Top ▲

P2Y14 receptor

Click here for help

Immunopharmacology Ligand  Target has curated data in GtoImmuPdb

Target id: 330

Nomenclature: P2Y14 receptor

Family: P2Y receptors

Contents:

Gene and Protein Information Click here for help
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 338 3q25.1 P2RY14 purinergic receptor P2Y14 8,33
Mouse 7 338 3 28.96 cM P2ry14 purinergic receptor P2Y, G-protein coupled, 14 11
Rat 7 305 2q26 P2ry14 purinergic receptor P2Y14 11
Previous and Unofficial Names Click here for help
G protein coupled receptor for UDP-glucose | G protein-coupled receptor 105 | GPR105 | P2Y purinoceptor 14 | G-protein coupled receptor 105 | purinergic receptor P2Y
Database Links Click here for help
Specialist databases
GPCRdb p2y14_human (Hs), p2y14_mouse (Mm), p2y14_rat (Rn)
Other databases
Alphafold Q15391 (Hs), Q9ESG6 (Mm), O35881 (Rn)
ChEMBL Target CHEMBL4518 (Hs), CHEMBL1770046 (Mm), CHEMBL4295660 (Rn)
Ensembl Gene ENSG00000174944 (Hs), ENSMUSG00000036381 (Mm), ENSRNOG00000013872 (Rn)
Entrez Gene 9934 (Hs), 140795 (Mm), 171108 (Rn)
Human Protein Atlas ENSG00000174944 (Hs)
KEGG Gene hsa:9934 (Hs), mmu:140795 (Mm), rno:171108 (Rn)
OMIM 610116 (Hs)
Pharos Q15391 (Hs)
RefSeq Nucleotide NM_014879 (Hs), NM_133200 (Mm), NM_133577 (Rn)
RefSeq Protein NP_055694 (Hs), NP_573463 (Mm), NP_598261 (Rn)
UniProtKB Q15391 (Hs), Q9ESG6 (Mm), O35881 (Rn)
Wikipedia P2RY14 (Hs)
Natural/Endogenous Ligands Click here for help
UDP
UDP-galactose
UDP-glucose
UDP-glucuronic acid
UDP N-acetyl-glucosamine
Potency order of endogenous ligands (Human)
UDP= UDP-glucose

Download all structure-activity data for this target as a CSV file go icon to follow link

Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
α.β-methylene-2-thio-UDP Small molecule or natural product Hs Full agonist 9.0 pEC50 9
⤷ pEC50 9.0 (EC50 9.2x10-10 M) [9]
MRS4183 Small molecule or natural product Ligand is labelled Hs Agonist 9.0 pEC50 22
⤷ pEC50 9.0 (EC50 9.6x10-10 M) [22]
Description: Measuring inhibition of forskolin-stimulated cAMP formation in CHO cells expressing the human P2Y14 receptor
MRS2905 Small molecule or natural product Hs Agonist 9.0 pEC50 21
⤷ pEC50 9.0 (EC50 9.2x10-10 M) [21]
2-thio-UDP Small molecule or natural product Hs Full agonist 8.7 pEC50 9
⤷ pEC50 8.7 (EC50 1.92x10-9 M) [9]
UDP-glucose Small molecule or natural product Click here for species-specific activity table Ligand is endogenous in the given species Ligand has a PDB structure Mm Full agonist 7.7 pEC50 11
⤷ pEC50 7.7 [11]
UDP-galactose Small molecule or natural product Click here for species-specific activity table Ligand is endogenous in the given species Ligand has a PDB structure Mm Full agonist 7.6 pEC50 11
⤷ pEC50 7.6 [11]
UDP-glucose Small molecule or natural product Ligand is endogenous in the given species Ligand has a PDB structure Rn Full agonist 7.6 pEC50 11
⤷ pEC50 7.6 [11]
UDP-glucuronic acid Small molecule or natural product Ligand has a PDB structure Hs Full agonist 7.2 pEC50 12
⤷ pEC50 7.2 [12]
UDP-glucuronic acid Small molecule or natural product Ligand is endogenous in the given species Ligand has a PDB structure Mm Full agonist 7.2 pEC50 11
⤷ pEC50 7.2 [11]
MRS2802 Small molecule or natural product Hs Agonist 7.2 pEC50 9
⤷ pEC50 7.2 (EC50 6.3x10-8 M) [9]
UDP Small molecule or natural product Click here for species-specific activity table Ligand is endogenous in the given species Ligand has a PDB structure Hs Full agonist 7.1 pEC50 6
⤷ pEC50 7.1 (EC50 7.4x10-8 M) [6]
UDP-galactose Small molecule or natural product Ligand is endogenous in the given species Ligand has a PDB structure Rn Full agonist 7.1 pEC50 11
⤷ pEC50 7.1 [11]
UDP N-acetyl-glucosamine Small molecule or natural product Ligand is endogenous in the given species Ligand has a PDB structure Mm Full agonist 7.0 pEC50 11
⤷ pEC50 7.0 [11]
UDP-galactose Small molecule or natural product Click here for species-specific activity table Ligand is endogenous in the given species Ligand has a PDB structure Hs Full agonist 7.0 pEC50 8
⤷ pEC50 7.0 [8]
UDP-glucuronic acid Small molecule or natural product Ligand is endogenous in the given species Ligand has a PDB structure Rn Full agonist 7.0 pEC50 11
⤷ pEC50 7.0 [11]
MRS2690 Small molecule or natural product Hs Agonist 6.6 – 7.3 pEC50 16,24
⤷ pEC50 6.6 – 7.3 (EC50 2.29x10-7 – 4.9x10-8 M) [16,24]
UDP N-acetyl-glucosamine Small molecule or natural product Ligand is endogenous in the given species Ligand has a PDB structure Rn Full agonist 6.8 pEC50 11
⤷ pEC50 6.8 [11]
UDP N-acetyl-glucosamine Small molecule or natural product Ligand has a PDB structure Hs Full agonist 6.0 pEC50 12
⤷ pEC50 6.0 [12]
UDP-glucose Small molecule or natural product Click here for species-specific activity table Ligand is endogenous in the given species Ligand has a PDB structure Hs Full agonist 7.1 pIC50 12
⤷ pIC50 7.1 [12]
UDP Small molecule or natural product Ligand is endogenous in the given species Ligand has a PDB structure Rn Full agonist 6.5 pIC50 13
⤷ pIC50 6.5 [13]
View species-specific agonist tables
Agonist Comments
UDP-galactose, UDP glucuronic acid and UDP N-acethyl-glucosamine have also been reported to act as partial agonists [36]. Several analogues of UDP-glucose modified on nucleobase, ribose and glucose moieties have been synthesyzed and pharmacologically characterized in association with modeling studies [24]. Molecular dynamics of P2Y14 has allowed analysis of the putative receptor binding site to UDP-glucose and derivatives [20]. Covalent conjugation of polyamidoamine dendrimers to UDP-glucose enhances pharmacological activity of the agonist [10]. Further compounds with agonist activity have been synthesized and not included in this table [9].
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
PPTN Small molecule or natural product Hs Antagonist 10.1 pKi 2
⤷ pKi 10.1 (KB 4.34x10-10 M) [2]
MRS4174 Small molecule or natural product Ligand is labelled Hs Antagonist 10.1 pKi 23
⤷ pKi 10.1 (Ki 8x10-11 M) [23]
P2Y14R antagonist I-17 Small molecule or natural product Immunopharmacology Ligand Hs Antagonist 9.2 pIC50 28
⤷ pIC50 9.2 (IC50 6x10-10 M) [28]
MRS4625 Small molecule or natural product Hs Antagonist 7.6 pIC50 31
⤷ pIC50 7.6 (IC50 2.76x10-8 M) [31]
MRS4625 Small molecule or natural product Mm Antagonist 7.5 pIC50 31
⤷ pIC50 7.5 (IC50 2.97x10-8 M) [31]
MRS4458 Small molecule or natural product Immunopharmacology Ligand Hs Antagonist 6.8 pIC50 40
⤷ pIC50 6.8 (IC50 1.69x10-7 M) [40]
MRS4478 Small molecule or natural product Immunopharmacology Ligand Hs Antagonist 6.6 pIC50 40
⤷ pIC50 6.6 (IC50 2.69x10-7 M) [40]
View species-specific antagonist tables
Antagonist Comments
UDP was previously described to be a competitive antagonist in cells transfected with the human receptor [13]. This statement has been revised by further studies from the same group [6]. SAR studies identified compounds acting as antagonists at P2Y14 with good pharmacokynetic properties [17-18,34]. A non-nucleotidic ligand has been demonstrated to be active on P2Y14 [19].
Immunopharmacology Comments
In reponse to activation by uridine nucleotides (which can be released by stressed ot damaged tissues and organs) the P2Y14 receptor (P2Y14R) activates pro-inflammatory activity in part by increasing neutrophil motility [2,37], and this boosts the innate and adaptive immune responses [1,5,7]. In order to examine the potential anti-inflammatory effects arising from P2Y14R blockade, selective antagonist molecules are being developed [40].
Primary Transduction Mechanisms Click here for help
Transducer Effector/Response
Gi/Go family Adenylyl cyclase inhibition
References:  35
Secondary Transduction Mechanisms Click here for help
Transducer Effector/Response
Gi/Go family Phospholipase C stimulation
Comments: 

