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一种新型水溶性聚噻吩衍生物作为探针用于实时监测活细胞溶酶体中的腺苷 5'-三磷酸酶活性。

A new water-soluble polythiophene derivative as a probe for real-time monitoring adenosine 5'-triphosphatase activity in lysosome of living cells.

机构信息

School of Materials Science & Engineering, Tianjin Key Laboratory for Photoelectric Materials and Devices, Key Laboratory of Display Materials & Photoelectric Devices, Ministry of Education, Tianjin University of Technology, Tianjin 300384, China.

School of Materials Science & Engineering, Tianjin Key Laboratory for Photoelectric Materials and Devices, Key Laboratory of Display Materials & Photoelectric Devices, Ministry of Education, Tianjin University of Technology, Tianjin 300384, China.

出版信息

Talanta. 2018 May 15;182:396-404. doi: 10.1016/j.talanta.2018.02.008. Epub 2018 Feb 7.

Abstract

Detection of the adenosine 5'-triphosphatase (ATPase) activity in lysosome of living cells is of great importance for clinical diagnosis of many related diseases, including cancer. In this work, a new water-soluble polythiophene derivative named ZnPT bearing both quaternary ammonium salt groups and dipicolylamine-Zn (DPA-Zn) complexes in its side chain, was designed and synthesized for this propose. The probe mainly localized to lysosome with good biocompatibility and membrane penetration. The real-time, continuous, direct, and label-free assays were achieved through a fluorescence "turn-on" mode by taking advantages of the reaction specificity of ATPase with ATP and the high binding selectivity of ZnPT toward ATP substrate over its hydrolysis product (ADP). This well designed strategy should provide a facile and effective way for investigating ATPase-relevant biological processes.

摘要

检测活细胞溶酶体中的腺苷 5'-三磷酸酶(ATPase)活性对于许多相关疾病(包括癌症)的临床诊断具有重要意义。在这项工作中,设计并合成了一种新的水溶性聚噻吩衍生物 ZnPT,其侧链上同时含有季铵盐基团和二吡啶甲胺-锌(DPA-Zn)配合物。该探针主要定位于溶酶体,具有良好的生物相容性和膜穿透性。通过利用 ATPase 与 ATP 的反应特异性以及 ZnPT 对 ATP 底物相对于其水解产物(ADP)的高结合选择性,采用荧光“开启”模式实现了实时、连续、直接和无标记的检测。这种精心设计的策略应该为研究与 ATPase 相关的生物学过程提供一种简单有效的方法。

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