Target Information
Target General Infomation | |||||
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Target ID |
T49072
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Former ID |
TTDR00562
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Target Name |
Urotensin II receptor
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Gene Name |
UTS2R
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Synonyms |
G protein coupled receptor 14; UR-II-R; Urotensin-II receptor GPR14; UTS2R
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Target Type |
Clinical Trial
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Disease | Asthma [ICD10: J45] | ||||
Diabetic nephropathy [ICD9: 250.4; ICD10: E11.21] | |||||
Renal failure [ICD9: 584, 585; ICD10: N17, N18, N19] | |||||
Function |
High affinity receptor for urotensin-2 and urotensin-2B. The activity of this receptor is mediated by a G-protein that activate a phosphatidylinositol-calcium second messenger system.
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BioChemical Class |
GPCR rhodopsin
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Target Validation |
T49072
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UniProt ID | |||||
Sequence |
MALTPESPSSFPGLAATGSSVPEPPGGPNATLNSSWASPTEPSSLEDLVATGTIGTLLSA
MGVVGVVGNAYTLVVTCRSLRAVASMYVYVVNLALADLLYLLSIPFIVATYVTKEWHFGD VGCRVLFGLDFLTMHASIFTLTVMSSERYAAVLRPLDTVQRPKGYRKLLALGTWLLALLL TLPVMLAMRLVRRGPKSLCLPAWGPRAHRAYLTLLFATSIAGPGLLIGLLYARLARAYRR SQRASFKRARRPGARALRLVLGIVLLFWACFLPFWLWQLLAQYHQAPLAPRTARIVNYLT TCLTYGNSCANPFLYTLLTRNYRDHLRGRVRGPGSGGGRGPVPSLQPRARFQRCSGRSLS SCSPQPTDSLVLAPAAPARPAPEGPRAPA |
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Drugs and Mode of Action | |||||
Agonist | AC-7954 | Drug Info | [527493] | ||
FL104 | Drug Info | [530177] | |||
urotensin II-related peptide | Drug Info | [526843] | |||
Inhibitor | Ac-FWKY-NH2 | Drug Info | [530610] | ||
Ac-SFWKYS-NH2 | Drug Info | [530610] | |||
Ac-WKY-NH2 | Drug Info | [530610] | |||
Ac-[CFWKFC]-NH2 | Drug Info | [530610] | |||
Ac-[CFWkYC]-NH2 | Drug Info | [530610] | |||
AGTAD[CFWKYC]V | Drug Info | [530610] | |||
ICI-199441 | Drug Info | [529514] | |||
JNJ-28318706 | Drug Info | [530360] | |||
PALOSURAN | Drug Info | [530610] | |||
SB-328872 | Drug Info | [529558] | |||
SB-436811 | Drug Info | [530610] | |||
SB-706375 | Drug Info | [530610] | |||
Antagonist | GSK1440115 | Drug Info | [544303] | ||
S6716 | Drug Info | [526316] | |||
SAR101099 | Drug Info | [543795] | |||
SB-611812 | Drug Info | [527752] | |||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
References | |||||
Ref 523601 | ClinicalTrials.gov (NCT01424280) Single Dose Study of GSK1440115 in Patients With Asthma. U.S. National Institutes of Health. | ||||
Ref 539371 | (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: 2164). | ||||
Ref 540453 | (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: 3516). | ||||
Ref 526316 | Identification of nonpeptidic urotensin II receptor antagonists by virtual screening based on a pharmacophore model derived from structure-activity relationships and nuclear magnetic resonance studies on urotensin II. J Med Chem. 2002 Apr 25;45(9):1799-805. | ||||
Ref 526843 | Identification of urotensin II-related peptide as the urotensin II-immunoreactive molecule in the rat brain. Biochem Biophys Res Commun. 2003 Oct 24;310(3):860-8. | ||||
Ref 527493 | Isochromanone-based urotensin-II receptor agonists. Bioorg Med Chem. 2005 Apr 15;13(8):3057-68. | ||||
Ref 527752 | A role for urotensin II in restenosis following balloon angioplasty: use of a selective UT receptor blocker. J Mol Cell Cardiol. 2005 Nov;39(5):785-91. Epub 2005 Sep 19. | ||||
Ref 529514 | Bioorg Med Chem Lett. 2008 Jul 1;18(13):3716-9. Epub 2008 May 20.Potent and selective small-molecule human urotensin-II antagonists with improved pharmacokinetic profiles. | ||||
Ref 529558 | Bioorg Med Chem Lett. 2008 Jul 15;18(14):3950-4. Epub 2008 Jun 10.Urotensin-II receptor antagonists: synthesis and SAR of N-cyclic azaalkyl benzamides. | ||||
Ref 530177 | Novel and potent small-molecule urotensin II receptor agonists. Bioorg Med Chem. 2009 Jul 1;17(13):4657-65. | ||||
Ref 530360 | J Med Chem. 2009 Dec 10;52(23):7432-45.Nonpeptide urotensin-II receptor antagonists: a new ligand class based on piperazino-phthalimide and piperazino-isoindolinone subunits. | ||||
Ref 530610 | J Med Chem. 2010 Apr 8;53(7):2695-708.Urotensin-II receptor modulators as potential drugs. |
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