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作 者:孙守飞 张静 薛晓霞 赵杰 SUN Shoufei;ZHANG Jing;XUE Xiaoxia;ZHAO Jie(Shandong Cisen Fodu Pharmaceutical Co.,Ltd.,Jining 272500,China;Cisen Pharmaceutical Co.,Ltd.,Jining 272073,China;Shandong Center for Food and Drug Evaluation&Inspection,Jinan 250014,China)
机构地区:[1]山东辰欣佛都药业股份有限公司,山东济宁272500 [2]辰欣药业股份有限公司,山东济宁272073 [3]山东省食品药品审评查验中心,山东济南250014
出 处:《药学研究》2024年第1期89-92,98,共5页Journal of Pharmaceutical Research
基 金:济宁市重点研发计划(产业创新重大技术“全球揭榜”)项目(No.2022JBZP005)。
摘 要:流行性感冒(简称流感)是流感病毒引起的对人类健康危害较重的呼吸道传染病。目前抗流感药物的应用主要面临病毒耐药性和对高致病性流感病毒的效价低的问题,如M2离子通道抑制剂和神经氨酸酶抑制剂存在药效低、时间窗口窄和耐药性等缺点。近来的抗流感药物研发的靶点聚焦于病毒RNA聚合酶。流感病毒RNA聚合酶是病毒在宿主细胞内完成复制和转录过程的关键酶,其中PA亚基通过内切酶活性为流感病毒的转录过程提供引物,成为潜在抗流感药物靶点。本文总结了以PA亚基内切酶为靶点的抗流感药物研究进展,旨在为开发安全有效的新型抗病毒RNA聚合酶抑制剂提供参考。Influenza is a respiratory infectious disease caused by influenza virus,which is more harmful to human health.At present,the main problems faced by anti influenza drugs are virus resistance and low potency for highly pathogenic influenza virus.Due to the shortcomings of influenza drugs such as M2 ion channel inhibitor and neuraminidase inhibitor,such as low efficacy,narrow time window and drug resistance,recent anti influenza drug development focuses on viral RNA polymerase.Influenza virus RNA polymerase is a key enzyme for virus replication and transcription in host cells.The PA subunit provides primers for the transcription process of influenza virus through endonuclease activity and becomes a potential anti influenza drug target.Therefore,this article summarized the research progress of anti influenza drugs targeting the activity of PA subunit endonuclease,aiming to provide a reference for the development of new safe and effective antiviral RNA polymerase inhibitors.
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