The inhibition of human immunodeficiency virus type 1 reverse transcriptase by avarol and avarone derivatives

Shoshana Loya, Amnon Hizi

Research output: Contribution to journalArticlepeer-review

Abstract

We have analyzed the effects of several natural compounds related to avarols and avarones on the catalytic functions of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT). The most potent substances, designated as avarone A,B and E and avarol F, inhibited indiscriminately the enzymatic activities of HIV-1 RT, namely the RNA-dependent and DNA-dependent DNA polymerase as well as the ribonuclease H. The inhibition of the DNA polymerase activity was found to be non-competitive with respect to either the template-primer or the deoxynucleotide-triphosphate. These studies suggest that the hydroxyl group at the ortho position to the carbonyl group at the quinone ring is involved in blocking the RT activity. The identification of the active site of the inhibitors will hopefully lead to the rational design of new potent anti-HIV drugs.

Original languageEnglish
Pages (from-to)131-134
Number of pages4
JournalFEBS Letters
Volume269
Issue number1
DOIs
StatePublished - 20 Aug 1990

Keywords

  • AIDS
  • Avarol
  • Avarone
  • HIV-1
  • Inhibitor
  • Reverse transcriptase

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