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Title: Inhibition of human immunodeficiency virus type 1 integration by diketo derivatives
Authors: Pluymers, Willem
Pais, Godwin
Van Maele, Bénédicte
Pannecouque, Christophe
Fikkert, Valery
Burke, Terrence R
De Clercq, Erik
Witvrouw, Myriam
Neamati, Nouri
Debyser, Zeger # ×
Issue Date: Oct-2002
Series Title: Antimicrobial Agents and Chemotherapy vol:46 issue:10 pages:3292-7
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.
URI: 
ISSN: 0066-4804
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Laboratory of Virology and Chemotherapy (Rega Institute)
Molecular Virology and Gene Therapy
× corresponding author
# (joint) last author

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