Target Information
Target General Infomation | |||||
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Target ID |
T85467
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Former ID |
TTDC00037
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Target Name |
Prostaglandin E2 receptor EP3 subtype
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Gene Name |
PTGER3
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Synonyms |
PGE receptor, EP3 subtype; PGE2-R; Prostanoid EP3 receptor; PTGER3
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Target Type |
Clinical Trial
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Disease | Asthma [ICD10: J45] | ||||
Glaucoma [ICD9: 365; ICD10: H40-H42] | |||||
Peripheral vascular disease [ICD9: 443.9; ICD10: I73.9] | |||||
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89] | |||||
Solid tumours [ICD9: 140-199, 210-229; ICD10: C00-D48] | |||||
BioChemical Class |
GPCR rhodopsin
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Target Validation |
T85467
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UniProt ID | |||||
Sequence |
MKETRGYGGDAPFCTRLNHSYTGMWAPERSAEARGNLTRPPGSGEDCGSVSVAFPITMLL
TGFVGNALAMLLVSRSYRRRESKRKKSFLLCIGWLALTDLVGQLLTTPVVIVVYLSKQRW EHIDPSGRLCTFFGLTMTVFGLSSLFIASAMAVERALAIRAPHWYASHMKTRATRAVLLG VWLAVLAFALLPVLGVGQYTVQWPGTWCFISTGRGGNGTSSSHNWGNLFFASAFAFLGLL ALTVTFSCNLATIKALVSRCRAKATASQSSAQWGRITTETAIQLMGIMCVLSVCWSPLLI MMLKMIFNQTSVEHCKTHTEKQKECNFFLIAVRLASLNQILDPWVYLLLRKILLRKFCQI RYHTNNYASSSTSLPCQCSSTLMWSDHLER |
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Drugs and Mode of Action | |||||
Drug(s) | LAROPIPRANT | Drug Info | Phase 4 | Discovery agent | [523049], [540312] |
ONO-9054 | Drug Info | Phase 2 | Glaucoma | [533184] | |
PGF2alpha | Drug Info | Clinical trial | Solid tumours | [532003] | |
DG041 | Drug Info | Discontinued in Phase 2 | Peripheral vascular disease | [541141], [547397] | |
GR-63799X | Drug Info | Discontinued in Phase 1 | Asthma | [539236], [545501] | |
Agonist | 11-deoxy-PGE1 | Drug Info | [534595] | ||
16,16-dimethyl-PGE2 | Drug Info | [534478] | |||
17-phenyl-omega-trinor-PGE2 | Drug Info | [534478] | |||
butaprost (free acid form) | Drug Info | [525673] | |||
carbacyclin | Drug Info | [534478] | |||
cicaprost | Drug Info | [534478] | |||
cloprostenol | Drug Info | [525673] | |||
fluprostenol | Drug Info | [525673] | |||
I-BOP | Drug Info | [534478] | |||
isocarbacyclin | Drug Info | [534478] | |||
M&B 28767 | Drug Info | [534478] | |||
ONO-8713 | Drug Info | [534595] | |||
ONO-AE-248 | Drug Info | [525582] | |||
ONO-AE1-329 | Drug Info | [525735] | |||
ONO-AP-324 | Drug Info | [534778] | |||
PGD2 | Drug Info | [534595] | |||
PGF2alpha | Drug Info | [534478] | |||
SC46275 | Drug Info | [528220] | |||
STA2 | Drug Info | [534478] | |||
U46619 | Drug Info | [525673] | |||
Inhibitor | 3-(2-((E)-3-phenylprop-1-enyl)phenyl)acrylic acid | Drug Info | [528393] | ||
3-(2-(4-methoxycinnamyl)phenyl)acrylic acid | Drug Info | [528393] | |||
3-(2-(naphthalen-2-ylmethyl)phenyl)acrylic acid | Drug Info | [528393] | |||
3-(2-cinnamylphenyl)acrylic acid | Drug Info | [528393] | |||
FR-181157 | Drug Info | [527579] | |||
LAROPIPRANT | Drug Info | [528672] | |||
Antagonist | AH6809 | Drug Info | [525673] | ||
DG041 | Drug Info | [536080], [536517] | |||
L-798,106 | Drug Info | [530182] | |||
L-826266 | Drug Info | [531234] | |||
Molecule 21 | Drug Info | [543779] | |||
ONO-AE2-227 | Drug Info | [526239] | |||
ONO-AE3-208 | Drug Info | [526303] | |||
ONO-AE3-240 | Drug Info | [526517] | |||
ONO-AE5-599 | Drug Info | [528849] | |||
Modulator | GR-63799X | Drug Info | [525462] | ||
ONO-9054 | Drug Info | [533184] | |||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
KEGG Pathway | Calcium signaling pathway | ||||
cAMP signaling pathway | |||||
Neuroactive ligand-receptor interaction | |||||
Regulation of lipolysis in adipocytes | |||||
Pathways in cancer | |||||
NetPath Pathway | IL2 Signaling Pathway | ||||
Reactome | Prostanoid ligand receptors | ||||
G alpha (i) signalling events | |||||
WikiPathways | Prostaglandin Synthesis and Regulation | ||||
GPCRs, Class A Rhodopsin-like | |||||
Small Ligand GPCRs | |||||
GPCR ligand binding | |||||
GPCR downstream signaling | |||||
References | |||||
