Ministry of Education Key Laboratory for the Synthesis and Application of Organic Functional Molecules & Hubei Collaborative Innovation Center for Advanced Organic chemical Materials, Hubei University, Wuhan 430062, P. R. China.
National Engineering Research Center for Nanomedicine, College of Life Science and Technology, Huazhong University of Science and Technology, Wuhan 430074, P. R. China.
Analyst. 2019 Jan 21;144(2):463-467. doi: 10.1039/c8an01486h. Epub 2018 Nov 8.
Leucine aminopeptidase (LAP), one of the important cancer-related biomarkers, is significantly over-expressed in many malignant tumor cells. Developing an effective fluorescent probe for high-specificity and in situ trapping of endogenous LAP in living samples is still challenging. In this project, we report a water-soluble near-infrared (NIR) fluorescent probe (CHMC-M-Leu) for specific monitoring of LAP in vitro and in vivo. The novel fluorescent probe (CHMC-M-Leu) contains a NIR-emitting fluorophore (CHMC-M) as the reporter and l-leucine as the enzyme-active trigger moiety which are linked together by a p-aminobenzyl alcohol (PABA) section. Upon exposure to LAP, the fluorescence at 625 nm gets impressively enhanced, which belongs to the near-infrared region and is beneficial for imaging in vivo. Furthermore, the novel fluorescent probe exhibits fast response and highly chemoselective detection of LAP in various bio-related species. In addition, CHMC-M-Leu shows favourable cellular uptake and was successfully used to monitor endogenous LAP in living cells.
亮氨酸氨肽酶（LAP）是一种重要的癌症相关生物标志物，在许多恶性肿瘤细胞中过度表达。开发一种有效的荧光探针，用于在活样本中特异性地捕获内源性 LAP，仍然具有挑战性。在本项目中，我们报告了一种水溶性近红外（NIR）荧光探针（CHMC-M-Leu），用于体外和体内特异性监测 LAP。新型荧光探针（CHMC-M-Leu）包含一个近红外发射荧光团（CHMC-M）作为报告基团，l-亮氨酸作为酶活性触发部分，通过对氨基苯甲醇（PABA）部分连接在一起。暴露于 LAP 后，625nm 处的荧光显著增强，属于近红外区域，有利于体内成像。此外，该新型荧光探针在各种生物相关物种中对 LAP 表现出快速响应和高度选择性的检测。此外，CHMC-M-Leu 表现出良好的细胞摄取能力，并成功用于监测活细胞内源性 LAP。
