Antivirals blocking entry of enteroviruses and therapeutic potential.
Antivirals blocking entry of enteroviruses and therapeutic potential.
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DOI：
10.1186/s12929-021-00708-8
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发表时间：
2021-01-15
影响因子：
11
通讯作者：
Poh CL
中科院分区：
文献类型：
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作者：
Anasir MI;Zarif F;Poh CL
已知来自小核糖核酸病毒科的肠道病毒（EV）属的病毒引起疾病，例如手足口病（HFMD）、呼吸道疾病、脑炎和心肌炎。EV的衣壳是开发可干扰病毒进入的直接作用小分子的有吸引力的靶标。一些衣壳结合剂已经在临床试验中进行了评估，但大多数由于功效不足或不可接受的脱靶效应而失败。此外，大多数衣壳结合剂表现出低的抗性屏障。或者，已经鉴定了宿主靶向抑制剂，例如来源于EV衣壳的肽，其可以识别细胞受体。然而，与小分子化合物的效力（nM范围）相比，这些肽中的大多数显示出低的抗EV效力（µM范围）。尽管如此，抗EV肽的开发是必要的，因为它们可以在治疗EV的药物组合策略中补充小分子。最后，基于结构的抗病毒肽设计方法应被用来挖掘有效的抗EV肽。
Viruses from the genus Enterovirus (EV) of the Picornaviridae family are known to cause diseases such as hand foot and mouth disease (HFMD), respiratory diseases, encephalitis and myocarditis. The capsid of EV is an attractive target for the development of direct-acting small molecules that can interfere with viral entry. Some of the capsid binders have been evaluated in clinical trials but the majority have failed due to insufficient efficacy or unacceptable off-target effects. Furthermore, most of the capsid binders exhibited a low barrier to resistance. Alternatively, host-targeting inhibitors such as peptides derived from the capsid of EV that can recognize cellular receptors have been identified. However, the majority of these peptides displayed low anti-EV potency (µM range) as compared to the potency of small molecule compounds (nM range). Nonetheless, the development of anti-EV peptides is warranted as they may complement the small-molecules in a drug combination strategy to treat EVs. Lastly, structure-based approach to design antiviral peptides should be utilized to unearth potent anti-EV peptides.
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影响因子：
3.5
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通讯作者：
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