P2Y14 coupled to Gαi, can activate PLCβ via beta/gamma subunits. It has been demonstrated that in endothelial cells calcium influx are mediated by β/γ subunits of Gα0 but not to Gαi [311,154].

Primary glial cells have been reported to respond to UDP-glucose with increases of intracellular calcium concentrations highlighting a role for this receptor in glial cells [4,14].
References:  4,30
Tissue Distribution Click here for help
Glial cells mainly in white matter, less abundant in grey matter.
Species:  Human
Technique:  Immunohistochemistry.
References:  30
Placenta, adipose tissue, intestine > stomach, skeletal muscle > spleen, lung, heart > peripheral blood mononuclear cells, pituitary, various brain regions >> kidney, liver, prostate, pancreas, bone marrow.
Species:  Human
Technique:  RT-PCR.
References:  8
Spleen and isolated T- and B-lymphocytes.
Species:  Human
Technique:  RT-PCR.
References:  35
Heart, placenta, smooth muscle >> spleen, lymph node, thymus.
Species:  Human
Technique:  Northern blotting.
References:  27
Platelets
Species:  Human
Technique:  Western blotting
References:  3
HL-60 cells differentiated with DMSO (not expressed in wild-type HL-60 cells)
Species:  Human
Technique:  RT-PCR
References:  12
Dental follicle cells and adipose tissue-derived stem cells
Species:  Human
Technique:  RT-PCR
References:  41
Neurons from dorsal root ganglia
Species:  Mouse
Technique:  RT-PCR
References:  29
Spleen, thymus > brain, heart, lung.
Species:  Mouse
Technique:  RT-PCR.
References:  11
Spinal microglia
Species:  Rat
Technique:  RT-PCR
References:  25
Forestomach>>distal stomach, rectum, colon, duodenum, jeunum, ileum, vagus nerve
Species:  Rat
Technique:  Real-time PCR
References:  3
Expression Datasets Click here for help

Show »

Log average relative transcript abundance in mouse tissues measured by qPCR from Regard, J.B., Sato, I.T., and Coughlin, S.R. (2008). Anatomical profiling of G protein-coupled receptor expression. Cell, 135(3): 561-71. [PMID:18984166] [Raw data: website]

