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Molecular Pharmacology

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Research ArticleArticle

A Second Target for the Peptoid Tat/Transactivation Response Element Inhibitor CGP64222: Inhibition of Human Immunodeficiency Virus Replication by Blocking CXC-Chemokine Receptor 4-Mediated Virus Entry

Dirk Daelemans, Dominique Schols, Myriam Witvrouw, Christophe Pannecouque, Sigrid Hatse, Sonia van Dooren, François Hamy, Thomas Klimkait, Erik de Clercq and Anne-Mieke VanDamme
Molecular Pharmacology January 2000, 57 (1) 116-124;
Dirk Daelemans
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Dominique Schols
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Myriam Witvrouw
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Christophe Pannecouque
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Sigrid Hatse
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Sonia van Dooren
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François Hamy
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Thomas Klimkait
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Erik de Clercq
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Anne-Mieke VanDamme
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Abstract

The peptoid CGP64222 has been previously demonstrated to inhibit the human immunodeficiency virus (HIV) Tat/transactivation response element complex formation. It has previously been shown that CGP64222 selectively inhibits HIV-1 long terminal repeat-driven gene expression and HIV-1LAV replication in lymphocytes. Here, we show that CGP64222 inhibits the replication of a wide range of laboratory strains of HIV-1 and HIV-2 in MT-4 cells. However, CGP64222 proved inactive in MT-4 cells against HIV-1 strains that are resistant to the bicyclams. The bicyclams are known to specifically interact with CXC-chemokine receptor 4, the main coreceptor used by T-tropic HIV strains to enter the cells. Mechanism of action studies revealed that CGP64222 can inhibit the HIV replicative cycle, also through a selective interaction with the CXC-chemokine receptor 4 coreceptor.

Footnotes

  • Send reprint requests to: Dr. Dirk Daelemans, Rega Institute for Medical Research, Minderbroedersstraat 10, B-3000 Leuven, Belgium. E-mail: Dirk.Daelemans{at}uz.kuleuven.ac.be

  • ↵1 Current address: Institute for Medical Mikrobiology, University of Basle, Petersplatz 10 CH-4003 Basle, Switzerland.

  • This work was supported by grants from the Belgian Nationaal Fonds voor Wetenschappelijk Onderzoek (G.3304.96), the Geconcerteerde Onderzoeksacties (GOA 95/5), and the Biomedical Research Programme of the European Union (EU Biomed. 2 grant BMH4-CT-95-1634). D.D. acknowledges a fellowship from the Flemish Institute supporting Scientific-Technological Research in Industry (IWT).

  • Abbreviations:
    HIV
    human immunodeficiency virus
    CMV
    cytomegalovirus
    LTR
    long terminal repeat
    FITC
    fluorescein isothiocyanate
    mAb
    monoclonal antibody
    MFI
    mean fluorescence intensity
    M-tropic
    macrophage-tropic
    PBL
    peripheral blood lymphocyte
    PCR
    polymerase chain reaction
    PMA
    phorbol-12-myristate-13-acetate
    RANTES
    regulated on activation normal T cell expressed and secreted
    AZT
    3′-azido-2′,3′-dideoxythymidine
    Ag
    antigen
    ELISA
    enzyme-linked immunosorbent assay
    RT
    reverse transcription
    SDF-1α
    stromal cell-derived factor-1α
    TAR
    transactivation responsive element
    T-tropic
    T cell line-tropic
    CXCR4
    CXC-chemokine receptor 4
    MIP-1α
    macrophage inflammatory protein 1α
    • Received April 27, 1999.
    • Accepted August 20, 1999.
  • The American Society for Pharmacology and Experimental Therapeutics
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Molecular Pharmacology: 57 (1)
Molecular Pharmacology
Vol. 57, Issue 1
1 Jan 2000
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Research ArticleArticle

A Second Target for the Peptoid Tat/Transactivation Response Element Inhibitor CGP64222: Inhibition of Human Immunodeficiency Virus Replication by Blocking CXC-Chemokine Receptor 4-Mediated Virus Entry

Dirk Daelemans, Dominique Schols, Myriam Witvrouw, Christophe Pannecouque, Sigrid Hatse, Sonia van Dooren, François Hamy, Thomas Klimkait, Erik de Clercq and Anne-Mieke VanDamme
Molecular Pharmacology January 1, 2000, 57 (1) 116-124;

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Research ArticleArticle

A Second Target for the Peptoid Tat/Transactivation Response Element Inhibitor CGP64222: Inhibition of Human Immunodeficiency Virus Replication by Blocking CXC-Chemokine Receptor 4-Mediated Virus Entry

Dirk Daelemans, Dominique Schols, Myriam Witvrouw, Christophe Pannecouque, Sigrid Hatse, Sonia van Dooren, François Hamy, Thomas Klimkait, Erik de Clercq and Anne-Mieke VanDamme
Molecular Pharmacology January 1, 2000, 57 (1) 116-124;
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