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Differential phosphorylation of azidothymidine, dideoxycytidine, and dideoxyinosine in resting and activated peripheral blood mononuclear cells.
- W. Gao, T. Shirasaka, D. Johns, S. Broder, H. Mitsuya
- BiologyThe Journal of clinical investigation
- 1 May 1993
It is concluded that AZT, ddC, and ddI exert disproportionate antiviral effects depending on the activation state of the target cells, i.e., ddI and ddC exert antiviral activity more favorably in resting cells than in activated cells, while AZT preferentially protects activated cells against HIV infection.
7-Hydroxymethotrexate as a urinary metabolite in human subjects and rhesus monkeys receiving high dose methotrexate.
- S. Jacobs, R. Stoller, B. Chabner, D. Johns
- Medicine, BiologyThe Journal of clinical investigation
- 1 February 1976
Evidence indicates that in primates, the in vivo conversion of methotrexate to 7-hydroxymethotrexate is a dose-dependent phenomenon, with the enzyme system(s) catalyzing the reaction having a low affinity for the drug.
Human liver aldehyde oxidase: differential inhibition of oxidation of charged and uncharged substrates.
- D. Johns
- Biology, ChemistryThe Journal of clinical investigation
- 1 September 1967
This mode of oxidation appears to be unique to substrates with a positively charged quaternary nitrogen; the hydroxylation of other nonaldehydic heterocyclic substrates for the human enzyme is sensitive to conventional aldehyde oxidase inhibitors.
Cellular pharmacology of cyclopentenyl cytosine in Molt-4 lymphoblasts.
Cytidine, uridine, and nitrobenzylthioinosine all strongly repressed the anabolic phosphorylation of CPEC when added to Molt-4 cells along with the drug, suggesting that the initial interiorization was mediated by facilitated diffusion.
Replication of human immunodeficiency virus in monocytes. Granulocyte/macrophage colony-stimulating factor (GM-CSF) potentiates viral production yet enhances the antiviral effect mediated by…
It is suggested that GM-CSF increases HIV-1 replication in M/M, while at the same time enhancing the anti-HIV activity of AZT and related congeners in these cells.
Long-term toxicity/activity profile of 2',3'-dideoxyinosine in AIDS or AIDS-related complex
The disposition and metabolism of 2',3'-dideoxycytidine, an in vitro inhibitor of human T-lymphotrophic virus type III infectivity, in mice and monkeys.
- J. Kelley, C. Litterst, D. Johns
- Biology, ChemistryDrug metabolism and disposition: the biological…
- 1 September 1987
The pharmacokinetics and metabolism of the anti-human T-lymphotrophic virus type III/lymphadenopathy-associated virus agent 2',3-dideoxycytidine have been examined in BDF1 mice and rhesus monkeys,…
Pharmacokinetics of 2′, 3′‐dideoxyadenosine and 2′, 3′‐dideoxyinosine in patients with severe human immunodeficiency virus infection
This article describes the pharmacokinetics of 2′,3′‐dideoxyadenosine (ddA) and 2′,3′‐dideoxyinosine (ddI) as determined during phase I clinical trials in patients with acquired immunodeficiency…
Arabinofuranosyl-5-azacytosine: antitumor and cytotoxic properties.
Its broad spectrum antitumor activity, its selective toxicity to tumor cells, and its ability to produce cytodifferentiation render ara-AC of interest as a potential antineoplastic agent in humans.