Target Information
Target General Infomation | |||||
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Target ID |
T18876
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Former ID |
TTDC00151
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Target Name |
Prostaglandin E2 receptor, EP4 subtype
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Gene Name |
PTGER4
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Synonyms |
EP sub 4 receptor; PGE receptor, EP4 subtype; Prostanoid EP4 receptor; PTGER4
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Target Type |
Clinical Trial
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Disease | Asthma [ICD10: J45] | ||||
Acute heart failure [ICD9: 428; ICD10: I50] | |||||
Fracture [ICD10: M48.5] | |||||
Glaucoma [ICD9: 365; ICD10: H40-H42] | |||||
Inflammatory disease [ICD9: 140-229, 147, 173, 573.3, 710-719; ICD10: C11, C44, K75.9, M00-M25] | |||||
Migraine [ICD9: 346; ICD10: G43] | |||||
Osteoarthritis; Pain [ICD9: 338, 715,780; ICD10: M15-M19, M47, R52, G89] | |||||
Osteoarthritis [ICD9: 715; ICD10: M15-M19, M47] | |||||
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89] | |||||
Solid tumours [ICD9: 140-199, 210-229; ICD10: C00-D48] | |||||
Ulcerative colitis [ICD9: 556; ICD10: K51] | |||||
Function |
Receptor for prostaglandin E2 (PGE2). The activity of this receptor is mediated by G(s) proteins that stimulate adenylate cyclase. Has a relaxing effect on smooth muscle. May play an important role in regulating renal hemodynamics, intestinal epithelial transport, adrenal aldosterone secretion, and uterine function.
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BioChemical Class |
GPCR rhodopsin
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Target Validation |
T18876
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UniProt ID | |||||
Sequence |
MSTPGVNSSASLSPDRLNSPVTIPAVMFIFGVVGNLVAIVVLCKSRKEQKETTFYTLVCG
LAVTDLLGTLLVSPVTIATYMKGQWPGGQPLCEYSTFILLFFSLSGLSIICAMSVERYLA INHAYFYSHYVDKRLAGLTLFAVYASNVLFCALPNMGLGSSRLQYPDTWCFIDWTTNVTA HAAYSYMYAGFSSFLILATVLCNVLVCGALLRMHRQFMRRTSLGTEQHHAAAAASVASRG HPAASPALPRLSDFRRRRSFRRIAGAEIQMVILLIATSLVVLICSIPLVVRVFVNQLYQP SLEREVSKNPDLQAIRIASVNPILDPWIYILLRKTVLSKAIEKIKCLFCRIGGSRRERSG QHCSDSQRTSSAMSGHSRSFISRELKEISSTSQTLLPDLSLPDLSENGLGGRNLLPGVPG MGLAQEDTTSLRTLRISETSDSSQGQDSESVLLVDEAGGSGRAGPAPKGSSLQVTFPSET LNLSEKCI |
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Drugs and Mode of Action | |||||
Drug(s) | BGC-20-1531 | Drug Info | Phase 2 | Migraine | [522648], [540329] |
ONO-AE1-437 | Drug Info | Phase 2 | Asthma | [543189] | |
RQ-00000007 (oral) | Drug Info | Phase 2 | Pain | [541167], [548890] | |
EP4-R antagonist | Drug Info | Phase 1 | Osteoarthritis; Pain | [549532] | |
ONO-4232 | Drug Info | Phase 1 | Acute heart failure | [549519] | |
PGF2alpha | Drug Info | Clinical trial | Solid tumours | [532003] | |
ONO-4819 | Drug Info | Discontinued in Phase 2 | Fracture | [539230], [547505] | |
Agonist | 1-OH-PGE1 | Drug Info | [534478] | ||
11-deoxy-PGE1 | Drug Info | [525852] | |||
11-deoxy-PGE2 | Drug Info | [534595] | |||
13,14-dihydro-PGE1 | Drug Info | [525852] | |||
16,16-dimethyl-PGE2 | Drug Info | [534478] | |||
19(R)-OH-PGE2 | Drug Info | [534595] | |||
butaprost (free acid form) | Drug Info | [534595] | |||
carbacyclin | Drug Info | [534478] | |||
cicaprost | Drug Info | [525673] | |||
CP734432 | Drug Info | [530142] | |||
KAG-308 | Drug Info | [543780] | |||
L902688 | Drug Info | [543780] | |||
M&B 28767 | Drug Info | [534478] | |||
ONO-4232 | Drug Info | [549789] | |||
ONO-4819 | Drug Info | [536219], [536465], [537179] | |||
ONO-AE1-329 | Drug Info | [525735] | |||
ONO-AE1-437 | Drug Info | [527162] | |||
PF-04475270 | Drug Info | [543780] | |||
PGD2 | Drug Info | [534595] | |||
PGF2alpha | Drug Info | [534595] | |||
TCS 2510 | Drug Info | [543780] | |||
U46619 | Drug Info | [534595] | |||
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] | |||
8-aza-11-deoxyprostaglandin E1 | Drug Info | [527306] | |||
FR-181157 | Drug Info | [527530] | |||
Antagonist | AH23848 | Drug Info | [534595] | ||
BGC-20-1531 | Drug Info | [544082] | |||
CR-5790 | Drug Info | [543780] | |||
