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科学通报  2013 

以P2X7受体为靶标的高通量筛选方法

, PP. 1739-1747

Keywords: 人源P2X7受体,高通量药物筛选,荧光成像分析系统,膜电位检测,溴化乙啶内吞检测,钙内流检测

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Abstract:

P2X7受体是嘌呤-配体门控离子通道受体家族P2X的一员.一些研究表明,P2X7受体主要在上皮细胞和免疫系统细胞中表达,参与免疫调节的过程,如炎性细胞因子释放、膜融合及细胞凋亡.P2X7受体是神经退行性疾病、类风湿关节炎、神经性疼痛药物筛选的重要靶标,已成为大型制药公司新的研究热点.构建表达人源P2X7受体(hP2X7R)的人胚肾细胞系HEK-293,利用荧光成像分析系统(FlexStation),针对P2X7受体特性,比较和验证了3种用于检测P2X7受体高表达细胞系药理学特征的高通量荧光检测方法,分别是膜电位检测法、溴化乙啶内吞检测法和钙内流检测法.对3种不同方法的比较研究表明,钙内流检测法简便、快捷,更适用于P2X7受体调节剂的低成本、高通量药物筛选.

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