基于CE的固定化EGFR微反应器的制备

Gang-yi Shen, Wanting Yu, Lingpeng Pei, Xun Cui
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引用次数: 0

摘要

表皮生长因子受体(epidermal growth factor receptor, EGFR)作为受体酪氨酸激酶家族的成员,与肿瘤的生长密切相关。因此,它已成为抗肿瘤药物筛选的重要和潜在靶标分子。本研究建立了一种新的固定化EGFR微反应器,用于快速筛选EGFR抑制剂。用三种化学修饰方法将酶固定在毛细管内壁。结合毛细管电泳技术,可寻址固定化EGFR微反应器可方便地从复杂混合物中分离和捕获EGFR抑制剂,并具有高选择性。用吉非替尼对微反应器的性能进行了研究,结果表明微反应器具有良好的识别能力。进一步考察了三种方法对固定化酶稳定性和活性的影响。结果表明,逐层组装是最优的方法,具有良好的稳定性和活性。该筛选平台作为一种简便、通用的方法,有望广泛应用于新型蛋白抑制剂的发现。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Preparation of Immobilized EGFR Micro-reactor Based on CE
As the member of receptor tyrosine kinase family, epidermal growth factor receptor (EGFR) is closely related to the growth of tumor. Thus, it has become a significant and potential target molecule for the screening of anti-tumor drug. In this study, a new immobilized EGFR micro-reactor was established for fast screening EGFR inhibitors. Enzyme was immobilized into the inner wall of capillary with three chemical modification methods. Combined with capillary electrophoresis technique, the addressable immobilized EGFR micro-reactor could easily separate and capture EGFR inhibitors from the complex mixtures with high selectivity. The performance of the micro-reactor was studied with Gefitinib, which showed good recognization ability. The influence on stability and activity of the immobilized enzyme prepared by three methods was further investigated. It was demonstrated that the layer-by-layer assembling method was the optimized one, which showed both good stability and activity. It is expected that this screening platform would be widely used in the discovery of the new protein inhibitors as a convenient and universal method.
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