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6'-C-奈拉滨类似物作为S-腺苷同型半胱氨酸水解酶活性抑制剂和人类免疫缺陷病毒复制抑制剂的立体特异性

Stereospecificity of 6'-C-neplanocin A analogues as inhibitors of S-adenosylhomocysteine hydrolase activity and human immunodeficiency virus replication.

作者信息

Daelemans D, Vandamme A M, Shuto S, Matsuda A, De Clercq E

机构信息

Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium.

出版信息

Nucleosides Nucleotides. 1998 Jan-Mar;17(1-3):479-86. doi: 10.1080/07328319808005192.

DOI:10.1080/07328319808005192
PMID:9708357
Abstract

The R- and S-isomers of 6'-C-neplanocin A analogues, which are all known as inhibitors of S-adenosylhomocysteine (AdoHcy) hydrolase, were studied for their inhibitory effects on Human Immunodeficiency Virus type 1 (HIV-1) replication and HIV-1 Tat-mediated transactivation. The R-isomers showed much greater activity against AdoHcy hydrolase than the S-isomers. The same differential activity was observed against the HIV-1 replication and the Tat transactivation.

摘要

6'-C-奈拉滨类似物的R-和S-异构体均为已知的S-腺苷同型半胱氨酸(AdoHcy)水解酶抑制剂,研究了它们对1型人类免疫缺陷病毒(HIV-1)复制及HIV-1反式激活因子(Tat)介导的反式激活作用的抑制效果。R-异构体对AdoHcy水解酶的活性比S-异构体强得多。在HIV-1复制及Tat反式激活方面也观察到了同样的差异活性。

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