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Molecular Pharmacology

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Abstract

Antiretrovirus specificity and intracellular metabolism of 2',3' -didehydro-2',3'-dideoxythymidine (stavudine) and its 5'-monophosphate triester prodrug So324.

J Balzarini, H Egberink, K Hartmann, D Cahard, T Vahlenkamp, H Thormar, E De Clercq and C McGuigan
Molecular Pharmacology November 1996, 50 (5) 1207-1213;
J Balzarini
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H Egberink
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K Hartmann
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D Cahard
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T Vahlenkamp
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H Thormar
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E De Clercq
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C McGuigan
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Abstract

2',3'-Didehydro-2',3'-dideoxythymidine (d4T) and its lipophilic 5'-monophosphate triester prodrug, So324, were evaluated for their antiretroviral and metabolic properties in four different animal species cell lines. The antiretrovirus activity of So324 was approximately 4-10-fold greater than that of d4T against human immunodeficiency virus types 1 and 2 and simian immunodeficiency virus in human T lymphocyte CEM and MT-4 cells and against feline immunodeficiency virus in feline Crandell kidney cells, 50-fold greater against visna virus in sheep choroid plexus cells, but 5-fold inferior against murine (Moloney) sarcoma virus in murine embryo fibroblast (C3H) cells. Although the administration of both d4T and So324 resulted in the formation of the 5'-monophosphate (d4T-MP), 5'-diphosphate, and 5'-triphosphate in the different cell lines, a new d4T metabolite markedly accumulated in So324-treated cells and exceeded d4T-TP levels by 13-242-fold depending on the cell line used. This metabolite could be identified as alaninyl d4T-MP. Alanyl d4T-MP may be considered to be an intracellular depot form of d4T and/or d4T-MP, which may account for the superior antiretroviral activity of the lipophilic d4T-MP triester So324 compared with d4T.

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Molecular Pharmacology
Vol. 50, Issue 5
1 Nov 1996
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Abstract

Antiretrovirus specificity and intracellular metabolism of 2',3' -didehydro-2',3'-dideoxythymidine (stavudine) and its 5'-monophosphate triester prodrug So324.

J Balzarini, H Egberink, K Hartmann, D Cahard, T Vahlenkamp, H Thormar, E De Clercq and C McGuigan
Molecular Pharmacology November 1, 1996, 50 (5) 1207-1213;

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Abstract

Antiretrovirus specificity and intracellular metabolism of 2',3' -didehydro-2',3'-dideoxythymidine (stavudine) and its 5'-monophosphate triester prodrug So324.

J Balzarini, H Egberink, K Hartmann, D Cahard, T Vahlenkamp, H Thormar, E De Clercq and C McGuigan
Molecular Pharmacology November 1, 1996, 50 (5) 1207-1213;
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