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首页> 外文期刊>Microbes and infection >Establishment of a new cell line inducibly expressing HIV-1 protease for performing safe and highly sensitive screening of HIV protease inhibitors
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Establishment of a new cell line inducibly expressing HIV-1 protease for performing safe and highly sensitive screening of HIV protease inhibitors

机译：建立可诱导表达HIV-1蛋白酶的新细胞系，用于安全，高度敏感地筛选HIV蛋白酶抑制剂

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The human immunodeficiency virus type 1 (HIV-1) protease (PR) plays an essential role in processing viral polyproteins into mature proteins. As a result, it is a major target for the development of drugs against AIDS. However, due to the rapid emergence of drug-resistant HIV, the development of novel HIV PR inhibitors is urgently needed. We recently established a new cell line E-PR293 which can be used as a safe, convenient and highly efficient assay system to screen HIV-1 PR inhibitors. In the cells, the HIV-1 PR is expressed in a chimeric protein with the green fluorescence protein (GFP). This assay measures the PR activity as a function of either the fluorescence of GFP or the cytotoxic activity of HIV-1 PR which is expressed in the cell. E-PR293 cells were maintained in the presence of doxycycline, which suppresses the expression of HIV-1 PR. The removal of doxycycline induces the expression of HIV-1 PR, which is used to screen HIV-1 PR inhibitors. In E-PR293 cells, the 50% inhibitory concentration of the cytotoxic effects by nelfinavir and saquinavir were as low as nanomolar levels, almost equal to those found in the HIV-infection assay. (c) 2006 Elsevier SAS. All rights reserved.
机译：人类1型免疫缺陷病毒（HIV-1）蛋白酶（PR）在将病毒多蛋白加工成成熟蛋白方面起着至关重要的作用。因此，它是开发抗艾滋病药物的主要目标。然而，由于抗药性HIV的迅速出现，迫切需要开发新型HIV PR抑制剂。我们最近建立了一种新的细胞系E-PR293，可以用作筛选HIV-1 PR抑制剂的安全，便捷和高效的检测系统。在细胞中，HIV-1 PR与绿色荧光蛋白（GFP）在嵌合蛋白中表达。该测定法根据细胞中表达的GFP的荧光或HIV-1 PR的细胞毒性活性来测量PR活性。 E-PR293细胞在强力霉素的存在下得以维持，这抑制了HIV-1 PR的表达。强力霉素的去除会诱导HIV-1 PR的表达，该蛋白可用于筛选HIV-1 PR抑制剂。在E-PR293细胞中，奈非那韦和沙奎那韦对细胞毒性作用的50％抑制浓度低至纳摩尔水平，几乎等于在HIV感染测定法中发现的浓度。 （c）2006年Elsevier SAS。版权所有。

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