Inhibition of sialidase activity as a therapeutic approach.
Inhibition of sialidase activity as a therapeutic approach.
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DOI：
10.2147/dddt.s176220
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发表时间：
2018
期刊：
影响因子：
--
通讯作者：
Orekhov AN
中科院分区：
文献类型：
--
作者：
Glanz VY;Myasoedova VA;Grechko AV;Orekhov AN
对新的抗流感药物的需求持续存在，最近影响到全球数千人的流感大流行突显了这一点。阻止病毒传播的方法之一是抑制病毒唾液酸酶(神经氨酸酶)。这种酶切割新形成的病毒粒子和宿主细胞表面之间的唾液酸链，将病毒粒子从细胞中释放出来，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。与第一批被批准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很好，可以针对甲型和乙型流感病毒。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病理疾病有用，如癌症。在这篇综述中，我们讨论了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，以及目前面临的挑战。
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.