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肌醇需求酶1(IRE1)激酶抑制剂高通量筛选模型的建立

, PP. 103-113

Keywords: 肌醇需求酶-1,激酶抑制剂,昆虫表达,均相时间分辨荧光,高通量筛选

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Abstract:

运用昆虫蛋白表达体系成功表达纯化得到高纯度的内质网单次跨膜蛋白肌醇需求酶1(IRE1)细胞质区域段,并建立基于均相时间分辨荧光(HTRF,HomogeneousTime-resolvedFluorescence)原理的激酶活性检测体系,优化激酶抑制剂的高通量筛选模型.该模型Z′因子等于0.58,CV值等于7.5%,符合高通量筛选要求,表明高通量筛选模型建立成功.本工作为进一步发现IRE1激酶抑制剂及其后续研究工作奠定坚实基础.

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