P2RY1

Purinergic receptor P2Y, G-protein coupled, 1

Available structures

Ortholog search: PDBe, RCSB

List of PDB id codes
1Y36, 4XNV, 4XNW

Identifiers

Symbols

P2RY1 ; P2Y1

External IDs

OMIM: 601167 MGI: 105049 HomoloGene: 1926 IUPHAR: 323 ChEMBL: 4315 GeneCards: P2RY1 Gene

Gene ontology
Molecular function	• receptor activity • protein binding • ATP binding • A1 adenosine receptor binding • ADP binding • G-protein coupled purinergic nucleotide receptor activity • ATP-activated adenosine receptor activity • ADP-activated adenosine receptor activity • protein heterodimerization activity • scaffold protein binding
Cellular component	• mitochondrion • cytosol • plasma membrane • integral component of plasma membrane • cell surface • basolateral plasma membrane • apical plasma membrane • dendrite • cell body • postsynaptic membrane • neuronal postsynaptic density
Biological process	• positive regulation of protein phosphorylation • adenosine receptor signaling pathway • cell surface receptor signaling pathway • G-protein coupled receptor signaling pathway • adenylate cyclase-inhibiting G-protein coupled receptor signaling pathway • phospholipase C-activating G-protein coupled receptor signaling pathway • positive regulation of cytosolic calcium ion concentration • aging • blood coagulation • glial cell migration • response to mechanical stimulus • regulation of receptor activity • negative regulation of norepinephrine secretion • sensory perception of pain • signal transduction involved in regulation of gene expression • platelet activation • positive regulation of inositol trisphosphate biosynthetic process • G-protein coupled purinergic nucleotide receptor signaling pathway • regulation of vasodilation • eating behavior • positive regulation of ion transport • positive regulation of transcription from RNA polymerase II promoter • positive regulation of hormone secretion • negative regulation of binding • positive regulation of penile erection • positive regulation of ERK1 and ERK2 cascade • response to growth factor • cellular response to organic cyclic compound • protein localization to plasma membrane • relaxation of muscle
Sources: Amigo / QuickGO

RNA expression pattern

More reference expression data

Orthologs

Species

Human

Mouse

RefSeq (mRNA)

RefSeq (protein)

Location (UCSC)

Chr 3:
152.83 – 152.84 Mb

Chr 3:
61 – 61.01 Mb

PubMed search

P2Y purinoceptor 1 is a protein that in humans is encoded by the P2RY1 gene.^[1]

The product of this gene, P2Y₁ belongs to the family of G-protein coupled receptors. This family has several receptor subtypes with different pharmacological selectivity, which overlaps in some cases, for various adenosine and uridine nucleotides. This receptor functions as a receptor for extracellular ATP and ADP. In platelets binding to ADP leads to mobilization of intracellular calcium ions via activation of phospholipase C, a change in platelet shape, and probably to platelet aggregation.^[2]

References

↑ Ayyanathan K, Webbs TE, Sandhu AK, Athwal RS, Barnard EA, Kunapuli SP (Mar 1996). "Cloning and chromosomal localization of the human P2Y1 purinoceptor". Biochem Biophys Res Commun 218 (3): 783–788. doi:10.1006/bbrc.1996.0139. PMID 8579591.
↑ "Entrez Gene: P2RY1 purinergic receptor P2Y, G-protein coupled, 1".

External links

"P2Y Receptors: P2Y₁". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.

