Structure-based design of non-hypertrophic apelin receptor modulator. (https://pubmed.ncbi.nlm.nih.gov/38428423/)

These scientists studied a hormone called apelin that helps keep the heart healthy. They found that activating a specific receptor in the body, called the apelin receptor, could be a good way to treat heart problems. However, they also discovered that some treatments targeting this receptor can have negative side effects.

To find a better solution, the scientists used a special technique called cryoelectron microscopy to look at the structure of the apelin receptor when it is activated by different substances. They found two new substances, called WN353 and WN561, that can activate the receptor in a way that is good for the heart without causing bad side effects.

They tested these new substances in experiments and found that WN561 was especially effective at treating heart problems like cardiac hypertrophy, which is when the heart muscle becomes too thick. Compared to other treatments, WN561 had fewer negative effects on the body.

Overall, the scientists believe that these new substances could be used to create better medicines for heart conditions in the future.

Wang WW., Ji SY., Zhang W., Zhang J., Cai C., Hu R., Zang SK., Miao L., Xu H., Chen LN., Yang Z., Guo J., Qin J., Shen DD., Liang P., Zhang Y., Zhang Y. Structure-based design of non-hypertrophic apelin receptor modulator. Cell. 2024 Mar 14;187(6):1460-1475.e20. doi: 10.1016/j.cell.2024.02.004. Epub 2024 Feb 29.