Introduction of P2RY4
P2RY4 is encoded by the P2RY4 gene. It belongs to the G-protein-coupled receptor (GPCR) family which has proved to be the drug targets of approximately 34% of all modern medicinal drugs. It is one of the eight subtypes of G protein-coupled P2Y receptors (P2RY1, P2RY2, P2RY4, P2RY6, P2RY11, P2RY12, P2RY13, and P2RY14). P2RY4 possesses seven transmembrane alpha helices and uses uridine nucleotides as the preferred endogenous agonist. Meanwhile, P2RY4 is also known as uridine nucleotides receptor and is activated by UTP and ATP partially, but cannot be activated by UDP or ADP.
|Basic Information of P2RY4|
|Protein Name||P2Y purinoceptor 4|
|Aliases||Uridine nucleotide receptor, UNR|
|Organism||Homo sapiens (Human)|
Function of P2RY4 Membrane Protein
G protein-coupled P2Y receptors family is expressed in almost all human tissues and they are of great interest as potential drug targets for many diseases, especially for neurodegenerative disorders and cardiovascular diseases. The activity of P2RY4 is mediated by uridine 5'-triphosphate (UTP) and adenosine triphosphate (ATP). P2RY4 expresses widely in the body, including central nervous system, heart, gastrointestinal tract, and skin. In the gastrointestinal tract, P2RY4 is reported to regulate the secretion of chloride. So, the P2RY4 agonists can be used as a possible target to treat the cystic fibrosis and P2RY4 antagonists are the possible targets for the treatment of diarrhea. P2RY4 also is reported to regulate the production of the amyloid precursor protein (APP) in the brain. Because the accumulation of APP in brain is associated with the development of Alzheimer’s disease, P2RY4 antagonists are possible therapeutic agents for the treatment of Alzheimer’s disease. However, no potential antagonists for P2RY4 have been reported so far, the development of selective antagonists for P2RY4 is a promising field.
Fig.1 Schematic representation of mechanism of P2RY4. (Paniagua-Herranz, 2017)
Application of P2RY4 Membrane Protein in Literature
This article reviews the extracellular nucleotides and P2X- and P2Y-receptor-mediated signaling pathway in many pathophysiological processes make the antagonists for P2Y4 receptor as potentially valuable therapeutic targets.
This article reveals that both P2Y4 and NMDAR1 receptor are involved in the metabolic impairment and the consequent cell death. At the same time, this article reports that P2RY4 is the first purinergic metabotropic receptor to be causal to cell death under conditions of metabolism impairment.
Authors in this group describe that ATP functions as a “drink me” signal through activation of P2Y4 receptors for soluble amyloid beta peptide 1-42 in microglia and P2Y4 receptors might be used as a potential drug target for the treatment of Alzheimer's disease.
This article reports that PGE2 activates P2Y2/P2Y4 receptors and mediates pro or anti-inflammatory in rat cerebellar astrocytes. Inhabitation the interaction between PGE2 and P2Y signaling can impair the UTP induced intracellular calcium responses and the nucleotide elicited astrocyte migration.
This article identifies that loss of P2Y4 could bring a new therapeutic perspective for the treatment of cardiac ischemia because cardiac permeability and neutrophil infiltration are down-regulated in LPS induced inflammation P2Y4 null mice model. Meanwhile, the authors identify a new protein, ET-1, as P2Y4 target genes, which is involved and down-regulation in cardiac ischemia.
P2RY4 Preparation Options
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