EP4-R antagonist | Drug Info | [543780] | |||
ER819762 | Drug Info | [530872] | |||
GW 627368 | Drug Info | [527379] | |||
MK-2894 | Drug Info | [543780] | |||
ONO-AE2-227 | Drug Info | [526239] | |||
ONO-AE3-208 | Drug Info | [526303] | |||
ONO-AE3-240 | Drug Info | [526517] | |||
RQ-00000007 (oral) | Drug Info | [550316] | |||
RQ-00000008 | Drug Info | [543780] | |||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
KEGG Pathway | Neuroactive ligand-receptor interaction | ||||
Inflammatory mediator regulation of TRP channels | |||||
Renin secretion | |||||
Pathways in cancer | |||||
NetPath Pathway | FSH Signaling Pathway | ||||
IL2 Signaling Pathway | |||||
IL4 Signaling Pathway | |||||
TGF_beta_Receptor Signaling Pathway | |||||
Reactome | Prostanoid ligand receptors | ||||
G alpha (s) signalling events | |||||
WikiPathways | Prostaglandin Synthesis and Regulation | ||||
GPCRs, Class A Rhodopsin-like | |||||
Vitamin D Receptor Pathway | |||||
Small Ligand GPCRs | |||||
GPCR ligand binding | |||||
GPCR downstream signaling | |||||
References | |||||
Ref 522648 | ClinicalTrials.gov (NCT00888680) Double-blind, Placebo-controlled Study of BGC20-1531 in Migraine. 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 539230 | (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: 1930). | ||||
Ref 540329 | (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: 3380). | ||||
Ref 541167 | (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: 5858). | ||||
Ref 543189 | (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: 8541). | ||||
Ref 547505 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800016907) | ||||
Ref 548890 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800029996) | ||||
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 525852 | Pharmacological characterization of [(3)H]-prostaglandin E(2) binding to the cloned human EP(4) prostanoid receptor. Br J Pharmacol. 2000 Aug;130(8):1919-26. | ||||
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 527162 | An EP4 receptor agonist prevents indomethacin-induced closure of rat ductus arteriosus in vivo. Pediatr Res. 2004 Oct;56(4):586-90. Epub 2004 Aug 4. | ||||
Ref 527306 | J Med Chem. 2004 Dec 2;47(25):6124-7.Lactams as EP4 prostanoid receptor agonists. 3. Discovery of N-ethylbenzoic acid 2-pyrrolidinones as subtype selective agents. | ||||
Ref 527379 | Piglet saphenous vein contains multiple relaxatory prostanoid receptors: evidence for EP4, EP2, DP and IP receptor subtypes. Br J Pharmacol. 2005 Feb;144(3):405-15. | ||||
Ref 527530 | J Med Chem. 2005 May 5;48(9):3103-6.Discovery of diphenyloxazole and Ndelta-Z-ornithine derivatives as highly potent and selective human prostaglandin EP(4) receptor antagonists. | ||||
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 530142 | Ocular pharmacokinetics and hypotensive activity of PF-04475270, an EP4 prostaglandin agonist in preclinical models. Exp Eye Res. 2009 Nov;89(5):608-17. | ||||
Ref 530872 | A novel antagonist of the prostaglandin E(2) EP(4) receptor inhibits Th1 differentiation and Th17 expansion and is orally active in arthritis models. Br J Pharmacol. 2010 May;160(2):292-310. | ||||
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 536219 | Effects on improvement of blood flow in the chronically compressed cauda equina: comparison between a selective prostaglandin E receptor (EP4) agonist and a prostaglandin E1 derivate. Spine (Phila Pa1976). 2006 Apr 15;31(8):869-72. | ||||
Ref 536465 | Prostaglandin E2 EP4 agonist (ONO-4819) accelerates BMP-induced osteoblastic differentiation. Bone. 2007 Oct;41(4):543-8. Epub 2007 Jun 29. | ||||
Ref 537179 | Effect of a prostaglandin EP4 receptor agonist on early fixation of hydroxyapatite/titanium composite- and titanium-coated rough-surfaced implants in ovariectomized rats. J Biomed Mater Res A. 2009 Mar 25. | ||||
Ref 543780 | (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: 343). | ||||
Ref 544082 | BGC20-1531, a novel, potent and selective prostanoid EP4 receptor antagonist: a putative new treatment for migraine headache. Br J Pharmacol. 2009 January; 156(2): 316-327. |
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