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EnglishSo324 is a 2',3'-dideoxy-2',3'-didehydrothymidine-5'-monophosphate (d4T-MP) prodrug containing at the phosphate moiety a phenyl group and the methylester of alanine linked to the phosphate through a phosphoramidate linkage. So324 has anti-HIV activity in human GEM, MT4, and monocyte/macrophage cells that is superior to that of d4T. In contrast to d4T, So324 is also able to inhibit HIV replication in thymidine kinase-deficient CEM cells, After uptake of So324 by intact human lymphocytes, d4T-MP is released and subsequently converted intracellularly to d4T-TP. In addition, accumulation of substantial amounts of a novel d4T derivative has been found. This d4T metabolite has been characterized as alaninyl d4T-MP. The latter metabolite accumulates at approximate to 13- to 200-fold higher levels than d4T-TP depending the experimental conditions. Alaninyl d4T-MP should be considered as an intra- and/or extracellular depot form of d4T and/or d4T-MP. These findings may explain the superior anti-retroviral activity of So324 over d4T in cell culture.
Balzarini, J., Karlsson, A., Aquaro, S., Perno, C.F., Cahard, D., Naesens, L., et al. (1996). Mechanism of anti-HIV action of masked alaninyl d4T-MP derivatives. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 93(14), 7295-7299.
| Tipologia: | Articolo su rivista |
| Citazione: | Balzarini, J., Karlsson, A., Aquaro, S., Perno, C.F., Cahard, D., Naesens, L., et al. (1996). Mechanism of anti-HIV action of masked alaninyl d4T-MP derivatives. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 93(14), 7295-7299. |
| IF: | Con Impact Factor ISI |
| Lingua: | English |
| Settore Scientifico Disciplinare: | Settore MED/07 - Microbiologia e Microbiologia Clinica |
| Revisione (peer review): | Sì, ma tipo non specificato |
| Tipo: | Articolo |
| Rilevanza: | Rilevanza internazionale |
| Digital Object Identifier (DOI): | http://dx.doi.org/10.1073/pnas.93.14.7295 |
| Stato di pubblicazione: | Pubblicato |
| Data di pubblicazione: | 1996 |
| Titolo: | Mechanism of anti-HIV action of masked alaninyl d4T-MP derivatives |
| Autori: | |
| Autori: | Balzarini, J; Karlsson, A; Aquaro, S; Perno, CF; Cahard, D; Naesens, L; De Clercq, E; Mcguigan, C |
| Appare nelle tipologie: | 01 - Articolo su rivista |
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