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顺式-5-氟-1-[2-(羟甲基)-1,3-氧硫杂环戊烷-5-基]胞嘧啶的(-)和(+)对映体的5'-三磷酸酯同样抑制人类免疫缺陷病毒1型逆转录酶。

The 5'-triphosphates of the (-) and (+) enantiomers of cis-5-fluoro-1-[2-(hydroxymethyl)-1,3-oxathiolane-5-yl]cytosine equally inhibit human immunodeficiency virus type 1 reverse transcriptase.

作者信息

Wilson J E, Martin J L, Borroto-Esoda K, Hopkins S, Painter G, Liotta D C, Furman P A

机构信息

Division of Virology, Burroughs Wellcome Co., Research Triangle Park, North Carolina 27709.

出版信息

Antimicrob Agents Chemother. 1993 Aug;37(8):1720-2. doi: 10.1128/AAC.37.8.1720.

DOI:10.1128/AAC.37.8.1720
PMID:7692813
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC188052/
Abstract

The (-) enantiomer of cis-5-fluoro-1-[2-(hydroxymethyl)-1,3-oxathiolane-5-yl]cytosine is a potent inhibitor of human immunodeficiency virus type 1 in vitro. The 5'-triphosphates of the (-) and (+) enantiomers equally inhibited the production of full-length minus-strand DNA in an endogenous reverse transcriptase reaction, each competitively inhibited DNA synthesis, and each was used as a chain-terminating substrate.

摘要

顺式-5-氟-1-[2-(羟甲基)-1,3-氧硫杂环戊烷-5-基]胞嘧啶的(-)对映体在体外是1型人类免疫缺陷病毒的有效抑制剂。(-)和(+)对映体的5'-三磷酸酯在内源性逆转录酶反应中同等程度地抑制全长负链DNA的产生，二者均竞争性抑制DNA合成，且二者均用作链终止底物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/52ab/188052/e84c9a192b8c/aac00030-0178-a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/52ab/188052/3d963888383f/aac00030-0177-a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/52ab/188052/e84c9a192b8c/aac00030-0178-a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/52ab/188052/3d963888383f/aac00030-0177-a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/52ab/188052/e84c9a192b8c/aac00030-0178-a.jpg

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本文引用的文献

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2
Comparison of the effect of Carbovir, AZT, and dideoxynucleoside triphosphates on the activity of human immunodeficiency virus reverse transcriptase and selected human polymerases.卡波韦、齐多夫定和三磷酸双脱氧核苷对人类免疫缺陷病毒逆转录酶及所选人类聚合酶活性影响的比较。
Biochem Biophys Res Commun. 1989 Jun 15;161(2):393-8. doi: 10.1016/0006-291x(89)92611-9.
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3'-Azido-3'-deoxythymidine triphosphate as an inhibitor and substrate of purified human immunodeficiency virus reverse transcriptase.
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Stereochemical control of DNA biosynthesis.DNA生物合成的立体化学控制。
Nucleic Acids Res. 2000 Mar 1;28(5):1170-5. doi: 10.1093/nar/28.5.1170.
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Mechanisms of nucleoside analog antiviral activity and resistance during human immunodeficiency virus reverse transcription.人类免疫缺陷病毒逆转录过程中核苷类似物抗病毒活性及耐药性的机制
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