Ref 523049 | ClinicalTrials.gov (NCT01126073) Niacin/Laropiprant and Endothelial Function. U.S. National Institutes of Health. | ||||
Ref 532003 | Stereocontrolled organocatalytic synthesis of prostaglandin PGF2alpha in seven steps. Nature. 2012 Sep 13;489(7415):278-81. | ||||
Ref 533184 | IOP-Lowering Effect of ONO-9054, A Novel Dual Agonist of Prostanoid EP3 and FP Receptors, in Monkeys. Invest Ophthalmol Vis Sci. 2015 Apr;56(4):2547-52. | ||||
Ref 539236 | (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: 1937). | ||||
Ref 540312 | (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: 3356). | ||||
Ref 541141 | (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: 5822). | ||||
Ref 525462 | Effects of the prostanoid EP3-receptor agonists M&B 28767 and GR 63799X on infarct size caused by regional myocardial ischaemia in the anaesthetized rat. Br J Pharmacol. 1999 Feb;126(4):849-58. | ||||
Ref 525582 | Selective activation of the prostanoid EP(3) receptor reduces myocardial infarct size in rodents. Arterioscler Thromb Vasc Biol. 1999 Sep;19(9):2141-7. | ||||
Ref 525673 | The utilization of recombinant prostanoid receptors to determine the affinities and selectivities of prostaglandins and related analogs. Biochim Biophys Acta. 2000 Jan 17;1483(2):285-93. | ||||
Ref 525735 | The role of prostaglandin E receptor subtypes (EP1, EP2, EP3, and EP4) in bone resorption: an analysis using specific agonists for the respective EPs. Endocrinology. 2000 Apr;141(4):1554-9. | ||||
Ref 526239 | Involvement of prostaglandin E receptor subtype EP(4) in colon carcinogenesis. Cancer Res. 2002 Jan 1;62(1):28-32. | ||||
Ref 526303 | The prostaglandin receptor EP4 suppresses colitis, mucosal damage and CD4 cell activation in the gut. J Clin Invest. 2002 Apr;109(7):883-93. | ||||
Ref 526517 | Host prostaglandin E(2)-EP3 signaling regulates tumor-associated angiogenesis and tumor growth. J Exp Med. 2003 Jan 20;197(2):221-32. | ||||
Ref 527579 | Bioorg Med Chem Lett. 2005 Jul 1;15(13):3284-7.Metabolism investigation leading to novel drug design: orally active prostacyclin mimetics. Part 4. | ||||
Ref 528220 | Investigation of the pronounced synergism between prostaglandin E2 and other constrictor agents on rat femoral artery. Prostaglandins Leukot Essent Fatty Acids. 2006 Jun;74(6):401-15. | ||||
Ref 528393 | Bioorg Med Chem Lett. 2006 Nov 1;16(21):5639-42. Epub 2006 Aug 22.Comparison between two classes of selective EP(3) antagonists and their biological activities. | ||||
Ref 528672 | J Med Chem. 2007 Feb 22;50(4):794-806.Discovery of a potent and selective prostaglandin D2 receptor antagonist, [(3R)-4-(4-chloro-benzyl)-7-fluoro-5-(methylsulfonyl)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl]-acetic acid (MK-0524). | ||||
Ref 528849 | Involvement of prostaglandin E receptor EP3 subtype in duodenal bicarbonate secretion in rats. Life Sci. 2007 Jun 6;80(26):2446-53. Epub 2007 Apr 21. | ||||
Ref 530182 | Dual modulation of urinary bladder activity and urine flow by prostanoid EP3 receptors in the conscious rat. Br J Pharmacol. 2009 Sep;158(1):372-81. | ||||
Ref 531234 | Roles of affinity and lipophilicity in the slow kinetics of prostanoid receptor antagonists on isolated smooth muscle preparations. Br J Pharmacol. 2011 Feb;162(4):863-79. | ||||
Ref 533184 | IOP-Lowering Effect of ONO-9054, A Novel Dual Agonist of Prostanoid EP3 and FP Receptors, in Monkeys. Invest Ophthalmol Vis Sci. 2015 Apr;56(4):2547-52. | ||||
Ref 534478 | Ligand binding specificities of the eight types and subtypes of the mouse prostanoid receptors expressed in Chinese hamster ovary cells. Br J Pharmacol. 1997 Sep;122(2):217-24. | ||||
Ref 534595 | Molecular cloning and characterization of the four rat prostaglandin E2 prostanoid receptor subtypes. Eur J Pharmacol. 1997 Dec 11;340(2-3):227-41. | ||||
Ref 534778 | Characterization of a prostanoid EP3-receptor in guinea-pig aorta: partial agonist action of the non-prostanoid ONO-AP-324. Br J Pharmacol. 1998 Nov;125(6):1288-96. | ||||
Ref 536080 | Effects of a 5-lipoxygenase-activating protein inhibitor on biomarkers associated with risk of myocardial infarction: a randomized trial. JAMA. 2005 May 11;293(18):2245-56. |
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