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首页> 外文期刊>Proceedings of the National Academy of Sciences of the United States of America >Critical role of reverse transcriptase in the inhibitory mechanism of CNI-H0294 on HIV-1 nuclear translocation
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Critical role of reverse transcriptase in the inhibitory mechanism of CNI-H0294 on HIV-1 nuclear translocation

机译:逆转录酶在CNI-H0294抑制HIV-1核转运中的关键作用

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摘要

HIV-1 replication requires the translocation of viral genome into the nucleus of a target cell. We recently reported the synthesis of an arylene bis(methyl ketone) com- pound (CNI-H0294) that inhibits nuclear targeting of the HIV-1 genome and thus HIV-1 replication in monocyte cul- tures. Here we demonstrate that CNI-H0294 inhibits nuclear targeting of HIV-1-derived preintegration complexes by inac- tivating the nuclear localization sequence of the HIV-1 matrix antigen in a reaction that absolutely requires reverse trans- criptase.
机译:HIV-1复制需要将病毒基因组转位到靶细胞的核中。我们最近报道了亚芳基双(甲基酮)化合物(CNI-H0294)的合成,该化合物可抑制HIV-1基因组的核靶向,从而抑制HIV-1在单核细胞培养物中的复制。在这里,我们证明CNI-H0294通过在绝对需要逆转录酶的反应中激活HIV-1基质抗原的核定位序列,从而抑制了HIV-1衍生的预整合复合物的核靶向。

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