Target Information

Target General Infomation
Target ID
T49072
Former ID
TTDR00562
Target Name
Urotensin II receptor
Gene Name
UTS2R
Synonyms
G protein coupled receptor 14; UR-II-R; Urotensin-II receptor GPR14; UTS2R
Target Type
Clinical Trial
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.
BioChemical Class
GPCR rhodopsin
Target Validation
T49072
UniProt ID
Q9UKP6
Sequence
MALTPESPSSFPGLAATGSSVPEPPGGPNATLNSSWASPTEPSSLEDLVATGTIGTLLSA
MGVVGVVGNAYTLVVTCRSLRAVASMYVYVVNLALADLLYLLSIPFIVATYVTKEWHFGD
VGCRVLFGLDFLTMHASIFTLTVMSSERYAAVLRPLDTVQRPKGYRKLLALGTWLLALLL
TLPVMLAMRLVRRGPKSLCLPAWGPRAHRAYLTLLFATSIAGPGLLIGLLYARLARAYRR
SQRASFKRARRPGARALRLVLGIVLLFWACFLPFWLWQLLAQYHQAPLAPRTARIVNYLT
TCLTYGNSCANPFLYTLLTRNYRDHLRGRVRGPGSGGGRGPVPSLQPRARFQRCSGRSLS
SCSPQPTDSLVLAPAAPARPAPEGPRAPA
Drugs and Mode of Action
Drug(s) GSK1440115 Drug Info Phase 1 Asthma [523601]
SB-436811 Drug Info Phase 1 Asthma [523601], [539371]
PALOSURAN Drug Info Discontinued in Phase 2 Renal failure [540453], [547241]
SAR101099 Drug Info Discontinued in Phase 1 Diabetic nephropathy [549207]
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
KEGG Pathway Neuroactive ligand-receptor interaction
Reactome Peptide ligand-binding receptors
G alpha (q) signalling events
WikiPathways Gastrin-CREB signalling pathway via PKC and MAPK
GPCR ligand binding
GPCR downstream signaling
GPCRs, Other
References
Ref 523601ClinicalTrials.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 547241Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014355)
Ref 549207Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800033702)
Ref 526316Identification 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 526843Identification 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 527493Isochromanone-based urotensin-II receptor agonists. Bioorg Med Chem. 2005 Apr 15;13(8):3057-68.
Ref 527752A 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 529514Bioorg 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 529558Bioorg 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 530177Novel and potent small-molecule urotensin II receptor agonists. Bioorg Med Chem. 2009 Jul 1;17(13):4657-65.
Ref 530360J 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 530610J Med Chem. 2010 Apr 8;53(7):2695-708.Urotensin-II receptor modulators as potential drugs.
Ref 543795(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: 365).
Ref 544303Effects of Urotensin II Receptor Antagonist, GSK1440115, in Asthma. Front Pharmacol. 2013; 4: 54.

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