Development of low molecular weight HIV-1 protease dimerization inhibitors

J Med Chem. 2005 Mar 24;48(6):2239-42. doi: 10.1021/jm049581j.

Abstract

The role of HIV protease in viral replication has made it a significant target for inhibition. The focus of our studies is to target the dimerization interface of HIV-1 protease because disruption of the dimer will inhibit enzymatic activity. The initial strategy began with cross-linked peptides derived from the interface of HIV protease. Herein we describe the design of a focused library of agents based on a minimal pharmacophore for HIV-1 protease dimerization inhibition.

Publication types

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

MeSH terms

  • Combinatorial Chemistry Techniques
  • Cross-Linking Reagents / chemistry
  • Dimerization
  • HIV Protease / chemistry*
  • HIV Protease / genetics
  • HIV Protease Inhibitors / chemical synthesis*
  • HIV Protease Inhibitors / chemistry
  • Models, Molecular
  • Molecular Weight
  • Mutation
  • Oligopeptides / chemical synthesis*
  • Oligopeptides / chemistry
  • Structure-Activity Relationship

Substances

  • Cross-Linking Reagents
  • HIV Protease Inhibitors
  • Oligopeptides
  • HIV Protease