Title: Discovery of TSAO derivatives with an unusual HIV-1 activity/resistance profile
Authors: de Castro, Sonia ×
García-Aparicio, Carlos
Van Laethem, Kristel
Gago, Federico
Lobatón, Esther
De Clercq, Erik
Balzarini, Jan
Camarasa, María-José
Velázquez, Sonsoles #
Issue Date: Aug-2006
Publisher: Elsevier/North-Holland
Series Title: Antiviral Research vol:71 issue:1 pages:15-23
Abstract: The very first TSAO derivative that lacks the 4''-amino group at the 3'-spiro moiety (compound 3) has been prepared and the effect of this modification on the activity/resistance profile has been evaluated. This molecule proved HIV-1 specific (NNRTI-characteristic). A mixture of wild-type and V106V/A or L234L/I mutations were found in the RT of some, but not all compound 3-resistant virus strains. Compound 3 does not select for the TSAO-specific E138K mutation in the RT. However, the compound markedly lost its antiviral potential against a variety of virus strains that contain NNRTI-characteristic mutations in RT including E138K. The deaminated TSAO compound must fit differently in the HIV-1 RT enzyme than its prototype TSAO-m(3)T.
ISSN: 0166-3542
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Laboratory of Virology and Chemotherapy (Rega Institute)
Laboratory of Clinical and Epidemiological Virology (Rega Institute)
× corresponding author
# (joint) last author

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