Target Information
Target General Infomation | |||||
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Target ID |
T93515
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Former ID |
TTDC00179
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Target Name |
P2Y purinoceptor 2
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Gene Name |
P2RY2
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Synonyms |
ATP receptor; Adenosine P2Y2 receptor; P2U nucleotide receptor; P2U purinoceptor 1; P2U receptor; P2U1; P2Y2; Purinergic receptor; P2RY2
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Target Type |
Clinical Trial
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Disease | Cystic fibrosis [ICD9: 277; ICD10: E84] | ||||
Constipation [ICD9: 564; ICD10: K59.0] | |||||
Dry eye disease [ICD9: 370.33; ICD10: H16.229] | |||||
Lung cancer [ICD9: 162; ICD10: C33-C34] | |||||
Function |
Receptor for ATP and UTP coupled to G-proteins thatactivate a phosphatidylinositol-calcium second messenger system. The affinity range is UTP = ATP > ATP-gamma-S >> 2-methylthio-ATP = ADP.
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BioChemical Class |
GPCR rhodopsin
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Target Validation |
T93515
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UniProt ID | |||||
Sequence |
MAADLGPWNDTINGTWDGDELGYRCRFNEDFKYVLLPVSYGVVCVPGLCLNAVALYIFLC
RLKTWNASTTYMFHLAVSDALYAASLPLLVYYYARGDHWPFSTVLCKLVRFLFYTNLYCS ILFLTCISVHRCLGVLRPLRSLRWGRARYARRVAGAVWVLVLACQAPVLYFVTTSARGGR VTCHDTSAPELFSRFVAYSSVMLGLLFAVPFAVILVCYVLMARRLLKPAYGTSGGLPRAK RKSVRTIAVVLAVFALCFLPFHVTRTLYYSFRSLDLSCHTLNAINMAYKVTRPLASANSC LDPVLYFLAGQRLVRFARDAKPPTGPSPATPARRRLGLRRSDRTDMQRIEDVLGSSEDSR RTESTPAGSENTKDIRL |
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Drugs and Mode of Action | |||||
Agonist | 2-thioUTP | Drug Info | [528542] | ||
4-thio-UTP | Drug Info | [528028] | |||
5BrUTP | Drug Info | [534088] | |||
Diquafosol | Drug Info | [536223] | |||
INS-37217 | Drug Info | [536223] | |||
MDT-006 | Drug Info | [543770] | |||
MRS2698 | Drug Info | [528677] | |||
MRS2768 | Drug Info | [529505] | |||
PSB1114 | Drug Info | [531402] | |||
uridine triphosphate | Drug Info | [526232] | |||
UTP | Drug Info | [535089] | |||
UTPgammaS | Drug Info | [534088] | |||
Inhibitor | Acid blue 25 | Drug Info | [530711] | ||
PSB-0963 | Drug Info | [530711] | |||
PSB-716 | Drug Info | [529152] | |||
RB 2 | Drug Info | [529152] | |||
SB-416 | Drug Info | [529152] | |||
Antagonist | AR-C118925XX | Drug Info | [527128] | ||
AR-C126313 | Drug Info | [528677] | |||
Modulator | INS 316 | Drug Info | [526114] | ||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
KEGG Pathway | Neuroactive ligand-receptor interaction | ||||
Inflammatory mediator regulation of TRP channels | |||||
NetPath Pathway | IL5 Signaling Pathway | ||||
Reactome | G alpha (q) signalling events | ||||
P2Y receptors | |||||
Surfactant metabolism | |||||
WikiPathways | Nucleotide GPCRs | ||||
GPCRs, Class A Rhodopsin-like | |||||
Gastrin-CREB signalling pathway via PKC and MAPK | |||||
GPCR ligand binding | |||||
GPCR downstream signaling | |||||
References | |||||
Ref 536223 | Emerging drugs for the treatment of chronic obstructive pulmonary disease. Expert Opin Emerg Drugs. 2006 May;11(2):275-91. | ||||
Ref 539088 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1736). | ||||
Ref 526114 | Safety of aerosolized INS 365 in patients with mild to moderate cystic fibrosis: results of a phase I multi-center study. Pediatr Pulmonol. 2001 Aug;32(2):122-8. | ||||
Ref 526232 | Methanocarba modification of uracil and adenine nucleotides: high potency of Northern ring conformation at P2Y1, P2Y2, P2Y4, and P2Y11 but not P2Y6 receptors. J Med Chem. 2002 Jan 3;45(1):208-18. | ||||
Ref 527128 | Nucleotide-mediated mucin secretion from differentiated human bronchial epithelial cells. Am J Respir Cell Mol Biol. 2004 Oct;31(4):446-55. Epub 2004 Jul 1. | ||||
Ref 528028 | P2 receptors activated by uracil nucleotides--an update. Curr Med Chem. 2006;13(3):289-312. | ||||
Ref 528542 | Synthesis and structure-activity relationships of uracil nucleotide derivatives and analogues as agonists at human P2Y2, P2Y4, and P2Y6 receptors. J Med Chem. 2006 Nov 30;49(24):7076-87. | ||||
Ref 528677 | Molecular modeling of the human P2Y2 receptor and design of a selective agonist, 2'-amino-2'-deoxy-2-thiouridine 5'-triphosphate. J Med Chem. 2007 Mar 22;50(6):1166-76. Epub 2007 Feb 16. | ||||
Ref 529152 | Bioorg Med Chem Lett. 2008 Jan 1;18(1):223-7. Epub 2007 Oct 30.Combinatorial synthesis of anilinoanthraquinone derivatives and evaluation as non-nucleotide-derived P2Y2 receptor antagonists. | ||||
Ref 529505 | Synthesis and potency of novel uracil nucleotides and derivatives as P2Y2 and P2Y6 receptor agonists. Bioorg Med Chem. 2008 Jun 15;16(12):6319-32. | ||||
Ref 530711 | J Med Chem. 2010 Mar 11;53(5):2076-86.Development of potent and selective inhibitors of ecto-5'-nucleotidase based on an anthraquinone scaffold. | ||||
Ref 531402 | Structural modifications of UMP, UDP, and UTP leading to subtype-selective agonists for P2Y2, P2Y4, and P2Y6 receptors. J Med Chem. 2011 Apr 28;54(8):2878-90. | ||||
Ref 534088 | Pharmacological selectivity of the cloned human P2U-purinoceptor: potent activation by diadenosine tetraphosphate. Br J Pharmacol. 1995 Sep;116(1):1619-27. | ||||
Ref 535089 | P2Y(2) receptor stimulation increases tear fluid secretion in rabbits. Curr Eye Res. 2000 Oct;21(4):782-7. |
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