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Review ArticleMINIREVIEW

Inhibition of HIV Infection by Bicyclams, Highly Potent and Specific CXCR4 Antagonists

Erik De Clercq
Molecular Pharmacology May 2000, 57 (5) 833-839;
Erik De Clercq
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Abstract

The bicyclams represent a new entity of low-molecular weight molecules that inhibit human immunodeficiency virus (HIV) infection through a specific blockade of CXCR4 (fusin), the receptor for the CXC chemokine SDF-1 (soluble-derived factor), which is also used as coreceptor by T-lymphotropic HIV strains to enter their target cells. The bicyclam AMD3100 or 1,1′-[1,4-phenylenebis(methylene)]-bis-1,4,8,11-tetraazacyclotetradecane octahydrochloride dihydrate, is able to block the CXCR4 receptor and to inhibit HIV replication at nanomolar concentrations while not being toxic to the host cells at 100,000-fold higher concentrations. It is the most specific and most potent CXCR4 antagonist that has been described to date.

Footnotes

  • Send reprint requests to: Prof. Dr. Erik De Clercq, Rega Institute for Medical Research, Minderbroedersstraat 10, B-3000 Leuven, Belgium. E-mail: erik.declercq{at}rega.kuleuven.ac.be

  • Abbreviations:
    RANTES
    regulated upon activation normal T cell expressed and secreted
    SIV
    simian immunodeficiency virus
    mAb
    monoclonal antibody
    PBMC
    peripheral blood mononuclear cell
    AZT
    azidothymidine (zidovudine)
    • Received December 29, 1999.
    • Accepted February 4, 2000.
  • The American Society for Pharmacology and Experimental Therapeutics
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Molecular Pharmacology: 57 (5)
Molecular Pharmacology
Vol. 57, Issue 5
1 May 2000
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Review ArticleMINIREVIEW

Inhibition of HIV Infection by Bicyclams, Highly Potent and Specific CXCR4 Antagonists

Erik De Clercq
Molecular Pharmacology May 1, 2000, 57 (5) 833-839;

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Review ArticleMINIREVIEW

Inhibition of HIV Infection by Bicyclams, Highly Potent and Specific CXCR4 Antagonists

Erik De Clercq
Molecular Pharmacology May 1, 2000, 57 (5) 833-839;
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