adenosine-kinase and triciribine

adenosine-kinase has been researched along with triciribine* in 3 studies

Other Studies

3 other study(ies) available for adenosine-kinase and triciribine

ArticleYear
Phosphorylation of triciribine is necessary for activity against HIV type 1.
    AIDS research and human retroviruses, 1998, Oct-10, Volume: 14, Issue:15

    Triciribine (TCN) is a tricyclic nucleoside with known antineoplastic and antiviral activity. It is a potent and selective inhibitor of HIV-1 and HIV-2, including strains known to be resistant to AZT or TIBO. TCN is phosphorylated to its 5'-monophosphate (TCN-P) by intracellular adenosine kinase (AK), but is not converted to di- or triphosphates. We now report that 5'-phosphorylation is requisite for the activity of TCN against HIV-1. CEM cells incubated with TCN at concentrations ranging from 0.1 to 330 microM gave intracellular TCN-P concentrations from 27 to 775 microM, respectively. There was no difference in the amount of intracellular TCN-P detected in uninfected compared with HIV-1-infected CEM cells. The antiviral effect of TCN against HIV-1 was strongly antagonized by the AK inhibitor 5-iodotubercidin (ITu). In contrast, TCN and ITu only exhibited additive cytotoxicity. The 5'-deoxy analog of TCN, which cannot be phosphorylated, had no antiviral effect against HIV-1 at a concentration more than 100 times higher than the IC50 of TCN. Similarly, TCN was not active against HIV-1 in an AK-deficient cell line (AA-2) at concentrations shown to inhibit the virus by >95% in CEM cells. Consistent with its AK-deficient phenotype, this cell line phosphorylated TCN to only 3% of the extent observed in CEM cells. We conclude that TCN must be phosphorylated to TCN-P for activity against HIV-1.

    Topics: Acenaphthenes; Adenosine Kinase; Anti-HIV Agents; Biotransformation; Enzyme Inhibitors; HIV-1; Humans; Jurkat Cells; Phosphorylation; Ribonucleosides; Ribonucleotides; Tumor Cells, Cultured

1998
Phosphorylation of "tricyclic nucleoside" by adenosine kinases from L1210 cells and HEp-2 cells.
    Biochemical pharmacology, 1983, Sep-01, Volume: 32, Issue:17

    Topics: Adenosine Kinase; Animals; Carcinoma, Squamous Cell; Cell Line; Humans; Kinetics; Laryngeal Neoplasms; Leukemia L1210; Mice; Phosphorylation; Phosphotransferases; Ribonucleosides

1983
Biochemical properties of the nucleoside of 3-amino-1,5-dihydro-5-methyl-1,4,5,6,8-pentaazaacenaphthylene (NSC-154020).
    Biochemical pharmacology, 1978, Jan-15, Volume: 27, Issue:2

    Topics: Adenosine Deaminase; Adenosine Kinase; Animals; Cells, Cultured; Chromatography, High Pressure Liquid; Leukemia L1210; Neoplasm Proteins; Neoplasms, Experimental; Nucleic Acids; Ribonucleosides; Ribonucleotides

1978