There should be a chart of expression data here, you may need to enable JavaScript!
Functional Assays Click here for help
MAP kinase activation assay
Species:  Human
Tissue:  DMSO differentiated HL-60 cells
Response measured:  Activation of ERK 1/2
References:  12
Measurement of Ca2+ levels in monocyte-derived dendritic cells (MDDCs).
Species:  Human
Tissue:  MDDCs.
Response measured:  Ca2+ mobilisation.
References:  38
Measurement of Ca2+ levels in HEK 293 cells transfected with the P2Y14 recetor.
Species:  Human
Tissue:  HEK 293 cells.
Response measured:  Ca2+ mobilisation.
References:  30
Measurement of Ca2+ levels in epithelial cell lines A549 and BEAS-2B endogenously expressing the P2Y14 receptor.
Species:  Human
Tissue:  A549 and BEAS-2B cells.
Response measured:  Ca2+ mobilisation.
References:  32
Measurement of interleukin-8 (IL-8) secretion in epithelial cell lines A549 and BEAS-2B endogenously expressing the P2Y14 receptor.
Species:  Human
Tissue:  A549 and BEAS-2B cells.
Response measured:  Increase in IL-8 secretion.
References:  32
Measurement of cAMP levels in spleen-derived T-lymphocyte cells endogenously expressing the P2Y14 receptor.
Species:  Human
Tissue:  T-lymphocytes.
Response measured:  Small yet significant inhibition of cAMP accumulation.
References:  35
Measurement of cAMP levels in C6 cells
Species:  Rat
Tissue:  C6 glioma cells
Response measured:  inhibition of cAMP (abolished by PTX)
References:  26
Measurement of cAMP levels in neutrophils
Species:  Human
Tissue:  neutrophils
Response measured:  Inhibition of cAMP mediated by UDP-glucose stimulation, but not by UDP-galactose or UDP glucuronic acid. UDP N-acethyl-glucosamine produced a small but significant inhibition of cAMP
References:  36
Rho activation assay
Species:  Human
Tissue:  Neutrophils and HL-60 cells
Response measured:  Activation of Rho GTPases
References:  37
Intracellular calcium mobilization
Species:  Rat
Tissue:  RBL-2H3 mast cells
Response measured:  Calcium transients induced by UDP-glucose and MRS2690
References:  15
MAP kinase activation assay
Species:  Rat
Tissue:  RBL-2H3 mast cells
Response measured:  Activation of ERK1/2, JNK and P38 MAP kinases
References:  15
FLIPR and cellular impedance functional assays
Species:  Human
Tissue:  HEK293 cells
Response measured:  UMP and UDP selectively activate HEK cells coexpressing P2Y14 and Gqi5
References:  19
Physiological Functions Click here for help
Chemotaxis.
Species:  Human
Tissue:  Bone marrow stoma cells.
References:  27
Contractile effect on isolated forestomach
Species:  Rat
Tissue:  forestomach
References:  3
Role in neuroimmune function
Species:  Human
Tissue:  Glial cells
References:  30
Role in dendritic cells activation
Species:  Human
Tissue:  immunocytes
References:  38
Increase in mast cells degranulation
Species:  Rat
Tissue:  RBL-2H3 mast cells
References:  15
Inhibition of CFA induced hyperalgesia
Species:  Mouse
Tissue:  Peripheral neurous system
References:  29
Chemotaxis of neutrophils
Species:  Human
Tissue:  Neutrophils
References:  37
Regulation of mesenchymal differentiation
Species:  Human
Tissue:  Adipose tissue-derived mesenchymal stem cells
References:  41
Physiological Consequences of Altering Gene Expression Click here for help
In knockout mice there are no differences in terms of gastric emptying compared to wild-type
Species:  Rat
Tissue: 
Technique:  Gene targeting in embryonic stem cells
References:  3
Reduction of neuropathic pain. Inhibiting P2Y14 expression reverts mechanical allodynia induced after peripheral nerve injury
Species:  Rat
Tissue:  Peripheral nerves
Technique:  Antisense LNA
References:  25
P2Y14 knockout mice are protected from high-fat diet induced insulin resistance, show an improved insulin sensitivity, and a reduced hepatic steatosis
Species:  Mouse
Tissue:  Liver
Technique:  Gene knockouts
References:  39
P2Y14 ablation results in a reduced chemotaxis and number of macrophaes in the liver
Species:  Mouse
Tissue:  Macrophages
Technique:  Gene knockouts
References:  39
Phenotypes, Alleles and Disease Models Click here for help Mouse data from MGI

Show »

Allele Composition & genetic background Accession Phenotype Id Phenotype Reference
P2ry14tm1Gbtm P2ry14tm1Gbtm/P2ry14tm1Gbtm
B6.129P2-P2ry14		 MGI:2155705  MP:0002106 abnormal muscle physiology PMID: 19164486 
General Comments
P2Y14 is selectively activated by sugar nucleotides. Only recently UDP has been demonstrated to act as an agonist at this receptor [6]. The different transcript variants for P2Y14 found in human and mouse encode for the same receptor protein.

