with broad substrate specificity, such as HIV-1 protease, resistance-evading inhibitors are best designed against the immutable properties of the active site-the properties that must be conserved in any mutant protease to retain the ability to bind and cleave all of the native substrates. (ii) Robust resistance-evading inhibitors can be designed by optimizing activity simultaneously against a large set of mutant enzymes, incorporating as much of the mutational space as possible.

Publication types

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

MeSH terms

  • Amino Acid Sequence
  • Amino Acid Substitution
  • Drug Design
  • Evolution, Molecular*
  • HIV Protease / chemistry
  • HIV Protease / genetics*
  • HIV Protease / metabolism*
  • HIV Protease Inhibitors / chemical synthesis*
  • HIV Protease Inhibitors / pharmacology*
  • HIV-1 / enzymology
  • HIV-1 / genetics
  • Kinetics
  • Point Mutation*
  • Thermodynamics

Substances

  • HIV Protease Inhibitors
  • HIV Protease