Inhibition of the reverse transcriptase from HIV by 3′-azido-3′-Deoxythymidine triphosphate (cas 18423-43-3) and its threo analogue

Add time:09/01/2019    Source:sciencedirect.com

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 μM. 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 μM and 1.7 μM. Reverse transcriptase from nine HIV isolates were tested for inhibition by the erythro isomer and only slight differences in sensitivity were observed.

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