Therapeutic potential of GPR17, an orphan G protein-coupled receptor

The orphan G protein-coupled receptor GPR17 has emerged as a potential therapeutic target for multiple sclerosis (MS) and other demyelinating diseases. 

By contrast with current MS therapeutics, GPR17 antagonists are expected to induce myelin repair which may result in a curative treatment for this debilitating chronic disease.

A recent cryo-electron microscopy (cryoEM) study provided structural insights into the unliganded receptor.

Whereas its physiological agonist is still unknown, the development of potent and selective synthetic agonists and antagonists has enabled pharmacological research, including preclinical studies.

Several patents on GPR17 antagonists have been filed, and the results of the first clinical study are eagerly awaited.

https://www.cell.com/trends/pharmacological-sciences/fulltext/S0165-6147(25)00091-4

https://sciencemission.com/GPR17-%E2%80%93-orphan-G-protein-coupled-receptor