Inhibition of the reverse transcriptase from HIV by 3'-azido-3'-deoxythymidine triphosphate and its threo analogue.
Inhibition of the reverse transcriptase from HIV by 3'-azido-3'-deoxythymidine triphosphate and its threo analogue.
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3-叠氮基-3-脱氧胸苷三磷酸及其苏类似物对 HIV 逆转录酶的抑制。
DOI：
10.1016/0166-3542(87)90002-7
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发表时间：
1987
影响因子：
7.6
通讯作者：
B. Öberg
中科院分区：
文献类型：
--
作者：
L. Vrang;H. Bazin;G. Remaud;J. Chattopadhyaya;B. Öberg
合成了3′-叠氮-3′-脱氧胸腺嘧啶三磷酸（erythro）及其三异构体，并研究了其对HIV病毒分离株U 937/HTLV-III逆转录酶的抑制作用。红血球异构体是（rA）n(dT)12 - 18导向反应的竞争性抑制剂，kivalue为0.0022 μM。三异构体的活性至少降低了100倍。抑制作用对dTMP的掺入具有特异性，使用（rC）n(dG)12 - 18作为模板/引物的dGMP掺入不受影响。dTTP的km值在0.7 ~ 1.7 μM之间。对9株HIV分离株的逆转录酶进行了红细胞异构体抑制试验，结果发现它们的敏感性差异很小。
3′-Azido-3′-deoxythymidine triphosphate (erythro) and itsthreoisomer were synthesized and investigated for their inhibition of HIV reverse transcriptase from virus isolate U 937/HTLV-III. Theerythroisomer was a competitive inhibitor of the reaction directed by (rA)n(dT)12–18and theKivalue was 0.0022 μM. Thethreoisomer was at least 100-fold less active. The inhibition was specific for dTMP incorporation, and dGMP incorporation using (rC)n(dG)12–18as template/primer was not affected. TheKmvalue for dTTP varied between 0.7 μM and 1.7 μM. Reverse transcriptase from nine HIV isolates were tested for inhibition by theerythroisomer and only slight differences in sensitivity were observed.
人类嗜T淋巴细胞病毒III型感染的治疗前景。
影响因子：
39.2
作者：
Hirsch,MS;Kaplan,JC
通讯作者：
Kaplan,JC
治疗获得性免疫缺陷综合征。
影响因子：
9.1
作者：
Gupta,S;Gottlieb,MS
通讯作者：
Gottlieb,MS