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Research ArticleORIGINAL ARTICLE

A Novel and Efficient Approach to Discriminate between Pre- and Post-Transcription HIV Inhibitors

Dirk Daelemans, Christophe Pannecouque, George N. Pavlakis, Oriana Tabarrini and Erik De Clercq
Molecular Pharmacology May 2005, 67 (5) 1574-1580; DOI: https://doi.org/10.1124/mol.104.010249
Dirk Daelemans
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Christophe Pannecouque
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George N. Pavlakis
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Oriana Tabarrini
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Erik De Clercq
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Abstract

Established anti-human immunodeficiency virus (HIV) treatments are not always effective or well tolerated, highlighting the need for further refinement of antiviral drug design and development. Given the multitude of molecular targets with which the anti-HIV agents can interact, studies on the mechanism of action of newly discovered HIV inhibitors are quite elaborate. In this article, we describe the use of an efficient reporter system allowing rapid discrimination between a pre- or post-transcriptional mode of action of anti-HIV compounds based on infection by a replication competent HIV-1 molecular clone expressing the green fluorescent protein as part of the nef multiply spliced RNA. Using fluorescence microscopy and flow cytometry, this system enabled us to differentiate between compounds acting at a pre- or post-transciptional level of the virus life cycle. Antiviral activities were determined for four reference compounds as well as one putative novel HIV inhibitor. The results obtained were in agreement with the known characteristics of the reference compounds and revealed that the novel compound interfered with a target before or overlapping with HIV transcription. We showed that during a single replication cycle, compounds inhibiting a molecular target occurring before or coinciding with HIV transcription suppressed GFP expression, whereas compounds interfering at a later stage (such as protease inhibitors, which act after transcription) did not inhibit GFP expression. This GFP-based reporter system is adaptable for high-throughput screening.

  • Received December 13, 2004.
  • Accepted February 11, 2005.
  • The American Society for Pharmacology and Experimental Therapeutics
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Molecular Pharmacology: 67 (5)
Molecular Pharmacology
Vol. 67, Issue 5
1 May 2005
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Research ArticleORIGINAL ARTICLE

A Novel and Efficient Approach to Discriminate between Pre- and Post-Transcription HIV Inhibitors

Dirk Daelemans, Christophe Pannecouque, George N. Pavlakis, Oriana Tabarrini and Erik De Clercq
Molecular Pharmacology May 1, 2005, 67 (5) 1574-1580; DOI: https://doi.org/10.1124/mol.104.010249

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Research ArticleORIGINAL ARTICLE

A Novel and Efficient Approach to Discriminate between Pre- and Post-Transcription HIV Inhibitors

Dirk Daelemans, Christophe Pannecouque, George N. Pavlakis, Oriana Tabarrini and Erik De Clercq
Molecular Pharmacology May 1, 2005, 67 (5) 1574-1580; DOI: https://doi.org/10.1124/mol.104.010249
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