The DOI matches its Crossref record; 22 of the 22 references it cites were found in a registry or an index.
Differential Patterns of Intracellular Metabolism of 2′,3′-Didehydro-2′,3′-dideoxythymidine and 3′-Azido-2′,3′-dideoxythymidine, Two Potent Anti-human Immunodeficiency Virus Compounds
Open accessAbstract
3'-Azido-2',3'-dideoxythymidine (AZT) and 2',3'-didehydro-2',3'-dideoxythymidine (D4T) are potent and selective inhibitors of human immunodeficiency virus replication in MT-4 and ATH8 cells. They are also inhibitory to the replication of murine retroviruses, i.e. Moloney murine sarcoma virus-induced transformation of C3H cells. In MT-4 cells AZT is readily phosphorylated to its 5'-monophosphate, while the 5'-di- and 5'-triphosphates are generated to a 200-600-fold lower extent than the 5'-monophosphate. D4T is phosphorylated in MT-4 cells to its 5'-monophosphate at a 300-600-fold lower extent than AZT. The phosphorylation of AZT in the thymidine kinase-deficient cell line (Raji/TK-) is severely depressed, while D4T phosphorylation is only slightly diminished in Raji/TK- as compared to Raji/0 cells. D4T has a 10-fold lower affinity for phosphorylation by crude MT-4 cell extracts than AZT (Km, 142 and 14 microM, respectively), and the Vmax for phosphorylation of D4T is only 5% that of AZT. D4T is phosphorylated by MT-4 cell extracts about 180-fold less efficiently than AZT (Vmax/Km, 0.06 for D4T, as compared to 11 for AZT), and this is consistent with the differences found in the amounts of phosphorylated products of D4T and AZT formed in intact MT-4 cells. The 5'-triphosphates of AZT and D4T are equipotent in their inhibitory effects on the reverse transcriptases from human immunodeficiency virus and Moloney murine leukemia virus.
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Arts, E. J., & Hazuda, D. J. (2012) · Cold Spring Harbor Perspectives in Medicine · doi:10.1101/cshperspect.a007161 · Cited by 851
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Metadata
- Authors
- Balzarini, J., Herdewijn, P., & De Clercq, E.
- Venue
- Journal of Biological Chemistry
- Publisher
- Elsevier BV
- Published
- 1989-04
- Volume
- 264
- Issue
- 11
- Pages
- 6127-6133
- ISSN
- 0021-9258 (ISSN-L)
- OpenAlex
- W1548955637
- Cited by
- 338
- References
- 22
- FWCI
- 13.18
- Type
- journal article
- Language
- en
- Open access
- hybrid
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- CoChat. (2026). Citation check: Differential Patterns of Intracellular Metabolism of 2′,3′-Didehydro-2′,3′-dideoxythymidine and 3′-Azido-2′,3′-dideoxythymidine, Two Potent Anti-human Immunodeficiency Virus Compounds. https://app.cochat.ai/papers/10.1016/s0021-9258(18)83322-1
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- Balzarini, J., Herdewijn, P., & De Clercq, E. (1989). Differential Patterns of Intracellular Metabolism of 2′,3′-Didehydro-2′,3′-dideoxythymidine and 3′-Azido-2′,3′-dideoxythymidine, Two Potent Anti-human Immunodeficiency Virus Compounds. Journal of Biological Chemistry. https://doi.org/10.1016/s0021-9258(18)83322-1
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