Comparison of the DNA incorporation in human MOLT-4 cells of two 2'-beta-fluoronucleosides, 2'-beta-fluoro-2',3'-dideoxyadenosine and fialuridine.

Abstract

Incorporation of 2'-beta-fluoro-2',3'-dideoxyadenosine (F-ddA), a recently developed anti-HIV agent, into the cellular DNA of human MOLT-4 cells has been compared with the DNA incorporation seen with fialuridine (FIAU; 1-[2'-deoxy-2'-fluoro-beta-D-arabinofuranosyl]-5-iodouracil), a potent anti-hepatitis B (anti-HBV) nucleoside analogue recently found to cause severe hepatic toxicity in human subjects. At equimolar concentrations (10 microM), incorporation of F-ddA was less than 1% of that for FIAU, a difference attributable to the lack of a 3'-hydroxyl group in the former compound and a consequent inability of F-ddA, unlike FIAU, to form DNA internucleotide linkages.

• Authors: G S Ahluwalia, J S Driscoll, H Ford Jr, D G Johns
• Journal: Journal of pharmaceutical sciences (J Pharm Sci) Vol. 85 Issue 4 Pg. 454-5 (Apr 1996) ISSN: 0022-3549 [Print] United States
• PMID: 8901088 (Publication Type: Comparative Study, Journal Article)

Chemical References

• Antiviral Agents
• 2-fluoro-2',3'-dideoxyadenosine
• Arabinofuranosyluracil
• Dideoxyadenosine
• fialuridine
• DNA

Topics

• Antiviral Agents (metabolism)
• Arabinofuranosyluracil (analogs & derivatives, metabolism)
• Cell Line
• DNA (metabolism)
• Dideoxyadenosine (analogs & derivatives, metabolism)
• Humans