Wang Jiangyun/Liu Zhijie/Hua Tian's group has made important progress in the research of GPCR allosteric regulation mechanism

On October 1, 2021, the Journal of the American Chemical Society published an online publication titled "A Genetically Encoded F-19 NMR Probe Reveals the Allosteric Modulation Mechanism of Cannabinoid" by Wang Jiangyun's group and Shanghai University of Science and Technology Liu Zhijie and Hua Tian's group.

The fluorine atom is widely used in the study of protein dynamic conformation due to its high sensitivity to protein environmental changes, 100% natural abundance and no background signal

CB1 cannabinoid receptors in the brain is one of GPCR people express the highest amount, the regulation of many important physiological activities, is the treatment of neurological and psychiatric diseases, obesity and other important targets

Figure 1.

Through the close cooperation and unremitting efforts of the team, the dynamic process and polymorphism of the receptor were deciphered using ¹⁹ F-NMR, and combined with the X-ray crystallographic method, the unique regulation mechanism of the allosteric modulator Org27569 on CB1 was revealed.

Figure 2.

This work was jointly completed by the Institute of Biophysics, Chinese Academy of Sciences and the iHuman Institute of Shanghai University of Science and Technology

Article link: https://pubs.

(Contribution: Wang Jiangyun Research Group)