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以柯萨奇B3病毒3C蛋白酶为靶点的体外药物筛选模型的建立及应用

Establishment and application of in vitro drug screening model targeting coxsackievirus B3 3C protease

中文摘要英文摘要

建立以柯萨奇B组3型病毒3C蛋白酶(CVB3-3C)为靶点的药物筛选模型,并筛选新型抑制剂。使用原核表达模型实现CVB3-3C蛋白酶体外重组表达。经Ni-NTA亲和层析、阴离子交换层析纯化获得高纯度CVB3-3C蛋白。应用荧光共振能量转移法检测蛋白酶活性,建立药物筛选模型。对768种化合物进行筛选,获得了2种对CVB3-3C蛋白酶有较强抑制作用的化合物(MDCE-A008和MDCE-A043),IC50值分别为(60.61±6.26) μmol/L、(105.7±14.88) μmol/L。建立的CVB3-3C蛋白酶药物筛选模型,为获得有效抑制剂提供技术保证。

he establishment of drug screening model targeting coxsackievirus B3 3C protease (CVB3-3C) and screening new inhibitors was investigated. Prokaryotic expression system expressed CVB3-3C protease in vitro. CVB3-3C protease was purified by affinity chromatography and ion exchange chromatography. Fluorescence resonance energy transfer (FRET) was used to examine the target protease activity. Finally, a drug screening model was established.and 768 compounds were screened. Two compounds (MDCE-A008 and MDCE-A043) with high inhibition ratio were selected, IC50 are (60.61±6.26)μmol/L and (105.7±14.88)μmol/L, respectively. The established model targeting CVB3-3C provides technical guarantee for screening effective inhibitors.

汪颖、王文明、李国邦、唐延婷、贺秋红、郭宇

药学生物科学研究方法、生物科学研究技术基础医学

柯萨奇B3病毒3C蛋白酶药物筛选抑制剂

coxsackievirus B33C proteasedrug screeninginhibitors

汪颖,王文明,李国邦,唐延婷,贺秋红,郭宇.以柯萨奇B3病毒3C蛋白酶为靶点的体外药物筛选模型的建立及应用[EB/OL].(2015-01-20)[2025-08-23].http://www.paper.edu.cn/releasepaper/content/201501-324.点此复制

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