1887

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Volume 68, Issue 8

Inhibition of Human Immunodeficiency Virus Type I Reverse Transcriptase by Suramin-related Compounds Free

Abstract

Summary

Ninety analogues of suramin have been examined for their ability to inhibit the exogenous reverse transcriptase (RT) of human immunodeficiency virus type I (HIV- I). Of these compounds, 57 inhibited the poly(rC)oligo(dG)-dependent RT activity. Three classes of dose-response curves could be discriminated. Allocation of a compound to one class did not correspond with obvious structural features. Twenty- four substances were superior to suramin in our RT inhibition assay. The RT- inhibitory activity of these compounds did not correlate with their effect against filariae or trypanosomes. Preliminary antiviral evaluation in susceptible human T cells inoculated with HIV-I demonstrated therapeutic efficacy for some compounds with lower drug-related cellular toxicity than suramin. Certain structural features relevant for the RT-inhibitory effect of these compounds were recognized. Predictions are made for the design of more effective RT inhibitors. Such compounds will help to understand the molecular mechanism of reverse transcription and might be useful in the therapy of retroviral infections.

  • Received:
  • Accepted:
  • Published Online:
Keyword(s): HIV-I , reverse transcriptase and suramin-related compounds
© The Journal of General Virology 1987
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1987-08-01
2024-04-23
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Inhibition of Human Immunodeficiency Virus Type I Reverse Transcriptase by Suramin-related Compounds
J. Gen. Virol. 68, 2183 (1987); https://doi.org/10.1099/0022-1317-68-8-2183
/content/journal/jgv/10.1099/0022-1317-68-8-2183
/content/journal/jgv/10.1099/0022-1317-68-8-2183
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