Rare one and two amino acid inserts adjacent to codon 103 of the HIV-1 reverse transcriptase (RT) affect susceptibility to non-nucleoside RT inhibitors

Antivir Ther. 2005;10(2):363-6.

Abstract

HIV-1 strains that possess a one or two amino acid insert between codons 102 and 103 of the reverse transcriptase (RT) gene were identified in three HIV-1-infected individuals. Each strain also had one or more known mutations associated with nucleoside RT inhibitors (NRTIs) and non-nucleoside RT inhibitors (NNRTIs). Recombinant viruses from these strains had reduced susceptibility to efavirenz and nevirapine, and homology modelling predicted a loss of binding contacts with efavirenz. Mutagenesis studies indicated that replication of insert-containing strains was dependent on RT gene mutations and polymorphisms that co-evolved with the insert. These results suggest that inserts in the NNRTI-binding pocket contribute to NNRTI resistance, but are tolerated only under specific genetic conditions.

MeSH terms

  • Alkynes
  • Benzoxazines
  • Cell Line
  • Codon
  • Cyclopropanes
  • Drug Resistance, Viral / genetics
  • HIV Infections / virology
  • HIV-1 / drug effects
  • HIV-1 / genetics*
  • Humans
  • Models, Molecular
  • Mutation
  • Nevirapine / pharmacology
  • Nucleosides
  • Oxazines / pharmacology
  • RNA-Directed DNA Polymerase / chemistry
  • RNA-Directed DNA Polymerase / genetics*
  • Reverse Transcriptase Inhibitors / pharmacology*

Substances

  • Alkynes
  • Benzoxazines
  • Codon
  • Cyclopropanes
  • Nucleosides
  • Oxazines
  • Reverse Transcriptase Inhibitors
  • Nevirapine
  • RNA-Directed DNA Polymerase
  • efavirenz