Potent inhibition of drug-resistant HIV protease variants by monoclonal antibodies

Antiviral Res. 2008 Jun;78(3):275-7. doi: 10.1016/j.antiviral.2008.01.009. Epub 2008 Feb 20.

Abstract

The monoclonal antibodies 1696 and F11.2.32 strongly inhibit the activity of wild-type HIV-1 protease (PR) by binding to epitopes at the enzyme N-terminus (residues 1-6) and flap residues 36-46, respectively. Here we demonstrate that these antibodies are also potent inhibitors of PR variants resistant to active-site inhibitors used as anti-AIDS drugs. Our in vitro experiments revealed that the inhibitory potency of single-chain fragments (scFv) of these antibodies is not significantly affected by the presence of mutations in PR; inhibition constants for drug-resistant protease variants are 5-11 nM and 13-169 nM for scFv1696 and for scFvF11.2.32, respectively. Tethered dimer of HIV-1 PR variant proved to be a model protease variant resistant to dissociative inhibition by 1696, and, strikingly, it also displayed resistance to inhibition by F11.2.32 suggesting that dimer dissociation also plays a role in the inhibitory action of F11.2.32.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antibodies, Monoclonal / immunology
  • Antibodies, Monoclonal / pharmacology*
  • Antiretroviral Therapy, Highly Active
  • Dimerization
  • Drug Resistance, Viral / genetics*
  • Genetic Variation*
  • HIV Infections / drug therapy
  • HIV Infections / virology
  • HIV Protease / drug effects*
  • HIV Protease / genetics
  • HIV Protease / immunology
  • HIV Protease Inhibitors / pharmacology
  • HIV-1 / drug effects
  • HIV-1 / enzymology*
  • HIV-1 / genetics
  • Humans
  • Immunoglobulin Fragments / immunology
  • Immunoglobulin Fragments / pharmacology*
  • Models, Molecular
  • Mutation
  • Recombinant Proteins / immunology
  • Recombinant Proteins / pharmacology*

Substances

  • Antibodies, Monoclonal
  • HIV Protease Inhibitors
  • Immunoglobulin Fragments
  • Recombinant Proteins
  • immunoglobulin Fv
  • HIV Protease