Construction of the chimeric reverse transcriptase of simian immunodeficiency virus sensitive to nonnucleoside reverse transcriptase inhibitor

Microbiol Immunol. 1998;42(3):195-202. doi: 10.1111/j.1348-0421.1998.tb02271.x.

Abstract

A number of structurally diverse compounds have been shown to be potent inhibitors of the DNA polymerase activity of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT). The compounds can be grouped into two broad classes; nucleoside analogs and nonnucleoside RT inhibitors. The nonnucleoside RT inhibitors are quite specific for HIV-1 RT but not human immunodeficiency virus type 2 (HIV-2) and simian immunodeficiency virus (SIV) RT. We have investigated the property of SIV/HIV-1 chimeric viruses in which portions of SIV(MAC) RT were exchanged with the corresponding domain of HIV-1 RT; amino acids 176-190, 176-383 and 176-495 of HIV-1 RT. The chimeric virus, which was substituted amino acids 176-190 of RT, had detectable RT activity, and this chimeric RT was sensitive to three nonnucleoside RT inhibitors [nevirapine, HEPT derivative (E-EBU-dM) and TIBO derivative (R82913)]. To further study this chimeric virus, we purified the chimeric RT enzyme expressed in Escherichia coli and determined its kinetic properties; the Km, and Vmax values, and the Ki value of HEPT derivative calculated for the DNA polymerase activity. This study reveals that amino acids 176-190 of SIV(MAC) RT were important for the enzymatic activity and the SIV/HIV-1 chimeric RT, which had amino acids 176-190 of HIV-1, was sensitive to the nonnucleoside RT inhibitor.

MeSH terms

  • Amino Acid Sequence
  • Benzodiazepines / pharmacology
  • Cells, Cultured
  • HIV Reverse Transcriptase / drug effects
  • HIV Reverse Transcriptase / genetics
  • HIV-1 / enzymology
  • HIV-1 / growth & development
  • Humans
  • Imidazoles / pharmacology
  • Kinetics
  • Molecular Sequence Data
  • Nevirapine / pharmacology
  • RNA-Directed DNA Polymerase / drug effects*
  • RNA-Directed DNA Polymerase / genetics
  • Reassortant Viruses / enzymology
  • Reassortant Viruses / growth & development
  • Recombinant Fusion Proteins / drug effects
  • Reverse Transcriptase Inhibitors / pharmacology*
  • Simian Immunodeficiency Virus / enzymology*
  • Simian Immunodeficiency Virus / growth & development
  • Transfection
  • Uracil / analogs & derivatives*
  • Uracil / pharmacology

Substances

  • 1-ethoxymethyl-5-ethyl-6-(3,5-dimethylbenzyl)uracil
  • Imidazoles
  • Recombinant Fusion Proteins
  • Reverse Transcriptase Inhibitors
  • Benzodiazepines
  • R-82913
  • Uracil
  • Nevirapine
  • HIV Reverse Transcriptase
  • RNA-Directed DNA Polymerase