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抑制唾液酸酶活性作为一种治疗方法。

Inhibition of sialidase activity as a therapeutic approach.

作者信息

Glanz Victor Yu, Myasoedova Veronika A, Grechko Andrey V, Orekhov Alexander N

机构信息

Department of Genetics, Cytology and Bioengineering, Faculty of Biology and Medicine, Voronezh State University, Voronezh, Russia.

Laboratory of Angiopathology, Institute of General Pathology and Pathophysiology, Moscow, Russia,

出版信息

Drug Des Devel Ther. 2018 Oct 10;12:3431-3437. doi: 10.2147/DDDT.S176220. eCollection 2018.

Abstract

The demand for novel anti-influenza drugs persists, which is highlighted by the recent pandemics of influenza affecting thousands of people across the globe. One of the approaches to block the virus spreading is inhibiting viral sialidase (neuraminidase). This enzyme cleaves the sialic acid link between the newly formed virions and the host cell surface liberating the virions from the cell and maintaining the cycle of infection. Viral neuraminidases appear therefore as attractive therapeutic targets for preventing further spread of influenza infection. Compared to ion channel blockers that were the first approved anti-influenza drugs, neuraminidase inhibitors are well tolerated and target both influenza A and B viruses. Moreover, neuraminidase/sialidase inhibitors may be useful for managing some other human pathologies, such as cancer. In this review, we discuss the available knowledge on neuraminidase or sialidase inhibitors, their design, clinical application, and the current challenges.

摘要

对新型抗流感药物的需求持续存在,近期影响全球数千人的流感大流行凸显了这一点。阻断病毒传播的方法之一是抑制病毒唾液酸酶(神经氨酸酶)。这种酶切断新形成的病毒粒子与宿主细胞表面之间的唾液酸连接,使病毒粒子从细胞中释放出来并维持感染循环。因此,病毒神经氨酸酶似乎是预防流感感染进一步传播的有吸引力的治疗靶点。与首批获批的抗流感药物离子通道阻滞剂相比,神经氨酸酶抑制剂耐受性良好,对甲型和乙型流感病毒均有作用。此外,神经氨酸酶/唾液酸酶抑制剂可能对治疗其他一些人类疾病(如癌症)有用。在这篇综述中,我们讨论了关于神经氨酸酶或唾液酸酶抑制剂的现有知识、它们的设计、临床应用以及当前面临的挑战。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5e4e/6186905/5704217be4f1/dddt-12-3431Fig1.jpg

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