Structural insight into apelin receptor-G protein stoichiometry

The structure of a drug target for heart disease

31 October 2022

The three-dimensional structure of an important target of cardiovascular drugs has been determined for the first time.

The active human apelin receptor is a protein that plays a key role in the development of the heart. It has attracted a lot of interest as a target for new drugs to treat cardiovascular conditions. A better knowledge of how active human apelin receptor binds with small molecules would help to develop better drugs.

Now, a team led by researchers from ShanghaiTech University in China has used cryogenic-electron microscopy to determine the receptor’s structure in complex with a small signalling molecule.

Their findings reveal ways in which the signalling of these small molecules can be controlled. This will help to develop drugs for cardiac diseases that are more selective, and hence will have fewer side effects.

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References

1. Nature Structural & Molecular Biology 29, 688–697 (2022). doi: 10.1038/s41594-022-00797-5