HPV episome levels are potently decreased by pyrrole-imidazole polyamides
HPV episome levels are potently decreased by pyrrole-imidazole polyamides
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DOI：
10.1016/j.antiviral.2011.05.014
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发表时间：
2011-08-01
影响因子：
7.6
通讯作者：
Fisher, Chris
中科院分区：
文献类型：
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作者：
Edwards, Terri G.;Koeller, Kevin J.;Fisher, Chris
人乳头瘤病毒（HPV）会导致子宫颈癌和其他增生性疾病。目前还没有被批准的能直接降低病毒DNA载量且毒性低的HPV抗病毒药物。我们报道了两种发夹型n -甲基吡咯-咪唑聚酰胺的有效抗hpv活性，聚酰胺1 （PA1）和聚酰胺25 （PA25）。当对维持HPV发作的细胞进行测试时，两种聚酰胺都对三种不同的基因型具有有效的抗HPV活性。分别对HPV16 （W12细胞）、HPV18 （Ker4-18细胞）和HPV31 （HPV31维持细胞）进行了抑菌实验。从一个旨在识别富含at的DNA序列的聚酰胺文库中，例如位于HPV16复制起源的El或E2结合位点或附近的DNA序列（on），鉴定出四种具有明显IC(50)s的聚酰胺
Human papillomavirus (HPV) causes cervical cancer and other hyperproliferative diseases. There currently are no approved antiviral drugs for HPV that directly decrease viral DNA load and that have low toxicity. We report the potent anti-HPV activity of two N-methylpyrrole-imidazole polyamides of the hairpin type, polyamide 1 (PA1) and polyamide 25 (PA25). Both polyamides have potent anti-HPV activity against three different genotypes when tested on cells maintaining HPV episomes. The compounds were tested against HPV16 (in W12 cells), HPV18 (in Ker4-18 cells), and HPV31 (in HPV31 maintaining cells). From a library of polyamides designed to recognize AT-rich DNA sequences such as those in or near El or E2 binding sites of the HPV16 origin of replication (on), four polyamides were identified that possessed apparent IC(50)s