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寨卡病毒NS2B-NS3蛋白酶与酸盐抑制剂复合的晶体结构

Jian Lei¹, Guido Hansen², Christoph Nitsche³

¹Institute of Biochemistry, Center for Structural and Cell Biology in Medicine, University of Lübeck, Ratzeburger Allee 160, 23562 Lübeck, Germany. German Center for Infection Research (DZIF), Hamburg-Lübeck-Borstel-Riems Site, University of Lübeck, Germany.

Science (New York, N.Y.)

|July 9, 2016

概括

寨卡病毒蛋白酶是神经疾病的药物标,用一种抑制剂结晶. 这种结构揭示了酶活性和细胞膜潜在组合的关键相互作用.

科学领域:

病毒学
结构生物学
药物发现

背景情况:

寨卡病毒 (ZIKV) 爆发与严重的神经疾病有关.
ZIKV的NS2B/NS3蛋白酶对于病毒多蛋白处理至关重要,并且是一个有前途的药物标.

研究的目的:

确定ZIKV蛋白酶的结晶结构与新型胺酸抑制剂的复合.
阐明控制蛋白酶活性的分子相互作用,并确定抗病毒药物开发的潜在策略.

主要方法:

采用X射线结晶学来获得ZIKV蛋白酶与酸抑制剂结合的2. 7安格斯特罗姆分辨率结构.
生物化学分析的重点是抑制剂的P2部分与NS2B的非保存Asp{8}之间的相互作用.

主要成果:

晶体结构显示酸抑制剂与糖醇之间存在循环结.
在抑制剂的P2 4-氨基甲基氨酸和ZIKV NS2B Asp之间发现了关键的盐桥相互作用.
该研究观察到蛋白酶:抑制剂复合物的异常二元组合,可能模拟体内组合.

结论:

鉴定出Asp{83) 与P2残留物之间的盐桥相互作用对蛋白酶的高催化效率至关重要.
在病毒复制过程中,二元复合结构提供了对内细胞网膜中的蛋白酶组合的见解.
这些结构信息为设计强效和特异性的ZIKV蛋白酶抑制剂提供了基础.

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