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.
journal_name
Antiviral Resjournal_title
Antiviral researchauthors
Vrang L,Bazin H,Remaud G,Chattopadhyaya J,Oberg Bdoi
10.1016/0166-3542(87)90002-7subject
Has Abstractpub_date
1987-03-01 00:00:00pages
139-49issue
3eissn
0166-3542issn
1872-9096pii
0166-3542(87)90002-7journal_volume
7pub_type
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