Contents:
- Gene and Protein Information
- Previous and Unofficial Names
- Database Links
- Natural/Endogenous Ligands
- Rank order lists
- Agonists
- Antagonists
- Immuno Process Associations
- Transduction Mechanisms
- Tissue Distribution
- Expression Datasets
- Functional Assays
- Physiological Functions
- Physiological Consequences of Altering Gene Expression
- Phenotypes, Alleles and Disease Models
- Biologically Significant Variants
- General Comments
- References
- Contributors
- How to cite this page
Gene and Protein Information  |
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| class A G protein-coupled receptor | ||||||
| Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
| Human | 7 | 377 | 11q13.4 | P2RY2 | purinergic receptor P2Y2 | 60 |
| Mouse | 7 | 373 | 7 E2 | P2ry2 | purinergic receptor P2Y, G-protein coupled 2 | 54 |
| Rat | 7 | 374 | 1q32 | P2ry2 | purinergic receptor P2Y2 | 32,72 |
| Previous and Unofficial Names |
| ATP receptor | P2U purinoceptor 1 | P2Y ATP receptor 2 | P2Y purinoceptor 2 | purinergic receptor P2Y |
| Database Links |
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| Specialist databases | |
| GPCRdb | p2ry2_human (Hs), p2ry2_mouse (Mm), p2ry2_rat (Rn) |
| Other databases | |
| Alphafold | P41231 (Hs), P35383 (Mm), P41232 (Rn) |
| ChEMBL Target | CHEMBL4398 (Hs), CHEMBL1075298 (Mm), CHEMBL4419 (Rn) |
| DrugBank Target | P41231 (Hs) |
| Ensembl Gene | ENSG00000175591 (Hs), ENSMUSG00000032860 (Mm), ENSRNOG00000019283 (Rn) |
| Entrez Gene | 5029 (Hs), 18442 (Mm), 29597 (Rn) |
| Human Protein Atlas | ENSG00000175591 (Hs) |
| KEGG Gene | hsa:5029 (Hs), mmu:18442 (Mm), rno:29597 (Rn) |
| OMIM | 600041 (Hs) |
| Pharos | P41231 (Hs) |
| RefSeq Nucleotide | NM_002564 (Hs), NM_008773 (Mm), NM_017255 (Rn) |
| RefSeq Protein | NP_002555 (Hs), NP_032799 (Mm), NP_058951 (Rn) |
| UniProtKB | P41231 (Hs), P35383 (Mm), P41232 (Rn) |
| Wikipedia | P2RY2 (Hs) |
| Natural/Endogenous Ligands |
| ATP |
| UTP |
| Potency order of endogenous ligands (Human) |
| UTP > ATP |
Download all structure-activity data for this target as a CSV file 
| Agonists | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Key to terms and symbols | View all chemical structures | Click column headers to sort | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| Agonist Comments | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| PSB1114 is a potent, selective P2Y2 agonist with >60-fold selectivity for versus P2Y4 and P2Y6 receptors [24]. Reference [49] EC50 values are found using IP3 functional assays. References [62,81] EC50 values are found using Ca2+ functional assays. A library of nucleotide triphosphates incorporating a C-linked unnatural base (i.e., benzothiazole, benzoxazole and benzimidazole) was synthesized, a number of which offer potency comparable to that of the N-linked series, and significantly more stability than UTP [18]. |
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| Antagonists | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Key to terms and symbols | View all chemical structures | Click column headers to sort | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| Antagonist Comments | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| The rat P2Y2R is virtually insensitive to Reactive Blue 2 (pIC50 > 2) [9]. Although non-selective, suramin can be useful to discriminate between the P2Y2 and the P2Y4 receptor subtypes, the latter being insensitive to its antagonism [9]. A small library of 1-amino-4-phenylamino-2-sulfoanthraquinone derivatives related to Reactive Blue 2 has been synthesized, and some of them proved to be potential P2Y2R antagonists with low micromolar IC50 values [77]. |
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| Immuno Process Associations | ||
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| Primary Transduction Mechanisms
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| Transducer | Effector/Response |
| Gq/G11 family | Phospholipase C stimulation |
| Comments: In bronchial and intestinal epithelia, activation of P2Y2 receptor subtype leads to stimulation of chloride secretion through Gq/G11, and phospholipase C activation followed by inhibition of Na+ transport [21,30,80] | |
| References: 76,80 | |
| Secondary Transduction Mechanisms |
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| Transducer | Effector/Response |
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Gi/Go family G12/G13 family |
Other - See Comments |
| Comments: In hP2Y2R-transfected 1321N1 cells, P2Y2 receptor was found to couple through integrins to Gi/Go, leading to Rac activation, vitronectin up-regulation and increasing cell migration [6], and to G12, leading to Rho activation, cofilin and myosin light chain-2 phosphorylation, stress fiber formation and chemotaxis towards UTP [52]. Coupling of P2Y2 receptor to hematopoietic cell specific Gα16, belonging to the Gq family, was found in human erythroleukemia cells [46]. In the presence of nerve growth factor (NGF), the interaction between the P2Y2 receptor and tyrosine kinase A (TrkA) through Src was detected, followed by activation of ERK1/2 [3-4]. | |
| References: 6,52 | |
| Tissue Distribution
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| Expression Datasets |
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| Physiological Consequences of Altering Gene Expression
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| Phenotypes, Alleles and Disease Models
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| Biologically Significant Variants
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| General Comments |
| The three human transcript variants encode for the same 377 aa protein sequence [60]. P2Y2 receptors have been localized in mitochondria in rat astrocytes, C6 glioma cells and liver, suggesting their role in regulating mitochondrial calcium transport [8,47]. Denufosol tetrasodium is currently under evaluation as an inhaled treatment for cystic fibrosis (phase III clinical study), and diquafosol is in phase III clinical study for dry eye disease (http://clinicaltrials.gov/ct2/home). |
References
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