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Summary

Acyclovir, an acyclic analogue of deoxyguanosine, is a potent inhibitor of the replication of herpes simplex virus, types 1 and 2, and varicella zoster virus, and has extremely low toxicity for uninfected host cells. This selectivity is due to the specific phosphorylation of acyclovir by a herpes virus-coded thymidine kinase. Acyclovir monophosphate is subsequently converted to a triphosphate which is a potent inhibitor of the DNA polymerases of herpesviruses. These viral polymerases also use acyclovir triphosphate as a substrate, and incorporate the analog into the viral DNA primer-template, causing chain termination and inactivation of the polymerase. Uninfected cells do not phosphorylate acyclovir to any significant extent and have DNA polymerases which are much less sensitive to acyclovir triphosphate than are the herpesvirus DNA polymerases.

Following extensive toxicologic, metabolic and pharmacokinetic studies, acyclovir has undergone randomized, -topical, intravenous and oral. It has shown efficacy against herpes keratitis, initial and recurrent genital herpes, cutaneous and generalized herpes simplex virus infections in immunocompromised hosts, and herpes zoster.

Keywords

Herpes Zoster High Pressure Liquid Chromatography Vero Cell Thymidine Kinase Varicella Zoster Virus 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.

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Copyright information

© Martinus Nijhoff Publishing, Boston 1984

Authors and Affiliations

  • Gertrude B. Elion
    • 1
  1. 1.Wellcome Research LaboratoriesBurroughs Wellcome Co.USA

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