Target Information

Target General Infomation
Target ID
T15497
Former ID
TTDR00673
Target Name
Prostaglandin E2 receptor, EP1 subtype
Gene Name
PTGER1
Synonyms
EP1 receptor; PGE receptor, EP1 subtype; Prostanoid EP1 receptor; PTGER1
Target Type
Clinical Trial
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.
BioChemical Class
GPCR rhodopsin
Target Validation
T15497
UniProt ID
P34995
Sequence
MSPCGPLNLSLAGEATTCAAPWVPNTSAVPPSGASPALPIFSMTLGAVSNLLALALLAQA
AGRLRRRRSAATFLLFVASLLATDLAGHVIPGALVLRLYTAGRAPAGGACHFLGGCMVFF
GLCPLLLGCGMAVERCVGVTRPLLHAARVSVARARLALAAVAAVALAVALLPLARVGRYE
LQYPGTWCFIGLGPPGGWRQALLAGLFASLGLVALLAALVCNTLSGLALLRARWRRRSRR
PPPASGPDSRRRWGAHGPRSASASSASSIASASTFFGGSRSSGSARRARAHDVEMVGQLV
GIMVVSCICWSPMLVLVALAVGGWSSTSLQRPLFLAVRLASWNQILDPWVYILLRQAVLR
QLLRLLPPRAGAKGGPAGLGLTPSAWEASSLRSSRHSGLSHF
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 523049ClinicalTrials.gov (NCT01126073) Niacin/Laropiprant and Endothelial Function. U.S. National Institutes of Health.
Ref 532003Stereocontrolled organocatalytic synthesis of prostaglandin PGF2alpha in seven steps. Nature. 2012 Sep 13;489(7415):278-81.
Ref 534768Effect 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 546664Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009543)
Ref 547210Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014044)
Ref 547730Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018852)
Ref 525601New 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 525673The 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 525735The 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 526227Chemopreventive effects of ONO-8711, a selective prostaglandin E receptor EP(1) antagonist, on breast cancer development. Carcinogenesis. 2001 Dec;22(12):2001-4.
Ref 526324Cloned human EP1 prostanoid receptor pharmacology characterized using radioligand binding techniques. J Pharm Pharmacol. 2002 Apr;54(4):539-47.
Ref 528512The 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 528672J 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 529322MF498 [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 531389ONO-8130, a selective prostanoid EP1 receptor antagonist, relieves bladder pain in mice with cyclophosphamide-induced cystitis. Pain. 2011 Jun;152(6):1373-81.
Ref 531635Therapeutic target database update 2012: a resource for facilitating target-oriented drug discovery. Nucleic Acids Res. 2012 Jan;40(Database issue):D1128-36.
Ref 534478Ligand 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 534595Molecular cloning and characterization of the four rat prostaglandin E2 prostanoid receptor subtypes. Eur J Pharmacol. 1997 Dec 11;340(2-3):227-41.
Ref 534768Effect 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 535665The prostaglandin E2 receptor-1 (EP-1) mediates acid-induced visceral pain hypersensitivity in humans. Gastroenterology. 2003 Jan;124(1):18-25.

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