References

Show »

1. Abbracchio MP, Burnstock G, Boeynaems JM, Barnard EA, Boyer JL, Kennedy C, Knight GE, Fumagalli M, Gachet C, Jacobson KA et al.. (2006) International Union of Pharmacology LVIII: update on the P2Y G protein-coupled nucleotide receptors: from molecular mechanisms and pathophysiology to therapy. Pharmacol Rev, 58 (3): 281-341. [PMID:16968944]

2. Barrett MO, Sesma JI, Ball CB, Jayasekara PS, Jacobson KA, Lazarowski ER, Harden TK. (2013) A Selective High-Affinity Antagonist of the P2Y14 Receptor Inhibits UDP-Glucose-Stimulated Chemotaxis of Human Neutrophils. Mol Pharmacol, 84 (1): 41-9. [PMID:23592514]

3. Bassil AK, Bourdu S, Townson KA, Wheeldon A, Jarvie EM, Zebda N, Abuin A, Grau E, Livi GP, Punter L et al.. (2009) UDP-glucose modulates gastric function through P2Y14 receptor-dependent and -independent mechanisms. Am J Physiol Gastrointest Liver Physiol, 296 (4): G923-30. [PMID:19164486]

4. Bianco F, Fumagalli M, Pravettoni E, D'Ambrosi N, Volonté C, Matteoli M, Abbracchio MP, Verderio C. (2005) Pathophysiological roles of extracellular nucleotides in glial cells: differential expression of purinergic receptors in resting and activated microglia. Brain Res Brain Res Rev, 48: 144-156. [PMID:15850653]

5. Burnstock G. (2017) Purinergic Signalling: Therapeutic Developments. Front Pharmacol, 8: 661. [PMID:28993732]

6. Carter RL, Fricks IP, Barrett MO, Burianek LE, Zhou Y, Ko H, Das A, Jacobson KA, Lazarowski ER, Harden TK. (2009) Quantification of Gi-mediated inhibition of adenylyl cyclase activity reveals that UDP is a potent agonist of the human P2Y14 receptor. Mol Pharmacol, 76 (6): 1341-8. [PMID:19759354]

7. Cekic C, Linden J. (2016) Purinergic regulation of the immune system. Nat Rev Immunol, 16 (3): 177-92. [PMID:26922909]

8. Chambers JK, Macdonald LE, Sarau HM, Ames RS, Freeman K, Foley JJ, Zhu Y, McLaughlin MM, Murdock P, McMillan L et al.. (2000) A G protein-coupled receptor for UDP-glucose. J Biol Chem, 275 (15): 10767-71. [PMID:10753868]

9. Das A, Ko H, Burianek LE, Barrett MO, Harden TK, Jacobson KA. (2010) Human P2Y(14) receptor agonists: truncation of the hexose moiety of uridine-5'-diphosphoglucose and its replacement with alkyl and aryl groups. J Med Chem, 53 (1): 471-80. [PMID:19902968]

10. Das A, Zhou Y, Ivanov AA, Carter RL, Harden TK, Jacobson KA. (2009) Enhanced potency of nucleotide-dendrimer conjugates as agonists of the P2Y14 receptor: multivalent effect in G protein-coupled receptor recognition. Bioconjug Chem, 20 (8): 1650-9. [PMID:19572637]

11. Freeman K, Tsui P, Moore D, Emson PC, Vawter L, Naheed S, Lane P, Bawagan H, Herrity N, Murphy K et al.. (2001) Cloning, pharmacology, and tissue distribution of G-protein-coupled receptor GPR105 (KIAA0001) rodent orthologs. Genomics, 78 (3): 124-8. [PMID:11735218]

12. Fricks IP, Carter RL, Lazarowski ER, Harden TK. (2009) Gi-dependent cell signaling responses of the human P2Y14 receptor in model cell systems. J Pharmacol Exp Ther, 330 (1): 162-8. [PMID:19339661]

13. Fricks IP, Maddileti S, Carter RL, Lazarowski ER, Nicholas RA, Jacobson KA, Harden TK. (2008) UDP is a competitive antagonist at the human P2Y14 receptor. J Pharmacol Exp Ther, 325 (2): 588-94. [PMID:18252808]

14. Fumagalli M, Brambilla R, D'Ambrosi N, Volonté C, Matteoli M, Verderio C, Abbracchio MP. (2003) Nucleotide-mediated calcium signaling in rat cortical astrocytes: Role of P2X and P2Y receptors. Glia, 43: 218-203. [PMID:12898701]

15. Gao ZG, Ding Y, Jacobson KA. (2010) UDP-glucose acting at P2Y14 receptors is a mediator of mast cell degranulation. Biochem Pharmacol, 79 (6): 873-9. [PMID:19896471]

