摘要
每年流感季节导致数千人死亡,数百万人住院,给全球健康和经济造成沉重的负担。此外,重组病毒引起的流感大流行,如H5N1型病毒和甲型H1N1流感,由于在流感爆发的最初阶段缺乏有效的疫苗,引起更大的关注。流感病毒是流感感染的病原体。目前有四种药物在使用以对抗流感感染。金刚烷胺和金刚烷乙胺,M2质子通道阻滞剂抑制病毒病毒脱壳;奥司他韦和扎那米韦是神经氨酸酶(NA)抑制剂,抑制病毒释放。然而,近年来耐药性实例急剧增加,并有、这两类药物流感病毒耐药性的报告。因此,迫切需要开发新一代的抗流感药物。在少量的抗流感药物靶点中,病毒融合蛋白血凝素(HA)是最前言之一。本文综述讨论了HA,基于小分子的HA抑制剂、高活性肽,以及最近电脑设计的HA绑定药物在病毒复制中的作用。文本基于HA的成熟阶段分成四个部分:针对糖基化的HA抑制剂的蛋白水解活性的HA,宿主细胞受体附件的HA,针对膜融合HA-治疗的基于肽、小分子的抑制剂。特别感兴趣的领域的进一步发展针对HA、NA和广泛HA的双重抑制剂。
关键词: 金刚烷,融合抑制剂,血凝素,流感,膜融合。
Current Medicinal Chemistry
Title:Inhibitors Targeting the Influenza Virus Hemagglutinin
Volume: 22 Issue: 11
Author(s): F. Li, C. Ma and J. Wang
Affiliation:
关键词: 金刚烷,融合抑制剂,血凝素,流感,膜融合。
摘要: The annual flu season causes thousands of deaths and millions of hospitalizations, which pose a great burden to global health and economy. Moreover, a flu pandemic arising from reassortment viruses, such as H5N1 and H1N1, raises even greater concern due to the lack of effective vaccines at the initial stage of flu outbreak. The influenza virus is the causative agent of flu infection. Currently there are four drugs in use to combat influenza infection. Amantadine and rimantadine are M2 proton channel blockers that inhibit virus uncoating; oseltamivir and zanamivir are neuraminidase (NA) inhibitors that inhibit virus release. However, recent years have witnessed a drastic increase in instances of drug resistance, and flu strains that are resistant to both classes of drugs have been reported. Thus, there is a pressing need to develop the next generation of anti-influenza drugs. Among a handful of anti-influenza drug targets, the viral fusion protein hemagglutinin (HA) is one of the most advanced. This review discusses the biological roles of HA during viral replication and highlights peptide- and small molecule–based HA inhibitors, including recent computationally designed HA binders. The text is organized into four sections based on the maturation stages of HA: inhibitors targeting the glycosylation of HA, the proteolytic activation of HA, the attachment of HA to host cell receptors, and peptide- and small molecule–based inhibitors targeting HA-mediated membrane fusion. Of particular interest are advances in the areas of developing dual inhibitors targeting both HA and NA and broad-spectrum HA inhibitors targeting both groups of HAs.
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Cite this article as:
F. Li, C. Ma and J. Wang , Inhibitors Targeting the Influenza Virus Hemagglutinin, Current Medicinal Chemistry 2015; 22 (11) . https://dx.doi.org/10.2174/0929867322666150227153919
DOI https://dx.doi.org/10.2174/0929867322666150227153919 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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