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抗神经氨酸酶药物。

Antivirals Targeting the Neuraminidase.

机构信息

Influenza Division, National Center for Immunization and Respiratory Diseases, Centers for Disease Control and Prevention, Atlanta, Georgia 30329-4027, USA.

出版信息

Cold Spring Harb Perspect Med. 2022 Jan 4;12(1):a038455. doi: 10.1101/cshperspect.a038455.

Abstract

The neuraminidase (NA) of influenza A and B viruses plays a distinct role in viral replication and has a highly conserved catalytic site. Numerous sialic (neuraminic) acid analogs that competitively bind to the NA active site and potently inhibit enzyme activity have been synthesized and tested. Four NA inhibitors are now licensed in various parts of the world (zanamivir, oseltamivir, peramivir, and laninamivir) to treat influenza A and B infections. NA changes, naturally occurring or acquired under selective pressure, have been shown to reduce drug binding, thereby affecting the effectiveness of NA inhibitors. Drug resistance and other drawbacks have prompted the search for the next-generation NA-targeting therapeutics. One of the promising approaches is the identification of monoclonal antibodies (mAbs) targeting the conserved NA epitopes. Anti-NA mAbs demonstrate Fab-based antiviral activity supplemented with Fc-mediated immune effector functions. Antiviral Fc-conjugates offer another cutting-edge strategy that is based on a multimodal mechanism of action. These novel antiviral agents are composed of a small-molecule NA inhibitor and an Fc-region that simultaneously engages the immune system. The significant advancements made in recent years further support the value of NA as an attractive target for the antiviral development.

摘要

流感病毒 A 和 B 的神经氨酸酶(NA)在病毒复制中起着独特的作用,并且具有高度保守的催化位点。已经合成并测试了许多竞争性结合 NA 活性位点并能有效抑制酶活性的唾液酸(神经氨酸)类似物。目前有四种 NA 抑制剂(扎那米韦、奥司他韦、帕拉米韦和拉尼米韦)在世界不同地区获得许可,用于治疗甲型和乙型流感感染。已经表明,NA 的变化(自然发生或在选择性压力下获得)会降低药物结合,从而影响 NA 抑制剂的有效性。耐药性和其他缺点促使人们寻找新一代针对 NA 的治疗方法。一种有前途的方法是鉴定针对保守 NA 表位的单克隆抗体(mAb)。抗 NA mAb 证明基于 Fab 的抗病毒活性,同时补充 Fc 介导的免疫效应功能。抗病毒 Fc 缀合物提供了另一种基于多模式作用机制的前沿策略。这些新型抗病毒药物由小分子 NA 抑制剂和 Fc 区组成,同时与免疫系统结合。近年来取得的重大进展进一步支持了 NA 作为抗病毒药物开发有吸引力的靶标的价值。

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Antivirals Targeting the Neuraminidase.抗神经氨酸酶药物。
Cold Spring Harb Perspect Med. 2022 Jan 4;12(1):a038455. doi: 10.1101/cshperspect.a038455.

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