16. Gao ZG, Wei Q, Jayasekara MP, Jacobson KA. (2013) The role of P2Y(14) and other P2Y receptors in degranulation of human LAD2 mast cells. Purinergic Signal, 9 (1): 31-40. [PMID:22825617]

17. Gauthier JY, Belley M, Deschênes D, Fournier JF, Gagné S, Gareau Y, Hamel M, Hénault M, Hyjazie H, Kargman S et al.. (2011) The identification of 4,7-disubstituted naphthoic acid derivatives as UDP-competitive antagonists of P2Y14. Bioorg Med Chem Lett, 21 (10): 2836-9. [PMID:21507640]

18. Guay D, Beaulieu C, Belley M, Crane SN, DeLuca J, Gareau Y, Hamel M, Henault M, Hyjazie H, Kargman S et al.. (2011) Synthesis and SAR of pyrimidine-based, non-nucleotide P2Y14 receptor antagonists. Bioorg Med Chem Lett, 21 (10): 2832-5. [PMID:21507642]

19. Hamel M, Henault M, Hyjazie H, Morin N, Bayly C, Skorey K, Therien AG, Mancini J, Brideau C, Kargman S. (2011) Discovery of novel P2Y14 agonist and antagonist using conventional and nonconventional methods. J Biomol Screen, 16 (9): 1098-105. [PMID:21821827]

20. Ivanov AA, Fricks I, Kendall Harden T, Jacobson KA. (2007) Molecular dynamics simulation of the P2Y14 receptor. Ligand docking and identification of a putative binding site of the distal hexose moiety. Bioorg Med Chem Lett, 17: 761-766. [PMID:17088057]

21. Jacobson KA, Deflorian F, Mishra S, Costanzi S. (2011) Pharmacochemistry of the platelet purinergic receptors. Purinergic Signal, 7 (3): 305-24. [PMID:21484092]

22. Kiselev E, Balasubramanian R, Uliassi E, Brown KA, Trujillo K, Katritch V, Hammes E, Stevens RC, Harden TK, Jacobson KA. (2015) Design, synthesis, pharmacological characterization of a fluorescent agonist of the P2Y₁₄ receptor. Bioorg Med Chem Lett, 25 (21): 4733-9. [PMID:26303895]

23. Kiselev E, Barrett MO, Katritch V, Paoletta S, Weitzer CD, Brown KA, Hammes E, Yin AL, Zhao Q, Stevens RC et al.. (2014) Exploring a 2-naphthoic acid template for the structure-based design of P2Y14 receptor antagonist molecular probes. ACS Chem Biol, 9 (12): 2833-42. [PMID:25299434]

24. Ko H, Fricks I, Ivanov AA, Harden TK, Jacobson KA. (2007) Structure-activity relationship of uridine 5'-diphosphoglucose analogues as agonists of the human P2Y14 receptor. J Med Chem, 50 (9): 2030-9. [PMID:17407275]

25. Kobayashi K, Yamanaka H, Yanamoto F, Okubo M, Noguchi K. (2012) Multiple P2Y subtypes in spinal microglia are involved in neuropathic pain after peripheral nerve injury. Glia, 60 (10): 1529-39. [PMID:22736439]

26. Krzemiński P, Pomorski P, Barańska J. (2008) The P2Y14 receptor activity in glioma C6 cells. Eur J Pharmacol, 594 (1-3): 49-54. [PMID:18638471]

27. Lee BC, Cheng T, Adams GB, Attar EC, Miura N, Lee SB, Saito Y, Olszak I, Dombkowski D, Olson DP et al.. (2003) P2Y-like receptor, GPR105 (P2Y14), identifies and mediates chemotaxis of bone-marrow hematopoietic stem cells. Genes Dev, 17 (13): 1592-604. [PMID:12842911]

28. Liu W, Mao S, Wang Y, Wang M, Li M, Sun M, Yao Y, Song C, Duan Y. (2024) Discovery of N-Substituted Acetamide Derivatives as Promising P2Y14R Antagonists Using Molecular Hybridization Based on Crystallographic Overlay. J Med Chem, 67 (12): 10233-10247. [PMID:38874515]

