Department of Chemistry, Koç University, 34450 Istanbul, Turkey.
Department of Chemical and Physical Sciences, University of Toronto Mississauga, Mississauga, ON L5L 1C6, Canada.
Chem Commun (Camb). 2022 Sep 29;58(78):10929-10932. doi: 10.1039/d2cc03309g.
Carboxylesterase 2 (CES2) has crucial roles in both xenobiotic metabolism and formation of pathogenic states including cancer. Thus, it is highly critical to monitor intracellular CES2 activity in living cancer cells. Here, we report a CES2 activatable phenoxy 1,2-dioxetane based chemiluminescent agent (CL-CES2). The probe exhibited a selective turn-on response in the presence of CES2 enzyme and enabled detection of CES2 activity in three different cancer cells that possess varying enzyme concentrations with high signal to noise ratios. In contrast no signal was obtained with CES1, an isoform of CES2 enzyme. CL-CES2 marks the first ever example of a CES2-responsive chemiluminescent luminophore and holds a great potential in further understanding the roles of CES2 activity in tumorogenesis.
羧酸酯酶 2(CES2)在异生物质代谢和包括癌症在内的致病状态的形成中起着至关重要的作用。因此,监测活癌细胞内 CES2 的活性非常关键。在这里,我们报告了一种基于羧酸酯酶 2 激活的苯氧基 1,2-二氧杂环乙烷类化学发光探针(CL-CES2)。该探针在 CES2 酶存在下表现出选择性的开启响应,能够在具有不同酶浓度的三种不同癌细胞中检测 CES2 活性,具有高信噪比。相比之下,CES1(CES2 的同工酶)则没有信号产生。CL-CES2 是第一个 CES2 响应性化学发光发光团的例子,在进一步了解 CES2 活性在肿瘤发生中的作用方面具有很大的潜力。