一种新型二核苷酸对HIV整合酶的识别与抑制作用

Recognition and inhibition of HIV integrase by a novel dinucleotide.

作者信息

Taktakishvili M, Neamati N, Pommier Y, Nair V

机构信息

Department of Chemistry, The University of Iowa, Iowa City 52242, USA.

出版信息

Bioorg Med Chem Lett. 2000 Feb 7;10(3):249-51. doi: 10.1016/s0960-894x(99)00677-0.

DOI:10.1016/s0960-894x(99)00677-0

PMID:10698446

Abstract

The viral enzyme, HIV integrase, is involved in the integration of viral DNA into host cell DNA. In the quest for a small nucleotide system with nuclease stability of the internucleotide phosphate bond and critical structural features for recognition and inhibition of HIV-1 integrase, we have discovered a conceptually novel dinucleotide, pIsodApdC, which is a potent inhibitor of this key viral enzyme.

摘要

病毒酶HIV整合酶参与病毒DNA整合到宿主细胞DNA的过程。为了寻找一种具有核苷酸间磷酸二酯键核酸酶稳定性以及识别和抑制HIV-1整合酶关键结构特征的小核苷酸系统，我们发现了一种概念上全新的二核苷酸pIsodApdC，它是这种关键病毒酶的有效抑制剂。