Small molecule inhibitor of HIV-1 nuclear import suppresses HIV-1 replication in human lymphoid tissue ex vivo

A potential addition to current anti-HIV drug repertoire

Svetlana Glushakova, Larisa Dubrovsky, Jean-Charles B. Grivel, Omar Haffar, Michael Bukrinsky

Research output: Contribution to journalArticle

8 Citations (Scopus)

Abstract

Despite recent progress in anti-HIV therapy, which has to do mainly with introduction of protease inhibitors into clinical practice, drug toxicity and emergence of drug-resistant isolates during the long-term treatment of the patients necessitates search for new drugs that can be added to currently used components of a multi-drug cocktail in highly active anti-retroviral therapy (HAART). Recently, we described a class of arylene bis(methylketone) compounds that inhibit nuclear import of HIV-1 pre-integration complexes and suppress viral replication in macrophages and PBMC in vitro. In this report, we demonstrate that one of these compounds, CNI-H1194, inhibited HIV-1 replication in primary lymphoid tissue ex vivo. The compound did not antagonize the activity of currently used anti-HIV drugs that inhibit viral reverse transcriptase or protease. These results suggest that arylene bis(methylketone) compounds might be a valuable addition to HAART. (C) 2000 Elsevier Science B.V.

Original languageEnglish
Pages (from-to)89-95
Number of pages7
JournalAntiviral Research
Volume47
Issue number2
DOIs
Publication statusPublished - Aug 2000
Externally publishedYes

Fingerprint

Anti-HIV Agents
Cell Nucleus Active Transport
Lymphoid Tissue
HIV-1
Pharmaceutical Preparations
RNA-Directed DNA Polymerase
Therapeutics
Protease Inhibitors
Drug-Related Side Effects and Adverse Reactions
Peptide Hydrolases
Macrophages
HIV

Keywords

  • Histoculture
  • Lymphoid tissue
  • Nuclear import inhibitor
  • Reverse transcriptase

ASJC Scopus subject areas

  • Virology
  • Pharmacology

Cite this

Small molecule inhibitor of HIV-1 nuclear import suppresses HIV-1 replication in human lymphoid tissue ex vivo : A potential addition to current anti-HIV drug repertoire. / Glushakova, Svetlana; Dubrovsky, Larisa; Grivel, Jean-Charles B.; Haffar, Omar; Bukrinsky, Michael.

In: Antiviral Research, Vol. 47, No. 2, 08.2000, p. 89-95.

Research output: Contribution to journalArticle

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