Janssens R, Communi D, Pirotton S, et al. (1996). "Cloning and tissue distribution of the human P2Y1 receptor". Biochem. Biophys. Res. Commun. 221 (3): 588–593. doi:10.1006/bbrc.1996.0640. PMID 8630005.
Léon C, Vial C, Cazenave JP, Gachet C (1996). "Cloning and sequencing of a human cDNA encoding endothelial P2Y1 purinoceptor". Gene 171 (2): 295–297. doi:10.1016/0378-1119(96)00027-3. PMID 8666290.
Léon C, Hechler B, Vial C, et al. (1997). "The P2Y1 receptor is an ADP receptor antagonized by ATP and expressed in platelets and megakaryoblastic cells". FEBS Lett. 403 (1): 26–30. doi:10.1016/S0014-5793(97)00022-7. PMID 9038354.
Ayyanathan K, Naylor SL, Kunapuli SP (1997). "Structural characterization and fine chromosomal mapping of the human P2Y1 purinergic receptor gene (P2RY1)". Somat. Cell Mol. Genet. 22 (5): 419–424. doi:10.1007/BF02369897. PMID 9039850.
Maier R, Glatz A, Mosbacher J, Bilbe G (1997). "Cloning of P2Y6 cDNAs and identification of a pseudogene: comparison of P2Y receptor subtype expression in bone and brain tissues". Biochem. Biophys. Res. Commun. 237 (2): 297–302. doi:10.1006/bbrc.1997.7135. PMID 9268704.
Jin J, Daniel JL, Kunapuli SP (1998). "Molecular basis for ADP-induced platelet activation. II. The P2Y1 receptor mediates ADP-induced intracellular calcium mobilization and shape change in platelets". J. Biol. Chem. 273 (4): 2030–2034. doi:10.1074/jbc.273.4.2030. PMID 9442040.
Hall RA, Ostedgaard LS, Premont RT, et al. (1998). "A C-terminal motif found in the beta2-adrenergic receptor, P2Y1 receptor and cystic fibrosis transmembrane conductance regulator determines binding to the Na+/H+ exchanger regulatory factor family of PDZ proteins". Proc. Natl. Acad. Sci. U.S.A. 95 (15): 8496–8501. doi:10.1073/pnas.95.15.8496. PMC 21104. PMID 9671706.
Sabala P, Czajkowski R, Przybyłek K, et al. (2001). "Two subtypes of G protein-coupled nucleotide receptors, P2Y(1) and P2Y(2) are involved in calcium signalling in glioma C6 cells". Br. J. Pharmacol. 132 (2): 393–402. doi:10.1038/sj.bjp.0703843. PMC 1572584. PMID 11159687.
Yoshioka K, Saitoh O, Nakata H (2001). "Heteromeric association creates a P2Y-like adenosine receptor". Proc. Natl. Acad. Sci. U.S.A. 98 (13): 7617–7622. doi:10.1073/pnas.121587098. PMC 34717. PMID 11390975.
James G, Butt AM (2001). "Changes in P2Y and P2X purinoceptors in reactive glia following axonal degeneration in the rat optic nerve". Neurosci. Lett. 312 (1): 33–36. doi:10.1016/S0304-3940(01)02189-9. PMID 11578839.
Moore DJ, Chambers JK, Wahlin JP, et al. (2001). "Expression pattern of human P2Y receptor subtypes: a quantitative reverse transcription-polymerase chain reaction study". Biochim. Biophys. Acta 1521 (1–3): 107–19. doi:10.1016/S0167-4781(01)00291-3. PMID 11690642.
Czajkowski R, Lei L, Sabała P, Barańska J (2002). "ADP-evoked phospholipase C stimulation and adenylyl cyclase inhibition in glioma C6 cells occur through two distinct nucleotide receptors, P2Y(1) and P2Y(12)". FEBS Lett. 513 (2–3): 179–183. doi:10.1016/S0014-5793(02)02255-X. PMID 11904146.
Aktas B, Hönig-Liedl P, Walter U, Geiger J (2002). "Inhibition of platelet P2Y12 and alpha2A receptor signaling by cGMP-dependent protein kinase". Biochem. Pharmacol. 64 (3): 433–439. doi:10.1016/S0006-2952(02)01113-9. PMID 12147294.
Nurden P, Poujol C, Winckler J, et al. (2003). "Immunolocalization of P2Y1 and TPalpha receptors in platelets showed a major pool associated with the membranes of alpha -granules and the open canalicular system". Blood 101 (4): 1400–1408. doi:10.1182/blood-2002-02-0642. PMID 12393588.
Strausberg RL, Feingold EA, Grouse LH, et al. (2003). "Generation and initial analysis of more than 15,000 full-length human and mouse cDNA sequences". Proc. Natl. Acad. Sci. U.S.A. 99 (26): 16899–16903. doi:10.1073/pnas.242603899. PMC 139241. PMID 12477932.
Burrell HE, Bowler WB, Gallagher JA, Sharpe GR (2003). "Human keratinocytes express multiple P2Y-receptors: evidence for functional P2Y1, P2Y2, and P2Y4 receptors". J. Invest. Dermatol. 120 (3): 440–447. doi:10.1046/j.1523-1747.2003.12050.x. PMID 12603858.
Jagroop IA, Burnstock G, Mikhailidis DP (2003). "Both the ADP receptors P2Y1 and P2Y12, play a role in controlling shape change in human platelets". Platelets 14 (1): 15–20. doi:10.1080/0953710021000062914. PMID 12623443.
Greig AV, Linge C, Terenghi G, et al. (2003). "Purinergic receptors are part of a functional signaling system for proliferation and differentiation of human epidermal keratinocytes". J. Invest. Dermatol. 120 (6): 1007–1015. doi:10.1046/j.1523-1747.2003.12261.x. PMID 12787128.
Wang L, Ostberg O, Wihlborg AK, et al. (2003). "Quantification of ADP and ATP receptor expression in human platelets". J. Thromb. Haemost. 1 (2): 330–336. doi:10.1046/j.1538-7836.2003.00070.x. PMID 12871508.

