2. Academic Validation
  3. Inhibition of human immunodeficiency virus type 1 integration by diketo derivatives

Inhibition of human immunodeficiency virus type 1 integration by diketo derivatives

  • Antimicrob Agents Chemother. 2002 Oct;46(10):3292-7. doi: 10.1128/AAC.46.10.3292-3297.2002.
Wim Pluymers 1,  Godwin Pais,  Bénédicte Van Maele,  Christophe Pannecouque,  Valery Fikkert,  Terrence R Burke Jr,  Erik De Clercq,  Myriam Witvrouw,  Nouri Neamati,  Zeger Debyser
Affiliations

Affiliation

  • 1 Rega Institute for Medical Research, K.U. Leuven, Minderbroedersstraat 10, Belgium.
PMID: 12234864 DOI: 10.1128/AAC.46.10.3292-3297.2002
Abstract

A series of diketo derivatives was found to inhibit human immunodeficiency virus type 1 (HIV-1) integrase activity. Only L-708,906 inhibited the replication of HIV-1(III(B)) (50% effective concentration, 12 micro M), HIV-1 clinical strains, HIV-1 strains resistant to Reverse Transcriptase or fusion inhibitors, HIV-2 (ROD strain) and simian immunodeficiency virus (MAC(251)). The combinations of L-708,906 with zidovudine, nevirapine, or nelfinavir proved to be subsynergistic. In Cell Culture, addition of L-708,906 could be postponed for 7 h after Infection, a moment coinciding with HIV integration. Inhibition of integration in Cell Culture was confirmed by quantitative Alu-PCR.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-118740
    HIV-1抑制剂
    HIV
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