P2Y11 receptor (previously known as P2Y) 2.1:NUCT:5:P2Y11
| TM | aa | AC | Chr. Map | References | |
|---|---|---|---|---|---|
| Human | 7 | 374 | NM_002566* | 19p13.2 | Communi et al. (1997) |
| Functional assays | cAMP measurement in CHO-K1 cells stably expressing the P2Y11 receptor; IP3 measurement in 1321N1 astrocytoma cells stably expressing the P2Y11 receptor (Communi et al., 1997) | ||||
| Ligand | Action | Selectivity | Endogenous | References |
|---|---|---|---|---|
| ATP | Agonist | No | Yes | Communi et al. (1999b) |
| ADP | Agonist | No | Yes | Communi et al. (1999b) |
| ATPγS | Agonist | No | No | Communi et al. (1999b) |
| BzATP | Agonist | No | No | Communi et al. (1999b) |
| dATP | Agonist | No | No | Communi et al. (1999b) |
| ADPβS | Agonist | No | No | Communi et al. (1999b) |
| 2-MeSATP | Agonist | No | No | Communi et al. (1999b) |
| AR-C67085 | Agonist | No | No | Communi et al. (1999b) |
| ADPγS | Partial agonist | No | No | Communi et al. (1999b) |
| AMPαS | Partial agonist | No | No | Communi et al. (1999b) |
| A3P5PS | Partial agonist | No | No | Communi et al. (1999b) |
| Suramin | Antagonist | No | No | Communi et al. (1999b) |
| Reactive blue 2 | Antagonist | No | No | Communi et al. (1999b) |
| UTP | Agonist | No | Yes | White et al. (2003) |
| Agonist potencies** | cAMP: ATPγS (EC50 3.4 ± 0.3 μM) > BzATP (EC50 7.2 ± 0.5 μM) > dATP (EC50 8.9 ± 0.6 μM) > ATP (EC50 17.4 ± 6.1 μM) > ADPβS (EC50 29.7 ± 2.7 μM) > 2-MeSATP (EC50 50 ± 4 μM) (Communi et al., 1999b); IP3: BzATP (EC50 10.5 ± 0.3 μM) > ATPγS (EC50 13.5 ± 2.7 μM) > dATP (EC50 16.3 ± 0.7 μM) > ATP (EC50 65 ± 12 μM) > ADPβS (EC50 174 ± 28 μM) > 2-MeSATP (EC50 210 ± 6 μM) (Communi et al., 1999b) | |||
| Antagonist potencies | PI hydrolysis: suramin (IC50 1 μM), reactive blue 2 (IC50 9 μM); cAMP: suramin (IC50 16 μM) (Communi et al., 1999b) | |||
| Radioligand assays | None | |||
| Radioligands | None | |||
| Transduction mechanism | Gq/G11 and Gs (see “Comments”); PI hydrolysis (PLCβ activation) and elevated [Ca2+]i in expression systems; adenylate cyclase stimulation and elevated cAMP levels (Qi et al., 2001a) | |||
| Distribution | Brain, spleen, lymphocytes, intestine; all other tissues expressed more moderate levels of P2Y11 mRNA, with lowest levels detected in liver, cartilage, and bone (Moore et al., 2001) | |||
| Tissue function | Role in maturation, migration of dendritic cells (Wilkin et al., 2001; Schnurr et al., 2003), and in granulocytic differentiation (Communi et al., 2000); secretory role in pancreatic duct epithelial cells (Nguyen et al., 2001) | |||
| Phenotypes | None | |||
| Comments | In P2Y11 gene, an intron was found (Communi et al., 1997)*; P2Y11 couples to Gq and Gs, and the pharmacological profile of the GPCR is slightly different for each transduction pathway (PLCβ/IP3 and adenylate cyclase/cAMP) (Communi et al., 1999b; Qi et al., 2001a); the receptor does not activate PLA2 or PLD (Communi et al., 1999b); the P2Y12 antagonist ARC67085MX is an agonist here; a chimeric mRNA due to intergenic splicing between the P2Y11 and Ssf1 genes has been found in many mammalian cells—the function of this fusion protein is unknown (Communi et al., 2001); a canine (Qi et al., 2001a; Zambon et al., 2001) but no mouse and rat orthologs have been cloned; agonist potencies are species-dependent (Qi et al., 2001a; Zambon et al., 2001)** | |||
aa, amino acids; AC, accession; chr., chromosome.