Structural basis of ligand recognition and self-activation of orphan GPR52
© CHRISTOPH BURGSTEDT/SCIENCE PHOTO LIBRARY/Getty
The determination of the three-dimensional structure of a protein receptor implicated in psychiatric disorders will help efforts to develop drugs to treat those disorders.
Cells detect changes in their chemical environment via proteins on their surfaces known as receptors. G-protein-coupled receptors (GPCRs) are largest family of such receptors, with more than 800 of them known in humans. Many commercial drugs act by binding to GPCRs.
Now, a team led by researchers from ShanghaiTech University has determined for the first time the three-dimensional structure of GPR52, a GPCR that is highly expressed in the brain and that has been implicated in Huntington’s disease and other psychiatric disorders.
This structural knowledge is all the more valuable because GPR52 is an orphan GPCR, meaning that the natural occurring molecules that activate it by binding to it have yet to be identified.
- Nature 579, 152–157 (2020) doi: 10.1038/s41586-020-2019-0