The absence of mature oligodendrocytes for the repair of demyelination lesions is a critical factor in the pathology of Multiple Sclerosis (MS), and other debilitating CNS disorders of myelination. As such, regulating the maturation of oligodendrocytes and the resulting myelin production is an interesting target for potential new therapeutics.

GPR17 is an orphan G-protein-coupled receptor (GPCR) that is abundant in the CNS, and has been shown to play a key role in regulating oligodendrocyte differentiation and maturation. Unfortunately, little has been known about the exact mechanism through which GPR17 influences myelination.