2. Signaling Pathways
  3. GPCR/G Protein
  4. P2Y Receptor
  5. P2Y11 Receptor Isoform

P2Y11 Receptor

P2Y11 receptor is a human purinergic receptor coupled to phosphoinositide and cyclic AMP signaling[1]. ATP, ATPγS, BzATP, dATP, and AR-C67085 activate recombinant human P2Y11 receptor, while ADPβS, AMPαS, and A3P5PS act as partial agonists[1]. Mechanistically, ATP and UTP can both mobilize Ca2+ through human P2Y11 receptor, but they recruit distinct signaling pathways[2]. In immune biology, current evidence supports a role for P2Y11 in immune activation with cell type-specific effects[3]. In disease models, P2RY11 variants associate with narcolepsy and altered ATP-induced cell death in T lymphocytes and NK cells[4]. In rheumatoid arthritis-derived fibroblast-like synoviocytes, P2Y11R expression rises and NF340 suppresses IL-1β-induced TNF-α, IL-6, MMP expression, oxidative stress, and NFκB signaling[5]. In lung fibroblasts, extracellular ATP or oxidative stress induces premature senescence through P2Y11R-linked ER Ca2+ release and mitochondrial ROS production[6]. Compared with related isoforms, P2Y11 remains experimentally distinctive because rodents lack a murine P2ry11 orthologue and some antibodies, expression assays, agonists, and antagonists have specificity limitations[3]. Therefore, P2Y11 receptor studies require human-relevant systems and carefully validated pharmacological tools[3].

References:

P2Y11 Receptor Related Products (1):

Cat. No. Product Name Effect Purity
  • HY-108659
    NF340
    		Antagonist
    NF340 is a P2Y11 receptor inhibitor with a pIC50 of 7.3-7.7 against human P2Y11 receptor, and it exhibits high selectivity over other P2Y family receptors. NF340 binds to the ATP-binding amino acid residues of the P2Y11 receptor to inhibit its activity, block nociceptive activity, and reduce spinal dorsal horn P2Y11 receptor upregulation induced by spinal nerve injury. NF340 attenuates the NFκB signaling pathway activated by IL-1β by decreasing IκBα phosphorylation, nuclear p65 accumulation, and NFκB promoter activity. NF340 inhibits IL-1β-induced pro-inflammatory cytokine expression, reduces intracellular ROS and 4-HNE levels, and suppresses IL-1β-induced matrix metalloproteinase expression in primary fibroblast-like synoviocytes. NF340 inhibits ATP-induced elevation of intracellular Ca2+ concentration and cell migration in human hepatocellular carcinoma cells. NF340 can be used in the research of neuropathic pain, myocardial ischemia/reperfusion injury, inflammatory pain, rheumatoid arthritis, and hepatocellular carcinoma.