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- W147720747 abstract "1. Generally, phosphonates need to be converted into a prodrug to improve their bioavailability. Secondly, they have to be recognised by the host cell kinases for subsequent phosphorylation into triphosphates. Only after both of these two steps will they be effective as HIV-1 reverse transcriptase inhibitors. Therefore, the development of assays that can separate bioavailability from phosphorylation and enzyme inhibition are critical for high throughput screening of potential nucleotide reverse Transcriptase Inhibitors (NtRTIs). The objective of this study was to evaluate the cell-free phosphorylation of tenofovir and UMP, as test cases, using mammalian cell extracted nucleotide kinases. Further studies would then concentrate on cell-free phosphorylation of new compounds prepared as possible reverse transcriptase inhibitors to assess their capacity for phosphorylation as well as linking this directly to testing HIV-1 reverse transcriptase enzyme inhibition potential in a single assay." @default.
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- W147720747 date "2007-06-01" @default.
- W147720747 modified "2023-09-27" @default.
- W147720747 title "Cell free phosphorylation method to assess the utility of new nucleotides as nucleoside reserve transcriptase inhibitors" @default.
- W147720747 hasPublicationYear "2007" @default.
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