Target Information

Target General Infomation
Target ID
T85467
Former ID
TTDC00037
Target Name
Prostaglandin E2 receptor EP3 subtype
Gene Name
PTGER3
Synonyms
PGE receptor, EP3 subtype; PGE2-R; Prostanoid EP3 receptor; PTGER3
Target Type
Clinical Trial
Disease Asthma [ICD10: J45]
Glaucoma [ICD9: 365; ICD10: H40-H42]
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89]
Peripheral vascular disease [ICD9: 443.9; ICD10: I73.9]
Solid tumours [ICD9: 140-199, 210-229; ICD10: C00-D48]
BioChemical Class
GPCR rhodopsin
Target Validation
T85467
UniProt ID
P43115
Sequence
MKETRGYGGDAPFCTRLNHSYTGMWAPERSAEARGNLTRPPGSGEDCGSVSVAFPITMLL
TGFVGNALAMLLVSRSYRRRESKRKKSFLLCIGWLALTDLVGQLLTTPVVIVVYLSKQRW
EHIDPSGRLCTFFGLTMTVFGLSSLFIASAMAVERALAIRAPHWYASHMKTRATRAVLLG
VWLAVLAFALLPVLGVGQYTVQWPGTWCFISTGRGGNGTSSSHNWGNLFFASAFAFLGLL
ALTVTFSCNLATIKALVSRCRAKATASQSSAQWGRITTETAIQLMGIMCVLSVCWSPLLI
MMLKMIFNQTSVEHCKTHTEKQKECNFFLIAVRLASLNQILDPWVYLLLRKILLRKFCQI
RYHTNNYASSSTSLPCQCSSTLMWSDHLER
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 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 533184IOP-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 545501Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003508)
Ref 547397Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800015910)
Ref 525462Effects 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 525582Selective activation of the prostanoid EP(3) receptor reduces myocardial infarct size in rodents. Arterioscler Thromb Vasc Biol. 1999 Sep;19(9):2141-7.
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 526239Involvement of prostaglandin E receptor subtype EP(4) in colon carcinogenesis. Cancer Res. 2002 Jan 1;62(1):28-32.
Ref 526303The prostaglandin receptor EP4 suppresses colitis, mucosal damage and CD4 cell activation in the gut. J Clin Invest. 2002 Apr;109(7):883-93.
Ref 526517Host prostaglandin E(2)-EP3 signaling regulates tumor-associated angiogenesis and tumor growth. J Exp Med. 2003 Jan 20;197(2):221-32.
Ref 527579Bioorg Med Chem Lett. 2005 Jul 1;15(13):3284-7.Metabolism investigation leading to novel drug design: orally active prostacyclin mimetics. Part 4.
Ref 528220Investigation 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 528393Bioorg 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 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 528849Involvement 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 530182Dual 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 531234Roles 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 533184IOP-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 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 534778Characterization 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 536080Effects 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.
Ref 536517BAY x 1005 attenuates atherosclerosis in apoE/LDLR - double knockout mice. J Physiol Pharmacol. 2007 Sep;58(3):583-8.
Ref 543779(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: 342).

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