Selective Photoaffinity Probe for Monitoring Farnesoid X Receptor Expression in Cultured Cells

Autor: Xiao-Wei Xu, Ya Zhu, Jiang-Zhou Song, Gui-Qing Zou, Zhou Zhao, Qiu-Ling Zheng, Li-Juan Cao, Guang-Ji Wang, Hong Wang, Hai-Ping Hao
Rok vydání: 2022
Předmět:
Zdroj: Analytical Chemistry. 94:10722-10729
ISSN: 1520-6882
0003-2700
DOI: 10.1021/acs.analchem.2c01206
Popis: Farnesoid X receptor (FXR), a member of the nuclear receptor superfamily, is a vital ligand-activated transcriptional factor, which is highly expressed in the liver, intestine, and adrenal gland. However, FXR homeostasis is influenced by many factors, such as diet and circadian rhythm, and the expression of FXR differs in diverse organs. Currently, there is no method to monitor the FXR homeostasis in real time, which restricts us from further investigating the function of FXR under physiological and pathological conditions. In this project, classic FXR agonists were selected to be modified to targeting FXR. The photo-cross-linking diazirine group and alkynyl, a click reaction group, were incorporated to the ligands. Through biorthogonal reaction, fluorophore was linked to the ligands to realize the monitoring of FXR expression in cells.
Databáze: OpenAIRE