Target Information
Target General Infomation | |||||
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Target ID |
T38529
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Former ID |
TTDS00168
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Target Name |
Prostaglandin E2receptor, EP2 subtype
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Gene Name |
PTGER2
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Synonyms |
EP2 receptor; PGE receptor, EP2 subtype; Prostanoid EP2 receptor; PTGER2
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Target Type |
Successful
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Disease | Cancer [ICD9: 140-229; ICD10: C00-C96] | ||||
Diabetic foot ulcer [ICD9: 707; ICD10: L88-L89] | |||||
Endometriosis [ICD9: 617; ICD10: N80] | |||||
Glaucoma [ICD9: 365; ICD10: H40-H42] | |||||
Immune disorder [ICD10: D80-D89] | |||||
Medical abortion [ICD9: 779.6; ICD10: O04] | |||||
Miscarriage [ICD10: O03] | |||||
Osteoporosis [ICD9: 733.0, V07.4; ICD10: M80-M81, Z79.890] | |||||
Pulmonary arterial hypertension [ICD9: 416; ICD10: I27.0, I27.2] | |||||
Solid tumours [ICD9: 140-199, 210-229; ICD10: C00-D48] | |||||
Function |
Receptor for prostaglandin E2 (PGE2). The activity of this receptor is mediated by G(s) proteins that stimulate adenylate cyclase. The subsequent raise in intracellular cAMP is responsible for the relaxing effect of this receptor on smooth muscle.
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BioChemical Class |
GPCR rhodopsin
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Target Validation |
T38529
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UniProt ID | |||||
Sequence |
MGNASNDSQSEDCETRQWLPPGESPAISSVMFSAGVLGNLIALALLARRWRGDVGCSAGR
RSSLSLFHVLVTELVFTDLLGTCLISPVVLASYARNQTLVALAPESRACTYFAFAMTFFS LATMLMLFAMALERYLSIGHPYFYQRRVSRSGGLAVLPVIYAVSLLFCSLPLLDYGQYVQ YCPGTWCFIRHGRTAYLQLYATLLLLLIVSVLACNFSVILNLIRMHRRSRRSRCGPSLGS GRGGPGARRRGERVSMAEETDHLILLAIMTITFAVCSLPFTIFAYMNETSSRKEKWDLQA LRFLSINSIIDPWVFAILRPPVLRLMRSVLCCRISLRTQDATQTSCSTQSDASKQADL |
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Drugs and Mode of Action | |||||
Drug(s) | Dinoprostone | Drug Info | Approved | Medical abortion | [538546], [539217] |
Iloprost | Drug Info | Approved | Pulmonary arterial hypertension | [527466], [539263], [551871] | |
Lipo-alprostadil | Drug Info | Approved | Diabetic foot ulcer | [536297] | |
LAROPIPRANT | Drug Info | Phase 4 | Discovery agent | [523049], [540312] | |
CP-533536 | Drug Info | Phase 2 | Osteoporosis | [537118], [539228] | |
DE-117 | Drug Info | Phase 2 | Glaucoma | [524813] | |
Taprenepag | Drug Info | Phase 2 | Glaucoma | [522182], [541134] | |
PF-4418948 | Drug Info | Phase 1 | Endometriosis | [522833], [541135] | |
PGF2alpha | Drug Info | Clinical trial | Solid tumours | [532003] | |
ONO-8815Ly | Drug Info | Terminated | Miscarriage | [539232], [547048] | |
Agonist | 11-deoxy-PGE1 | Drug Info | [534478] | ||
16,16-dimethyl-PGE2 | Drug Info | [534478] | |||
17-phenyl-omega-trinor-PGE2 | Drug Info | [534595] | |||
19(R)-OH-PGE2 | Drug Info | [534595] | |||
AH13205 | Drug Info | [534478] | |||
butaprost (free acid form) | Drug Info | [525571] | |||
carbacyclin | Drug Info | [525673] | |||
cicaprost | Drug Info | [534478] | |||
CP-533536 | Drug Info | [537118], [549974] | |||
DE-117 | Drug Info | [551625] | |||
Iloprost | Drug Info | [536390] | |||
isocarbacyclin | Drug Info | [534478] | |||
Lipo-alprostadil | Drug Info | [536297] | |||
M&B 28767 | Drug Info | [534595] | |||
ONO-8815Ly | Drug Info | [531621] | |||
ONO-AE-248 | Drug Info | [525735] | |||
ONO-AE1-329 | Drug Info | [525735] | |||
PGD2 | Drug Info | [525571] | |||
PGF2alpha | Drug Info | [525571] | |||
Taprenepag | Drug Info | [531603] | |||
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] | |||
BUTAPROST | Drug Info | [529174] | |||
LAROPIPRANT | Drug Info | [528672] | |||
Antagonist | AH6809 | Drug Info | [525673] | ||
Dinoprostone | Drug Info | [537253] | |||
PF-00212062 | Drug Info | [543778] | |||
PF-4418948 | Drug Info | [550328] | |||
TG4-155 | Drug Info | [531794] | |||
TG7-171 | Drug Info | [532849] | |||
Modulator (allosteric modulator) | compound 1 | Drug Info | [530640] | ||
Modulator | R-65 | Drug Info | [543778] | ||
