Inhibition of hepatitis B virus DNA polymerase by 3'-azido-3'-deoxythymidine triphosphate but not by its threo analog.
An inhibitory effect of 3'-azido-3'-deoxythymidine triphosphate on hepatitis B virus DNA polymerase was found. No effect was seen by its threo analog. The effect was detected at and above a concentration of 0.05 microM. The inhibition of DNA polymerase activity was the same in ten different strains of HBV. The mechanism was shown to be competitive, with an inhibition constant (Ki) of approximately 0.04 microM, and the Km value for dTTP was 0.1 microM.
D000998:Antiviral Agents / Q000494:pharmacology*; D002353:Carrier State / Q000201:enzymology; D054306:Dideoxynucleotides; D006509:Hepatitis B / Q000201:enzymology; D006515:Hepatitis B virus / Q000201:enzymology*; D006801:Humans; D019384:Nucleic Acid Synthesis Inhibitors; D013936:Thymidine / Q000031:analogs & derivatives* / Q000494:pharmacology; D013942:Thymine Nucleotides / Q000494:pharmacology*; D015215:Zidovudine / Q000031:analogs & derivatives
D000998:Antiviral Agents; D054306:Dideoxynucleotides; D019384:Nucleic Acid Synthesis Inhibitors; D013942:Thymine Nucleotides; D015215:Zidovudine; C052873:zidovudine triphosphate; D013936:Thymidine