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Synthesis and HIV-1 integrase inhibitory activity of dimeric and tetrameric analogs of indolicidin

  1. Author:
    Krajewski, K.
    March, C.
    Long, Y. Q.
    Pommier, Y.
    Roller, P. P.

  2. Author Address

    NCI, CCR, Med Chem Lab, NIH, Ft Detrick, MD 21702 USA. NCI, Mol Pharmacol Lab, CCR, NIH, Bethesda, MD 20892 USA. Chinese Acad Sci, SIMM, SIBS, State Key Lab Drug Res, Shanghai 201203, Peoples R China Roller, PP, NCI, CCR, Med Chem Lab, NIH, Ft Detrick, MD 21702 USA
    1. Year: 2004
    2. Date: NOV 15
  2. Journal: Bioorganic & Medicinal Chemistry Letters
    1. 14
    2. 22
    3. Pages: 5595-5598
  4. Type of Article: Article
  1. Abstract:

    We found that indolicidin, a natural antimicrobial peptide, has HIV-1 integrase inhibitory activity. Subsequently, we also discovered analogs of indolicidin with substantially higher inhibitory potency. The dimers and tetramers of the most active sequence (ILPWKWPWWPWPP) were prepared by connection of the monomers' C-terminal ends, using lysine as a linker. The inhibitory potency of the dimeric peptide is higher than the monomeric peptide. The tetrameric peptide, prepared by connection of two dimers at C-ends using again lysine as the linker, is the most potent integrase inhibitor with IC50 value of 0.6 muM for both 3'-end processing and strand transfer. (C) 2004 Elsevier Ltd. All rights reserved

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External Sources

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  2. DOI: 10.1016/j.bmcl.2004.08.061
  3. View record in Web of Science®
  4. WOS: 000224715300028

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