This article incorporates text from the United States National Library of Medicine, which is in the public domain.

Cell surface receptor: G protein-coupled receptors

Class A: Rhodopsin like

Neurotransmitter

Adrenergic	α1 (A B D) α2 (A B C) β1 β2 β3

Purinergic	Adenosine (A1 A2A A2B A3) P2Y (1 2 4 5 6 8 9 10 11 12 13 14)

Serotonin	(all but 5-HT3) 5-HT1 (A B D E F) 5-HT2 (A B C) 5-HT (4 5A 6 7)

Other	Acetylcholine (M1 M2 M3 M4 M5) Dopamine (D1 D2 D3 D4 D5) Histamine (H1 H2 H3 H4) Melatonin (1A 1B 1C) TAAR (1 2 3 5 6 8 9)

Metabolites and
signaling molecules

Eicosanoid	CysLT (1 2) LTB4 (1 2) FPRL1 OXE Prostaglandin (DP (1 2), EP (1 2 3 4), FP) Prostacyclin Thromboxane

Other	Bile acid Cannabinoid (CB1 CB2, GPR (18 55 119)) EBI2 Estrogen Free fatty acid (1 2 3 4) Lactate Lysophosphatidic acid (1 2 3 4 5 6) Lysophospholipid (1 2 3 4 5 6 7 8) Niacin (1 2) Oxoglutarate PAF Sphingosine-1-phosphate (1 2 3 4 5) Succinate

Peptide

Neuropeptide	B/W (1 2) FF (1 2) S Y (1 2 4 5) Neuromedin (B U (1 2)) Neurotensin (1 2)

Other	Anaphylatoxin (C3a C5a) Angiotensin (1 2) Apelin Bombesin (BRS3 GRPR NMBR) Bradykinin (B1 B2) Chemokine Cholecystokinin (A B) Endothelin (A B) Formyl peptide (1 2 3) FSH Galanin (1 2 3) GHB receptor Gonadotropin-releasing hormone (1 2) Ghrelin Kisspeptin Luteinizing hormone/choriogonadotropin MAS (1 1L D E F G X1 X2 X3 X4) Melanocortin (1 2 3 4 5) MCHR (1 2) Motilin Opioid (Delta Kappa Mu Nociceptin & Zeta, but not Sigma) Orexin (1 2) Oxytocin Prokineticin (1 2) Prolactin-releasing peptide Relaxin (1 2 3 4) Somatostatin (1 2 3 4 5) Tachykinin (1 2 3) Thyrotropin Thyrotropin-releasing hormone Urotensin-II Vasopressin (1A 1B 2)

Miscellaneous

Orphan	GPR (1 3 4 6 12 15 17 18 19 20 21 22 23 25 26 27 31 32 33 34 35 37 39 42 44 45 50 52 55 61 62 63 65 68 75 77 78 81 82 83 84 85 87 88 92 101 103 109A 109B 119 120 132 135 137B 139 141 142 146 148 149 150 151 152 153 160 161 162 171 173 174 176 177 182 183)

Other	Adrenomedullin Olfactory Opsin (3 4 5 1LW 1MW 1SW RGR RRH) Protease-activated (1 2 3 4) SREB (1 2 3)

Class B: Secretin like

Adhesion	ADGRG (1 2 3 4 5 6 7)

Orphan	GPR (56 64 97 98 110 111 112 113 114 115 116 123 124 125 126 128 133 143 144 155 157)

Other	Brain-specific angiogenesis inhibitor (1 2 3) Cadherin (1 2 3) Calcitonin CALCRL CD97 Corticotropin-releasing hormone (1 2) EMR (1 2 3) Glucagon (GR GIPR GLP1R GLP2R) Growth hormone releasing hormone PACAPR1 GPR Latrophilin (1 2 3 ELTD1) Methuselah-like proteins Parathyroid hormone (1 2) Secretin Vasoactive intestinal peptide (1 2)

Class C: Metabotropic glutamate / pheromone

Taste	TAS1R (1 2 3) TAS2R (1 3 4 5 7 8 9 10 13 14 16 19 20 30 31 38 39 40 41 42 43 45 46 50 60)

