2. Academic Validation
  3. Selective Photoaffinity Probe for Monitoring Farnesoid X Receptor Expression in Cultured Cells

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

  • Anal Chem. 2022 Aug 2;94(30):10722-10729. doi: 10.1021/acs.analchem.2c01206.
Xiao-Wei Xu 1 2,  Ya Zhu 1 2,  Jiang-Zhou Song 1 2,  Gui-Qing Zou 1 2,  Zhou Zhao 3,  Qiu-Ling Zheng 1 3,  Li-Juan Cao 1 2,  Guang-Ji Wang 1 2,  Hong Wang 1 2,  Hai-Ping Hao 1 3
Affiliations

Affiliations

  • 1 State Key Laboratory of Natural Medicines, Key Lab of Drug Metabolism and Pharmacokinetics, China Pharmaceutical University, 210009, Nanjing, China.
  • 2 Department of Pharmacology, School of Pharmacy, China Pharmaceutical University, 210009, Nanjing, China.
  • 3 Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, 210009, Nanjing, China.
PMID: 35853240 DOI: 10.1021/acs.analchem.2c01206
Abstract

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.

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