Target Information

Target General Infomation
Target ID
T15497 (Former ID: TTDR00673)
Target Name
Prostaglandin E2 receptor EP1 (PTGER1)
Synonyms
Prostanoid EP1 receptor; Prostaglandin E2 receptor EP1 subtype; PGE2 receptor EP1 subtype; PGE receptor, EP1 subtype; PGE receptor EP1 subtype; EP1 receptor
Gene Name
PTGER1
Target Type
Clinical trial target
 [1]
Disease [+] 1 Target-related Diseases +
1 Thrombosis [ICD-11: DB61-GB90]
Function
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. Receptor for prostaglandin E2 (PGE2).
BioChemical Class
GPCR rhodopsin
UniProt ID
PE2R1_HUMAN
Sequence
MSPCGPLNLSLAGEATTCAAPWVPNTSAVPPSGASPALPIFSMTLGAVSNLLALALLAQA
AGRLRRRRSAATFLLFVASLLATDLAGHVIPGALVLRLYTAGRAPAGGACHFLGGCMVFF
GLCPLLLGCGMAVERCVGVTRPLLHAARVSVARARLALAAVAAVALAVALLPLARVGRYE
LQYPGTWCFIGLGPPGGWRQALLAGLFASLGLVALLAALVCNTLSGLALLRARWRRRSRR
PPPASGPDSRRRWGAHGPRSASASSASSIASASTFFGGSRSSGSARRARAHDVEMVGQLV
GIMVVSCICWSPMLVLVALAVGGWSSTSLQRPLFLAVRLASWNQILDPWVYILLRQAVLR
QLLRLLPPRAGAKGGPAGLGLTPSAWEASSLRSSRHSGLSHF
Drugs and Modes of Action
Clinical Trial Drug(s) [+] 2 Clinical Trial Drugs +
1 AS-013 Drug Info Phase 3 Thrombosis [2]
2 PGF2alpha Drug Info Clinical trial Solid tumour/cancer [3]
Discontinued Drug(s) [+] 3 Discontinued Drugs +
1 ZD6416 Drug Info Discontinued in Phase 2 Pain [4]
2 ONO-8130 Drug Info Terminated Pollakiuria [5]
3 ONO-8711 Drug Info Terminated Pain [6], [7]
Mode of Action [+] 3 Modes of Action +
Agonist [+] 11 Agonist drugs +
1 AS-013 Drug Info [2]
2 PGF2alpha Drug Info [8]
3 17-phenyl-omega-trinor-PGE2 Drug Info [8]
4 carbacyclin Drug Info [13]
5 cicaprost Drug Info [13]
6 cloprostenol Drug Info [14]
7 M&B 28767 Drug Info [16]
8 ONO-DI-004 Drug Info [19]
9 PGD2 Drug Info [14]
10 U46619 Drug Info [8]
11 ZK110841 Drug Info [14]
Antagonist [+] 8 Antagonist drugs +
1 BUTAPROST Drug Info [1]
2 ZD6416 Drug Info [9]
3 ONO-8711 Drug Info [11], [12]
4 AH6809 Drug Info [8]
5 GW848687X Drug Info [15]
6 MF266-1 Drug Info [17]
7 ONO-8713 Drug Info [18]
8 SC-19220 Drug Info [8]
Modulator [+] 3 Modulator drugs +
1 ONO-8130 Drug Info [10]
2 SC-51322 Drug Info [20]
3 ZM 325802 Drug Info [21]
Target Affiliated Biological Pathways
KEGG Pathway [+] 3 KEGG Pathways +
1 Calcium signaling pathway
2 Neuroactive ligand-receptor interaction
3 Pathways in cancer
Panther Pathway [+] 1 Panther Pathways +
1 PI3 kinase pathway
Reactome [+] 2 Reactome Pathways +
1 Prostanoid ligand receptors
2 G alpha (q) signalling events
WikiPathways [+] 6 WikiPathways +
1 Prostaglandin Synthesis and Regulation
2 GPCRs, Class A Rhodopsin-like
3 Gastrin-CREB signalling pathway via PKC and MAPK
4 Small Ligand GPCRs
5 GPCR ligand binding
6 GPCR downstream signaling
Target-Related Models and Studies
Target Validation
Target Validation Info 
References
REF 1 Evaluation of WO 2012/177618 A1 and US-2014/0179750 A1: novel small molecule antagonists of prostaglandin-E2 receptor EP2.Expert Opin Ther Pat. 2015 Jul;25(7):837-44.
REF 2 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 3 Stereocontrolled organocatalytic synthesis of prostaglandin PGF2alpha in seven steps. Nature. 2012 Sep 13;489(7415):278-81.
REF 4 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 5 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018852)
REF 6 URL: 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 7 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014044)
REF 8 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 9 The prostaglandin E2 receptor-1 (EP-1) mediates acid-induced visceral pain hypersensitivity in humans. Gastroenterology. 2003 Jan;124(1):18-25.
REF 10 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 11 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 12 Therapeutic target database update 2012: a resource for facilitating target-oriented drug discovery. Nucleic Acids Res. 2012 Jan;40(Database issue):D1128-36.
REF 13 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 14 Cloned human EP1 prostanoid receptor pharmacology characterized using radioligand binding techniques. J Pharm Pharmacol. 2002 Apr;54(4):539-47.
REF 15 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 s... Bioorg Med Chem Lett. 2007 Jan 15;17(2):385-9.
REF 16 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 17 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 18 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 19 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 20 Antihypertensive effects of selective prostaglandin E2 receptor subtype 1 targeting. J Clin Invest. 2007 Sep;117(9):2496-505.
REF 21 Characterization of the prostanoid receptor types involved in mediating calcitonin gene-related peptide release from cultured rat trigeminal neurones. Br J Pharmacol. 2001 Nov;134(6):1296-302.

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