Title: Highly specific inhibition of human immunodeficiency virus type 1 by a novel 6-substituted acyclouridine derivative
Authors: Baba, M ×
Tanaka, H
De Clercq, Erik
Pauwels, R
Balzarini, Jan
Schols, Dominique
Nakashima, H
Perno, C F
Walker, R T
Miyasaka, T #
Issue Date: Dec-1989
Series Title: Biochemical and Biophysical Research Communications vol:165 issue:3 pages:1375-81
Abstract: A novel 6-substituted acyclouridine derivative, 1-[(2-hydroxy-ethoxy) methyl]-6-phenylthiothymine (HEPT), has proved to be a potent and selective inhibitor of human immunodeficiency virus type 1 (HIV-1) in vitro. HEPT inhibits HIV-1 replication in various T4 cell cultures as well as peripheral blood lymphocytes and macrophages. The 50% antiviral effective concentration for HIV-1 (HTLV-IIIB) in MT-4 cells is 7.0 microM, while the 50% cytotoxic concentration for mock-infected MT-4 cells is 740 microM. Although HEPT is inhibitory to various strains of HIV-1, it has no effect on the replication of other retroviruses including HIV type 2. In contrast with the dideoxynucleoside (i.e. azidothymidine) 5'-triphosphates, the triphosphate of HEPT does not interact with HIV-1 reverse transcriptase. The mechanism of action of HEPT remains subject of further study.
ISSN: 0006-291X
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Laboratory of Virology and Chemotherapy (Rega Institute)
× corresponding author
# (joint) last author

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