Target Information
Target General Infomation | |||||
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Target ID |
T15497
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Former ID |
TTDR00673
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Target Name |
Prostaglandin E2 receptor, EP1 subtype
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Gene Name |
PTGER1
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Synonyms |
EP1 receptor; PGE receptor, EP1 subtype; Prostanoid EP1 receptor; PTGER1
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Target Type |
Clinical Trial
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Disease | Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89] | ||||
Pollakiuria [ICD10: R35] | |||||
Solid tumours [ICD9: 140-199, 210-229; ICD10: C00-D48] | |||||
Thrombosis [ICD9: 437.6, 453, 671.5, 671.9; ICD10: I80-I82] | |||||
Unspecified [ICD code not available] | |||||
Function |
Receptor for prostaglandin E2 (PGE2). The activity of this receptor is mediated by G(q) proteins which activate a phosphatidylinositol-calcium second messenger system. May play a role as an important modulator of renal function. Implicated the smooth muscle contractile response to PGE2 in various tissues.
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BioChemical Class |
GPCR rhodopsin
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Target Validation |
T15497
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UniProt ID | |||||
Sequence |
MSPCGPLNLSLAGEATTCAAPWVPNTSAVPPSGASPALPIFSMTLGAVSNLLALALLAQA
AGRLRRRRSAATFLLFVASLLATDLAGHVIPGALVLRLYTAGRAPAGGACHFLGGCMVFF GLCPLLLGCGMAVERCVGVTRPLLHAARVSVARARLALAAVAAVALAVALLPLARVGRYE LQYPGTWCFIGLGPPGGWRQALLAGLFASLGLVALLAALVCNTLSGLALLRARWRRRSRR PPPASGPDSRRRWGAHGPRSASASSASSIASASTFFGGSRSSGSARRARAHDVEMVGQLV GIMVVSCICWSPMLVLVALAVGGWSSTSLQRPLFLAVRLASWNQILDPWVYILLRQAVLR QLLRLLPPRAGAKGGPAGLGLTPSAWEASSLRSSRHSGLSHF |
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Drugs and Mode of Action | |||||
Drug(s) | LAROPIPRANT | Drug Info | Phase 4 | Discovery agent | [523049], [540312] |
AS-013 | Drug Info | Phase 3 | Thrombosis | [534768] | |
PGF2alpha | Drug Info | Clinical trial | Solid tumours | [532003] | |
ZD6416 | Drug Info | Discontinued in Phase 2 | Pain | [546664] | |
ONO-8130 | Drug Info | Terminated | Pollakiuria | [547730] | |
ONO-8711 | Drug Info | Terminated | Pain | [539222], [547210] | |
Agonist | 17-phenyl-omega-trinor-PGE2 | Drug Info | [534595] | ||
AS-013 | Drug Info | [534768] | |||
carbacyclin | Drug Info | [525673] | |||
cicaprost | Drug Info | [525673] | |||
cloprostenol | Drug Info | [526324] | |||
M&B 28767 | Drug Info | [534478] | |||
ONO-DI-004 | Drug Info | [525735] | |||
PGD2 | Drug Info | [526324] | |||
PGF2alpha | Drug Info | [534595] | |||
U46619 | Drug Info | [534595] | |||
ZK110841 | Drug Info | [526324] | |||
Antagonist | AH6809 | Drug Info | [534595] | ||
GW848687X | Drug Info | [528512] | |||
MF266-1 | Drug Info | [529322] | |||
ONO-8711 | Drug Info | [526227], [531635] | |||
ONO-8713 | Drug Info | [525601] | |||
SC-19220 | Drug Info | [534595] | |||
ZD6416 | Drug Info | [535665] | |||
Inhibitor | LAROPIPRANT | Drug Info | [528672] | ||
Modulator | ONO-8130 | Drug Info | [531389] | ||
SC-51322 | Drug Info | ||||
ZM 325802 | Drug Info | ||||
Pathways | |||||
KEGG Pathway | Calcium signaling pathway | ||||
Neuroactive ligand-receptor interaction | |||||
Pathways in cancer | |||||
PANTHER Pathway | PI3 kinase pathway | ||||
Reactome | Prostanoid ligand receptors | ||||
G alpha (q) signalling events | |||||
WikiPathways | Prostaglandin Synthesis and Regulation | ||||
GPCRs, Class A Rhodopsin-like | |||||
Gastrin-CREB signalling pathway via PKC and MAPK | |||||
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 534768 | Effect of lipo-pro-prostaglandin E1, AS-013 on rat inner ear microcirculatory thrombosis. Prostaglandins Leukot Essent Fatty Acids. 1998 Sep;59(3):203-7. | ||||
Ref 539222 | (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: 1920). | ||||
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 546664 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009543) | ||||
Ref 525601 | New class of biphenylene dibenzazocinones as potent ligands for the human EP1 prostanoid receptor. Bioorg Med Chem Lett. 1999 Sep 20;9(18):2699-704. | ||||
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 526227 | Chemopreventive effects of ONO-8711, a selective prostaglandin E receptor EP(1) antagonist, on breast cancer development. Carcinogenesis. 2001 Dec;22(12):2001-4. | ||||
Ref 526324 | Cloned human EP1 prostanoid receptor pharmacology characterized using radioligand binding techniques. J Pharm Pharmacol. 2002 Apr;54(4):539-47. | ||||
Ref 528512 | The discovery of 6-[2-(5-chloro-2-{[(2,4-difluorophenyl)methyl]oxy}phenyl)-1-cyclopenten-1-yl]-2-pyridinecarboxylic acid, GW848687X, a potent and selective prostaglandin EP1 receptor antagonist for the treatment of inflammatory pain. Bioorg Med Chem Lett. 2007 Jan 15;17(2):385-9. Epub 2006 Oct 20. | ||||
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 529322 | MF498 [N-{[4-(5,9-Diethoxy-6-oxo-6,8-dihydro-7H-pyrrolo[3,4-g]quinolin-7-yl)-3-methylbenzyl]sulfonyl}-2-(2-methoxyphenyl)acetamide], a selective E prostanoid receptor 4 antagonist, relieves joint inflammation and pain in rodent models of rheumatoid and osteoarthritis. J Pharmacol Exp Ther. 2008 May;325(2):425-34. | ||||
Ref 531389 | ONO-8130, a selective prostanoid EP1 receptor antagonist, relieves bladder pain in mice with cyclophosphamide-induced cystitis. Pain. 2011 Jun;152(6):1373-81. | ||||
Ref 531635 | Therapeutic target database update 2012: a resource for facilitating target-oriented drug discovery. Nucleic Acids Res. 2012 Jan;40(Database issue):D1128-36. | ||||
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. |
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