R-99 | Drug Info | [543778] | |||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
KEGG Pathway | cAMP signaling pathway | ||||
Neuroactive ligand-receptor interaction | |||||
Inflammatory mediator regulation of TRP channels | |||||
Renin secretion | |||||
Pathways in cancer | |||||
Reactome | Prostanoid ligand receptors | ||||
G alpha (s) signalling events | |||||
WikiPathways | Prostaglandin Synthesis and Regulation | ||||
GPCRs, Class A Rhodopsin-like | |||||
Ovarian Infertility Genes | |||||
Small Ligand GPCRs | |||||
GPCR ligand binding | |||||
GPCR downstream signaling | |||||
References | |||||
Ref 522182 | ClinicalTrials.gov (NCT00572455) Safety and Efficacy of PF-04217329 in Patients With Glaucoma or Elevated Eye Pressure.. U.S. National Institutes of Health. | ||||
Ref 522833 | ClinicalTrials.gov (NCT01002963) A Study To Investigate The Safety And Toleration Of A Single Dose Of PF-04418948 In Healthy Volunteers. U.S. National Institutes of Health. | ||||
Ref 523049 | ClinicalTrials.gov (NCT01126073) Niacin/Laropiprant and Endothelial Function. U.S. National Institutes of Health. | ||||
Ref 524813 | ClinicalTrials.gov (NCT02179008) Multi-center Phase II Study Assessing the Safety and Efficacy of DE-117 Ophthalmic Solution in Subjects With Primary Open-angle Glaucoma or Ocular Hypertension. 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 537118 | Discovery of CP-533536: an EP2 receptor selective prostaglandin E2 (PGE2) agonist that induces local bone formation. Bioorg Med Chem Lett. 2009 Apr 1;19(7):2075-8. Epub 2009 Jan 23. | ||||
Ref 538546 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 020411. | ||||
Ref 539217 | (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: 1916). | ||||
Ref 539228 | (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: 1929). | ||||
Ref 539232 | (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: 1932). | ||||
Ref 539263 | (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: 1966). | ||||
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 541134 | (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: 5816). | ||||
Ref 541135 | (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: 5817). | ||||
Ref 525571 | Importance of the extracellular domain for prostaglandin EP(2) receptor function. Mol Pharmacol. 1999 Sep;56(3):545-51. | ||||
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 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 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 529174 | Bioorg Med Chem Lett. 2008 Jan 15;18(2):821-4. Epub 2007 Nov 13.Synthesis and evaluation of a gamma-lactam as a highly selective EP2 and EP4 receptor agonist. | ||||
Ref 530640 | Neuroprotection by selective allosteric potentiators of the EP2 prostaglandin receptor. Proc Natl Acad Sci U S A. 2010 Feb 2;107(5):2307-12. | ||||
Ref 531603 | A phase 2, randomized, dose-response trial of taprenepag isopropyl (PF-04217329) versus latanoprost 0.005% in open-angle glaucoma and ocular hypertension. Curr Eye Res. 2011 Sep;36(9):809-17. | ||||
Ref 531621 | Prostaglandin E2 receptor type 2-selective agonist prevents the degeneration of articular cartilage in rabbit knees with traumatic instability. Arthritis Res Ther. 2011;13(5):R146. | ||||
Ref 531794 | Small molecule antagonist reveals seizure-induced mediation of neuronal injury by prostaglandin E2 receptor subtype EP2. Proc Natl Acad Sci U S A. 2012 Feb 21;109(8):3149-54. | ||||
Ref 532849 | Development of second generation EP2 antagonists with high selectivity. Eur J Med Chem. 2014 Jul 23;82:521-35. | ||||
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 536390 | Exploration of prostanoid receptor subtype regulating estradiol and prostaglandin E2 induction of spinophilin in developing preoptic area neurons. Neuroscience. 2007 May 25;146(3):1117-27. Epub 2007Apr 6. | ||||
Ref 537118 | Discovery of CP-533536: an EP2 receptor selective prostaglandin E2 (PGE2) agonist that induces local bone formation. Bioorg Med Chem Lett. 2009 Apr 1;19(7):2075-8. Epub 2009 Jan 23. | ||||
Ref 537253 | Concurrent dinoprostone and oxytocin for labor induction in term premature rupture of membranes: a randomized controlled trial. Obstet Gynecol. 2009 May;113(5):1059-65. |
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