Target Information

Target General Infomation
Target ID
T93515
Former ID
TTDC00179
Target Name
P2Y purinoceptor 2
Gene Name
P2RY2
Synonyms
ATP receptor; Adenosine P2Y2 receptor; P2U nucleotide receptor; P2U purinoceptor 1; P2U receptor; P2U1; P2Y2; Purinergic receptor; P2RY2
Target Type
Clinical Trial
Disease Constipation [ICD9: 564; ICD10: K59.0]
Cystic fibrosis [ICD9: 277; ICD10: E84]
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.
BioChemical Class
GPCR rhodopsin
Target Validation
T93515
UniProt ID
P41231
Sequence
MAADLGPWNDTINGTWDGDELGYRCRFNEDFKYVLLPVSYGVVCVPGLCLNAVALYIFLC
RLKTWNASTTYMFHLAVSDALYAASLPLLVYYYARGDHWPFSTVLCKLVRFLFYTNLYCS
ILFLTCISVHRCLGVLRPLRSLRWGRARYARRVAGAVWVLVLACQAPVLYFVTTSARGGR
VTCHDTSAPELFSRFVAYSSVMLGLLFAVPFAVILVCYVLMARRLLKPAYGTSGGLPRAK
RKSVRTIAVVLAVFALCFLPFHVTRTLYYSFRSLDLSCHTLNAINMAYKVTRPLASANSC
LDPVLYFLAGQRLVRFARDAKPPTGPSPATPARRRLGLRRSDRTDMQRIEDVLGSSEDSR
RTESTPAGSENTKDIRL
Drugs and Mode of Action
Drug(s) Diquafosol Drug Info Phase 3 Dry eye disease [536223], [539088]
INS-37217 Drug Info Phase 2 Cystic fibrosis [536223], [539089]
INS 316 Drug Info Discontinued in Phase 3 Lung cancer [546461]
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 536223Emerging 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 539089(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: 1737).
Ref 546461Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008257)
Ref 526114Safety 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 526232Methanocarba 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 527128Nucleotide-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 528028P2 receptors activated by uracil nucleotides--an update. Curr Med Chem. 2006;13(3):289-312.
Ref 528542Synthesis 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 528677Molecular 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 529152Bioorg 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 529505Synthesis 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 530711J 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 531402Structural 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 534088Pharmacological selectivity of the cloned human P2U-purinoceptor: potent activation by diadenosine tetraphosphate. Br J Pharmacol. 1995 Sep;116(1):1619-27.
Ref 535089P2Y(2) receptor stimulation increases tear fluid secretion in rabbits. Curr Eye Res. 2000 Oct;21(4):782-7.
Ref 536223Emerging drugs for the treatment of chronic obstructive pulmonary disease. Expert Opin Emerg Drugs. 2006 May;11(2):275-91.
Ref 543770(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. (Target id: 324).

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