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

Bioconjug Chem

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.

Published: May 2018

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.

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http://dx.doi.org/10.1021/acs.bioconjchem.8b00137DOI Listing

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