吡啶异羟肟酸是影响组蛋白去乙酰化酶6的特异性抗丙型肝炎病毒药物。
Pyridine hydroxamic acids are specific anti-HCV agents affecting HDAC6.
作者信息
Kozlov Maxim V, Kleymenova Alla A, Romanova Lyudmila I, Konduktorov Konstantin A, Kamarova Kamila A, Smirnova Olga A, Prassolov Vladimir S, Kochetkov Sergey N
机构信息
Engelhardt Institute of Molecular Biology, Russian Academy of Sciences, Vavilov Str. 32, 119991 Moscow, Russia.
Engelhardt Institute of Molecular Biology, Russian Academy of Sciences, Vavilov Str. 32, 119991 Moscow, Russia.
出版信息
Bioorg Med Chem Lett. 2015 Jun 1;25(11):2382-5. doi: 10.1016/j.bmcl.2015.04.016. Epub 2015 Apr 16.
Recently we reported benzohydroxamic acids (BHAs) as potent and selective inhibitors of hepatitis C virus (HCV) replicon propagation. In this work 12 pyridine hydroxamic acids (PHAs) were synthesized and tested in full-genome replicon assay. It was found that PHAs possessed very similar anti-HCV properties compared to BHAs. Both classes of hydroxamic acids caused hyperacetylation of α-tubulin pointing to inhibition of histone deacetylase 6 (HDAC6) as part of their antiviral activity. The tested compounds did not inhibit the growth of poliovirus, displaying high selectivity against HCV.
最近我们报道了苯并异羟肟酸（BHAs）是丙型肝炎病毒（HCV）复制子增殖的有效且选择性抑制剂。在这项工作中，合成了12种吡啶异羟肟酸（PHAs），并在全基因组复制子试验中进行了测试。结果发现，与BHAs相比，PHAs具有非常相似的抗HCV特性。两类异羟肟酸均导致α-微管蛋白的高度乙酰化，表明抑制组蛋白脱乙酰基酶6（HDAC6）是其抗病毒活性的一部分。所测试的化合物不抑制脊髓灰质炎病毒的生长，对HCV表现出高选择性。
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