title: The G Protein-Coupled Receptor GPR17: Overview and Update.
abstract: The GPR17 receptor is a G protein-coupled receptor (GPCR) that seems to respond to two unrelated families of endogenous ligands: nucleotide sugars (UDP, UDP-galactose, and UDP-glucose) and cysteinyl leukotrienes (LTD4, LTC4, and LTE4), with significant affinity at micromolar and nanomolar concentrations, respectively. This receptor has a broad distribution at the level of the central nervous system (CNS) and is found in neurons and in a subset of oligodendrocyte precursor cells (OPCs). Unfortunately, disparate results emerging from different laboratories have resulted in a lack of clarity with regard to the role of GPR17-targeting ligands in OPC differentiation and in myelination. GPR17 is also highly expressed in organs typically undergoing ischemic damage and has various roles in specific phases of adaptations that follow a stroke. Under such conditions, GPR17 plays a crucial role; in fact, its inhibition decreases the progression of ischemic damage. This review summarizes some important features of this receptor that could be a novel therapeutic target for the treatment of demyelinating diseases and for repairing traumatic injury.
authors.affiliation: School of Pharmacy, Medicinal Chemistry Unit, University of Camerino, Via S. Agostino, 1, 62032, Camerino, MC, Italy.
authors.forename: Gabriella
authors.identifier: http://orcid.org/0000-0002-9856-9873
authors.initials: G
authors.lastname: Marucci
authors.affiliation: School of Pharmacy, Medicinal Chemistry Unit, University of Camerino, Via S. Agostino, 1, 62032, Camerino, MC, Italy.
authors.forename: Diego
authors.initials: D
authors.lastname: Dal Ben
authors.affiliation: School of Pharmacy, Medicinal Chemistry Unit, University of Camerino, Via S. Agostino, 1, 62032, Camerino, MC, Italy.
authors.forename: Catia
authors.initials: C
authors.lastname: Lambertucci
authors.affiliation: School of Pharmacy, Medicinal Chemistry Unit, University of Camerino, Via S. Agostino, 1, 62032, Camerino, MC, Italy.
authors.forename: Claudia
authors.initials: C
authors.lastname: Santinelli
authors.affiliation: School of Pharmacy, Medicinal Chemistry Unit, University of Camerino, Via S. Agostino, 1, 62032, Camerino, MC, Italy.
authors.forename: Andrea
authors.initials: A
authors.lastname: Spinaci
authors.affiliation: School of Pharmacy, Medicinal Chemistry Unit, University of Camerino, Via S. Agostino, 1, 62032, Camerino, MC, Italy.
authors.forename: Ajiroghene
authors.initials: A
authors.lastname: Thomas
authors.affiliation: School of Pharmacy, Medicinal Chemistry Unit, University of Camerino, Via S. Agostino, 1, 62032, Camerino, MC, Italy.
authors.forename: Rosaria
authors.initials: R
authors.lastname: Volpini
authors.affiliation: School of Pharmacy, Medicinal Chemistry Unit, University of Camerino, Via S. Agostino, 1, 62032, Camerino, MC, Italy.
authors.forename: Michela
authors.identifier: http://orcid.org/0000-0002-8383-0813
authors.initials: M
authors.lastname: Buccioni
mesh_terms: D000818:Animals; D002454:Cell Differentiation; D006801:Humans; D008024:Ligands; D009186:Myelin Sheath / Q000378:metabolism; D009836:Oligodendroglia / Q000166:cytology / Q000378:metabolism; D011485:Protein Binding; D043562:Receptors, G-Protein-Coupled / Q000819:agonists / Q000037:antagonists & inhibitors / Q000378:metabolism*
chemical_list: D008024:Ligands; D043562:Receptors, G-Protein-Coupled
keywords: G protein-coupled receptors; leukotrienes; membrane proteins; myelination; oligodendrocyte precursor cells (OPCs)