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High throughput screening for cyanovirin-N mimetics binding to HIV-1 gp41

  1. Author:
    Beutler, J. A.
    McMahon, J. B.
    Johnson, T. R.
    O'Keefe, B. R.
    Buzzell, R. A.
    Robbins, D.
    Gardella, R.
    Wilson, J.
    Boyd, M. R.

  2. Author Address

    NCI, MTDDP, CCR, SAIC Frederick, Bldg 1052,Room 121, Frederick, MD 21702 USA NCI, MTDDP, CCR, SAIC Frederick, Frederick, MD 21702 USA NCI, Intramural Res Support Program, CCR, SAIC Frederick, Frederick, MD 21702 USA Beutler JA NCI, MTDDP, CCR, SAIC Frederick, Bldg 1052,Room 121, Frederick, MD 21702 USA
    1. Year: 2002
  2. Journal: Journal of Biomolecular Screening
    1. 7
    2. 2
    3. Pages: 105-110
  4. Type of Article: Article
  1. Abstract:

    The human immunodeficiency virus type-1 (HIV-1) envelope glycoprotein gp41 is an important mediator of viral entry into host cells. Previous studies showed that the virucidal protein cyanovirin-N (CV-N) bound to both gp120 and gp41, and that this binding was associated with its antiviral activity. We constructed an HTS assay based on the interaction of europium- labeled CV-N with recombinant glycosylated gp41 ectodomain to support identification of small-molecule mimetics of CV-N that might be developed as antiviral drug leads. Primary screening of over 107,000 natural product extracts in the assay yielded 347 confirmed hits. Secondary assays eliminated extracts that bound directly to labeled CV-N or for which the simple sugars mannose and N-acetylglucosamine blocked the interaction with gp41 (lectin activity). Extracts were further prioritized based on anti-HIV activity and other biological, biochemical, and chemical criteria. The distribution of source organism taxonomy of active extracts was analyzed, as was the cross-correlation of activity between the CV-N-gp41 binding competition assay and the previously reported CV-N-gp120 binding competition assay. A limited set of extracts was selected for bioassay-guided fractionation.

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External Sources

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  2. DOI: 10.1089/10870570252906558
  3. PMID: 12006108

Library Notes

  1. Student Author
NCI at Frederick

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