A novel fluorescent probe with Aggregation-Induced emission characteristics for PTP1B activity sensing and inhibitor screening

IF 4.3 2区化学 Q1 SPECTROSCOPY Spectrochimica Acta Part A: Molecular and Biomolecular Spectroscopy Pub Date : 2024-11-03 DOI:10.1016/j.saa.2024.125394

Xiangwei Ma , Zhenzhong Yang , Yuanlin Luo , Zehua Jin , Jingtao Zou , Yi Wang , Xiaoping Zhao

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Abstract

Protein tyrosine phosphatase 1B (PTP1B) is an attractive target for the treatment of metabolic diseases such as type 2 diabetes and obesity. In this study, a novel fluorescent probe with aggregation-induced emission (AIE) characteristics was designed and synthesized. Within the fluorescent probe, a tetraphenylethene core is connected to a peptide sequence that can be specifically recognized and hydrolysed by PTP1B. Due to the dephosphorylation of PTP1B, the fluorescent probe exhibited AIE in a turn-on manner, indicating PTP1B activity. This probe was successfully used to detect PTP1B activity in HepG2 cell lysates. Then, a probe-based method was applied to screen for potential PTP1B inhibitors from a natural product library, and three novel PTP1B inhibitors were discovered. These findings indicated that the proposed approach offered a new avenue for discovering potential PTP1B inhibitors.

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用于 PTP1B 活性检测和抑制剂筛选的具有聚集诱导发射特性的新型荧光探针。

蛋白酪氨酸磷酸酶 1B（PTP1B）是治疗 2 型糖尿病和肥胖症等代谢性疾病的一个极具吸引力的靶点。本研究设计并合成了一种具有聚集诱导发射（AIE）特性的新型荧光探针。在该荧光探针中，一个四苯基乙烯核心与一个肽序列相连，该序列可被 PTP1B 特异性识别并水解。由于 PTP1B 的去磷酸化作用，荧光探针以开启的方式显示出 AIE，表明 PTP1B 具有活性。该探针被成功用于检测 HepG2 细胞裂解物中 PTP1B 的活性。然后，应用基于探针的方法从天然产物库中筛选潜在的 PTP1B 抑制剂，发现了三种新型 PTP1B 抑制剂。这些发现表明，所提出的方法为发现潜在的 PTP1B 抑制剂提供了一条新途径。

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来源期刊

Spectrochimica Acta Part A: Molecular and Biomolecular Spectroscopy 物理-光谱学

CiteScore

8.40

自引率

11.40%

发文量

1364

审稿时长

40 days

期刊介绍： Spectrochimica Acta, Part A: Molecular and Biomolecular Spectroscopy (SAA) is an interdisciplinary journal which spans from basic to applied aspects of optical spectroscopy in chemistry, medicine, biology, and materials science. The journal publishes original scientific papers that feature high-quality spectroscopic data and analysis. From the broad range of optical spectroscopies, the emphasis is on electronic, vibrational or rotational spectra of molecules, rather than on spectroscopy based on magnetic moments. Criteria for publication in SAA are novelty, uniqueness, and outstanding quality. Routine applications of spectroscopic techniques and computational methods are not appropriate. Topics of particular interest of Spectrochimica Acta Part A include, but are not limited to: Spectroscopy and dynamics of bioanalytical, biomedical, environmental, and atmospheric sciences, Novel experimental techniques or instrumentation for molecular spectroscopy, Novel theoretical and computational methods, Novel applications in photochemistry and photobiology, Novel interpretational approaches as well as advances in data analysis based on electronic or vibrational spectroscopy.