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开发一种用于活细胞中布鲁顿酪氨酸激酶定量的选择性标记探针。

Development of a Selective Labeling Probe for Bruton's Tyrosine Kinase Quantification in Live Cells.

机构信息

State Key Laboratory of Chemical Oncogenomics, Key Laboratory of Chemical Genomics, School of Chemical Biology and Biotechnology, Shenzhen Graduate School , Peking University , Xili University Town, PKU Campus, Shenzhen 518055 , China.

出版信息

Bioconjug Chem. 2018 May 16;29(5):1640-1645. doi: 10.1021/acs.bioconjchem.8b00137. Epub 2018 Apr 13.

Abstract

As a key regulator of the B-cell receptor signaling pathway, Bruton's tyrosine kinase (Btk) has emerged as an important therapeutic target for various malignancies and autoimmune disorders. However, data on the expression profiles of Btk are lacking. Here, we report the discovery of a new, selective Btk probe and of a sandwich-type ELISA quantification method to detect endogenous Btk in live cells. We achieved selective labeling of Btk in vivo and quantified Btk levels in seven types of human lymphoma cell lines. This quantification method provides a powerful tool to study Btk in live cells that may also be useful in clinical settings.

摘要

作为 B 细胞受体信号通路的关键调节因子,布鲁顿酪氨酸激酶(Btk)已成为各种恶性肿瘤和自身免疫性疾病的重要治疗靶点。然而,目前关于 Btk 表达谱的数据还很缺乏。在这里,我们报告了一种新的、选择性的 Btk 探针的发现,以及一种用于检测活细胞内源性 Btk 的夹心型 ELISA 定量方法。我们实现了 Btk 在体内的选择性标记,并定量了七种类型的人类淋巴瘤细胞系中的 Btk 水平。这种定量方法为研究活细胞中的 Btk 提供了一种强大的工具,在临床环境中也可能很有用。

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