多肽类中东呼吸系统综合征冠状病毒进入抑制剂的研究进展

Development of peptidic MERS-CoV entry inhibitors

2012年,中东地区出现一种与严重急性呼吸综合征(SARS)病毒类似的新型人冠状病毒,即中东呼吸系统综合征(MERS)冠状病毒(MERS-Co V)。MERS患者的高死亡率引起了全球关注。MERS-Co V在侵染靶细胞时,其S蛋白的S1亚单位负责与受体DPP4结合,而S2亚单位通过HR1和HR2区域相互作用形成稳定的六螺旋结构从而介导病毒与靶细胞间的膜融合及病毒基因进入靶细胞内进行复制。因此,阻断病毒S蛋白S2亚单位的六螺旋的形成,可有效抑制MERS-Co V感染靶细胞。本文重点介绍了靶向于MERS-Co V S2亚单位的多肽类病毒进入抑制剂的研究进展。

In 2012, a new SARS-like coronavirus emerged in the Middle East, namely the Middle East respiratory syndrome coronavirus （MERS-CoV）. It has caused outbreaks with high mortality. During infection of target cell, MERS-CoV S protein S 1 subunit binds to the cellular receptor （DPP4）, and its S2 subunit HR1 and HR2 regions intact with each other to form a stable six-helix bundle to mediate the fusion between virus and target cell membranes. Hence, blocking the process of six-helix bundle formation can effectively inhibit MERS-CoV entry into the target cells. This review focuses on the recent advance in the development of peptidic entry inhibitors targeting the MERS-CoV S2 subunit