Lai Wei, Kaijing Xiang, Hongjian Kang, Yancheng Yu, Hongjie Fan, Han Zhou, Tao Hou, Yonglin Ge, Jixia Wang, Zhimou Guo, Yang Chen, Yaopeng Zhao, Xinmiao Liang
The orphan G protein-coupled receptor 35 (GPR35) is a potential target for the treatment of pain, inflammation, and metabolic diseases. Although many GPR35 agonists have been discovered, research on functional GPR35 ligands, such as fluorescent probes, is still limited. Herein, we developed a series of GPR35 fluorescent probes by conjugating a BODIPY fluorophore to DQDA , a known GPR35 agonist. All probes exhibited excellent GPR35 agonistic activity and desired spectroscopic properties, as determined by the DMR assay, bioluminescence resonance energy transfer (BRET)-based saturation, and kinetic binding experiments...
April 13, 2023: ACS Medicinal Chemistry Letters