Inhibition of the reverse transcriptase from HIV by 3'-azido-3'-deoxythymidine triphosphate and its threo analogue. NLM AIDSLINE Important note: Information in this article was accurate in 1987. The state of the art may have changed since the publication date.

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Inhibition of the reverse transcriptase from HIV by 3'-azido-3'-deoxythymidine triphosphate and its threo analogue.

Antiviral Res. 1987 Mar;7(3):139-49. Unique Identifier : AIDSLINE MED/87269549
Vrang L; Bazin H; Remaud G; Chattopadhyaya J; Oberg B

Abstract: 3'-Azido-3'-deoxythymidine triphosphate (erythro) and its threo isomer were synthesized and investigated for their inhibition of HIV reverse transcriptase from virus isolate U 937/HTLV-III. The erythro isomer was a competitive inhibitor of the reaction directed by (rA)n(dT)12-18 and the Ki value was 0.0022 microM. The threo isomer was at least 100-fold less active. The inhibition was specific for dTMP incorporation, and dGMP incorporation using (rC)n(dG)12-18 as template/primer was not affected. The Km value for dTTP varied between 0.7 microM and 1.7 microM. Reverse transcriptase from nine HIV isolates were tested for inhibition by the erythro isomer and only slight differences in sensitivity were observed.
Keywords: Antiviral Agents/*PHARMACOLOGY Chemistry Comparative Study Human HIV/DRUG EFFECTS/*ENZYMOLOGY Kinetics Reverse Transcriptase/*ANTAGONISTS & INHIB/METABOLISM Support, Non-U.S. Gov't Thymine Nucleotides/*PHARMACOLOGY JOURNAL ARTICLE

KWDantiviralagents/KWDpharmacologychemistrycomparativestudyhumanhiv/drugeffects/KWDenzymologykineticsreversetranscriptase/KWDantagonists&inhib/metabolismsupport,non-uKWDsKWDgov'tthyminenucleotides/KWDpharmacologyjournalarticle
871030
M87A0141

Copyright © 1987 - National Library of Medicine. Reproduced under license with the National Library of Medicine, Bethesda, MD.

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