P2Y13: Identification and Characterization of a Novel Gαi-Coupled ADP Receptor from Human and Mouse
Open Access
- 1 May 2002
- journal article
- Published by Elsevier in The Journal of Pharmacology and Experimental Therapeutics
- Vol. 301 (2) , 705-713
- https://doi.org/10.1124/jpet.301.2.705
Abstract
We have identified an orphan G protein-coupled receptor, SP174, that shares a high degree of homology with the recently described ADP receptor P2Y12. mRNA for SP174 is abundant in the brain and in cells of the immune system. In the present study, we demonstrate that SP174 is also a receptor for ADP, which is coupled to Gαi. ADP potently stimulates SP174 with an EC50 of 60 nM, and other related nucleotides are active as well, with a rank order of potency 2-methylthio-ADP tetrasodium = adenosine 5′-O-2-(thio)diphosphate = 2-methylthio-ATP tetrasodium > ADP > AP3A >ATP > IDP. This pharmacological profile is similar to that for P2Y12. We have also identified the murine homolog of SP174, which exhibits 75% homology to the human receptor. ADP is also a potent agonist at the murine receptor, and its pharmacological profile is similar to its human counterpart, but ADP and related nucleotides are more potent at the murine receptor than the human receptor. In keeping with the general nomenclature for the purinergic receptors, we propose designating this novel receptor P2Y13.Keywords
This publication has 21 references indexed in Scilit:
- Identification of a Novel Human ADP Receptor Coupled to GiJournal of Biological Chemistry, 2001
- Molecular identification and characterization of the platelet ADP receptor targeted by thienopyridine antithrombotic drugsJournal of Clinical Investigation, 2001
- ADP Is the Cognate Ligand for the Orphan G Protein-coupled Receptor SP1999Journal of Biological Chemistry, 2001
- An expressed sequence tag (EST) data mining strategy succeeding in the discovery of new G-protein coupled receptors11Edited by J. ThorntonJournal of Molecular Biology, 2001
- A G Protein-coupled Receptor for UDP-glucoseJournal of Biological Chemistry, 2000
- Deoxyadenosine Bisphosphate Derivatives as Potent Antagonists at P2Y1 ReceptorsJournal of Medicinal Chemistry, 1998
- P2-Purinergic Receptors: Subtype-Associated Signaling Responses and StructureAnnual Review of Pharmacology and Toxicology, 1995
- Substitution of three amino acids switches receptor specificity of Gqα to that of GiαNature, 1993
- G PROTEINS: TRANSDUCERS OF RECEPTOR-GENERATED SIGNALSAnnual Review of Biochemistry, 1987
- Human T-cell clones recognize chemically synthesized peptides of influenza haemagglutininNature, 1982