Other	Calcium-sensing receptor GABA B (1 2) Glutamate receptor (Metabotropic glutamate (1 2 3 4 5 6 7 8)) GPRC6A GPR (156 158 179) RAIG (1 2 3 4)

Class F: Frizzled / Smoothened

Frizzled	Frizzled (1 2 3 4 5 6 7 8 9 10)

Smoothened	Smoothened

Purinergics

Receptor
(ligands)

P0
(adenine)

Agonists: 8-Aminoadenine
Adenine

P1
(adenosine)

Agonists: 2-(1-Hexynyl)-N-methyladenosine
2-Cl-IB-MECA
2'-MeCCPA
4'-O-β-D-Glucosyl-9-O-(6''-deoxysaccharosyl)olivil
5'-N-ethylcarboxamidoadenosine
Adenosine
ADP
AMP
Apadenoson
ATL-146e
ATP
BAY 60–6583
Binodenoson
Capadenoson
CCPA
CGS-21680
CP-532,903
Evodenoson
GR 79236
LUF-5835
LUF-5845
N⁶-Cyclopentyladenosine
Neladenoson dalanate
Piclidenoson
Regadenoson
SDZ WAG 994
Selodenoson
Sonedenoson
Tecadenoson
UK-432,097

P2
(nucleotide)

P2X (ATP)	Agonists: 2-Me-SATP α,β-Me-ATP Adenosine ADP AMP Ap4A Ap5A ATP ATPγS BzATP Cibacron blue CTP D-β,γ-Me-ATP GTP HT-AMP Ivermectin L-β,γ-Me-ATP MRS-2219 PAPET-ATP UTP Zinc Antagonists: 5-BDBD A-317491 A-438079 A-740003 A-804598 A-839977 AF-353 AZ-10606120 AZ-11645373 BBG Calcium Calmidazolium Chelerythrine Copper Emodin (Rheum officinale) Evans Blue GW-791343 HMA Ip5I isoPPADS JNJ-47965567 KN-04 KN-62 Magnesium MRS-2159 NF-023 NF-110 NF-157 NF-279 NF-449 Oxidized-ATP Phenol Red Phenolphthalein PPADS PPNDS PSB-12062 Puerarin (Radix puerariae) Purotoxin 1 RB-2 Ro 0437626 Ro 51 RO-3 Sodium ferulate (Angelica sinensis, Ligusticum wallichii) Suramin TC-P 262 Tetramethylpyrazine (ligustrazine) (Ligusticum wallichii) TNP-ATP Zinc

P2Y	Agonists: 2-Me-SADP 2-Me-SATP 2-Thio-UTP 5-Br-UDP 5-OMe-UDP α,β-Me-ATP Adenosine ADP ADPβS Ap3A AR-C 67085MX ATP ATPγS CTP dATP Denufosol Diquafosol IDP ITP INS-365 INS-37217 MRS-2365 MRS-2690 MRS-2693 MRS-2768 MRS-2957 MRS-4062 NF-546 PAPET-ATP PSB-0474 PSB-1114 UDP UDPβS UDP-galactose UDP-glucose UDP-N-acetylglucosamine Up3U UTP UTPγS Antagonists: 2-Me-SAMP A3P5PS AMPαS Ap4A AR-C 66096 AR-C 67085MX AR-C 69931MX AR-C 118925XX ATP BzATP C1330-7 Cangrelor Clopidrogel Elinogrel Ip5I MRS-2179 MRS-2211 MRS-2279 MRS-2395 MRS-2500 MRS-2578 NF-157 NF-340 PIT PPADS Prasugrel PSB-0739 RB-2 Regrelor Suramin Ticagrelor Ticlopidine UDP

Transporter
(blockers)

CNTs	6-Hydroxy-7-methoxyflavone Adenosine dMeThPmR Estradiol KGO-2142 KGO-2173 MeThPmR Phloridzin Progesterone

ENTs	Barbiturates Benzodiazepines Cilostazol Dilazep Dipyridamole Estradiol Ethanol Hexobendine NBMPR Pentoxifylline Progesterone Propentofylline

PMAT	Decynium-22

Enzyme
(inhibitors)

XO	Allopurinol Amflutizole Benzbromarone Caffeic acid Cinnamaldehyde Cinnamomum osmophloeum Febuxostat Myo-inositol Kaempferol Myricetin Niraxostat Oxypurinol Phytic acid Pistacia integerrima Propolis Quercetin Tisopurine Topiroxostat

Others	Aminopterin Azathioprine Methotrexate Mycophenolic acid Pemetrexed Pralatrexate Many others

Others

Others: Chrysophanol (rhubarb)

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P2RY1

See also

References

External links

Further reading