Structural insights into the regulation of monomeric and dimeric apelin receptor
2025

Understanding the Apelin Receptor's Structure and Function

publication 10 minutes Evidence: high

Author Information

Author(s): Yue Yang, Liu Lier, Wu Lijie, Xu Chanjuan, Na Man, Liu Shenhui, Liu Yuxuan, Li Fei, Liu Junlin, Shi Songting, Lei Hui, Zhao Minxuan, Yang Tianjie, Ji Wei, Wang Arthur, Hanson Michael A., Stevens Raymond C., Liu Jianfeng, Xu Fei

Primary Institution: iHuman Institute, ShanghaiTech University, Shanghai, China

Hypothesis

How do ligand binding, receptor dimerization, and G protein coupling regulate the apelin receptor signaling pathway?

Conclusion

The study reveals that ligand binding and G protein coupling significantly influence the dimerization and activation of the apelin receptor.

Supporting Evidence

  • The apelin receptor is a promising drug target for cardiovascular health.
  • Binding of apelin-13 to the receptor induces significant vasodilation.
  • The study provides insights into the dynamic regulation of receptor dimerization.

Takeaway

This research shows how a special receptor in our body changes shape when it binds to certain molecules, which helps it send signals that are important for heart health.

Methodology

The study utilized cryo-electron microscopy to analyze the structures of the apelin receptor in different states.

Digital Object Identifier (DOI)

10.1038/s41467-024-55555-6

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