CAJ | 학술논문

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了技术保证。
건립이가살기 B 조3형병독3C 단백매（CVB3-3C）위파점적약물사선모형，병사선신형억제제。사용원핵표체모형실현 CVB3-3C 단백매체외중조표체。경 Ni-NTA 친화층석、음리자교환층석순화획득고순도 CVB3-3C 단백。응용형광공진능량전이법검측단백매활성，건립약물사선모형。대768충화합물진행사선，획득료2충대 CVB3-3C 단백매유교강억제작용적화합물（MDCE-A008화 MDCE-A043），IC50치분별위（60．61±6．26）μmol／L、（105．7±14．88）μmol／L。건립적 CVB3-3C 단백매약물사선모형위획득유효억제제제공료기술보증。
The establishment of drug screening model targeting coxsackievirus B3 3C protease (CVB3-3C)and screening new in-hibitors 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 ex-amine the target protease activity.Finally,a drug screening model was established.and 768 compounds were screened.Two com-pounds (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 inhib-itors.