Recognition and Inhibition of HIV Integrase by Novel Dinucleotides
Recognition and Inhibition of HIV Integrase by Novel Dinucleotides
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新型二核苷酸对 HIV 整合酶的识别和抑制
DOI：
10.1021/ja992528d
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发表时间：
2000
影响因子：
15
通讯作者：
V. Nair
中科院分区：
文献类型：
--
作者：
M. Taktakishvili;N. Neamati;Y. Pommier;S. Pal;V. Nair
HIV整合酶参与了病毒DNA与染色体DNA的整合，这是一种生物过程，涉及HIV DNA剪接和随后的整合步骤。在寻找具有核苷酸间磷酸键的核酸酶稳定性和识别和抑制HIV-1整合酶的关键结构特征的小核苷酸系统的过程中，我们发现了具有特定碱基序列的新型抗核酸酶二核苷酸，它们是这一关键病毒酶的抑制剂。用于合成新型二核苷酸的合成方法包括一种极好的新磷酸化试剂。
HIV integrase is involved in the integration of viral DNA into chromosomal DNA, a biological process that occurs by a sequence involving HIV DNA splicing and subsequent integration steps. In the quest for small nucleotide systems with nuclease stability of the internucleotide phosphate bond and critical structural features for recognition and inhibition of HIV-1 integrase, we have discovered novel, nuclease-resistant dinucleotides with defined base sequences that are inhibitors of this key viral enzyme. Synthetic methodologies utilized for the syntheses of the novel dinucleotides include an excellent new phosphorylating agent.