29. Malin SA, Molliver DC. (2010) Gi- and Gq-coupled ADP (P2Y) receptors act in opposition to modulate nociceptive signaling and inflammatory pain behavior. Mol Pain, 6: 21. [PMID:20398327]

30. Moore DJ, Murdock PR, Watson JM, Faull RL, Waldvogel HJ, Szekeres PG, Wilson S, Freeman KB, Emson PC. (2003) GPR105, a novel Gi/o-coupled UDP-glucose receptor expressed on brain glia and peripheral immune cells, is regulated by immunologic challenge: possible role in neuroimmune function. Brain Res Mol Brain Res, 118 (1-2): 10-23. [PMID:14559350]

31. Mufti F, Jung YH, Giancotti LA, Yu J, Chen Z, Phung NB, Jacobson KA, Salvemini D. (2020) P2Y14 Receptor Antagonists Reverse Chronic Neuropathic Pain in a Mouse Model. ACS Med Chem Lett, 11 (6): 1281-1286. [PMID:32551012]

32. Müller T, Bayer H, Myrtek D, Ferrari D, Sorichter S, Ziegenhagen MW, Zissel G, Virchow Jr JC, Luttmann W, Norgauer J et al.. (2005) The P2Y14 receptor of airway epithelial cells: coupling to intracellular Ca2+ and IL-8 secretion. Am J Respir Cell Mol Biol, 33 (6): 601-9. [PMID:16109883]

33. Nomura N, Miyajima N, Sazuka T, Tanaka A, Kawarabayasi Y, Sato S, Nagase T, Seki N, Ishikawa K, Tabata S. (1994) Prediction of the coding sequences of unidentified human genes. I. The coding sequences of 40 new genes (KIAA0001-KIAA0040) deduced by analysis of randomly sampled cDNA clones from human immature myeloid cell line KG-1. DNA Res, 1 (1): 27-35. [PMID:7584026]

34. Robichaud J, Fournier JF, Gagné S, Gauthier JY, Hamel M, Han Y, Hénault M, Kargman S, Levesque JF, Mamane Y et al.. (2011) Applying the pro-drug approach to afford highly bioavailable antagonists of P2Y(14). Bioorg Med Chem Lett, 21 (14): 4366-8. [PMID:21689930]

35. Scrivens M, Dickenson JM. (2005) Functional expression of the P2Y14 receptor in murine T-lymphocytes. Br J Pharmacol, 146 (3): 435-44. [PMID:15997228]

36. Scrivens M, Dickenson JM. (2006) Functional expression of the P2Y14 receptor in human neutrophils. Eur J Pharmacol, 543 (1-3): 166-73. [PMID:16820147]

37. Sesma JI, Kreda SM, Steinckwich-Besancon N, Dang H, García-Mata R, Harden TK, Lazarowski ER. (2012) The UDP-sugar-sensing P2Y(14) receptor promotes Rho-mediated signaling and chemotaxis in human neutrophils. Am J Physiol, Cell Physiol, 303 (5): C490-8. [PMID:22673622]

38. Skelton L, Cooper M, Murphy M, Platt A. (2003) Human immature monocyte-derived dendritic cells express the G protein-coupled receptor GPR105 (KIAA0001, P2Y14) and increase intracellular calcium in response to its agonist, uridine diphosphoglucose. J Immunol, 171 (4): 1941-9. [PMID:12902497]

39. Xu J, Morinaga H, Oh D, Li P, Chen A, Talukdar S, Mamane Y, Mancini JA, Nawrocki AR, Lazarowski E et al.. (2012) GPR105 ablation prevents inflammation and improves insulin sensitivity in mice with diet-induced obesity. J Immunol, 189 (4): 1992-9. [PMID:22778393]

40. Yu J, Ciancetta A, Dudas S, Duca S, Lottermoser J, Jacobson KA. (2018) Structure-Guided Modification of Heterocyclic Antagonists of the P2Y14 Receptor. J Med Chem, 61 (11): 4860-4882. DOI: 10.1021/acs.jmedchem.8b00168 [PMID:29767967]

41. Zippel N, Limbach CA, Ratajski N, Urban C, Luparello C, Pansky A, Kassack MU, Tobiasch E. (2012) Purinergic receptors influence the differentiation of human mesenchymal stem cells. Stem Cells Dev, 21 (6): 884-900. [PMID:21740266]

Contributors

Show »

How to cite this page