Target Information

Target General Infomation
Target ID
T38529
Former ID
TTDS00168
Target Name
Prostaglandin E2receptor, EP2 subtype
Gene Name
PTGER2
Synonyms
EP2 receptor; PGE receptor, EP2 subtype; Prostanoid EP2 receptor; PTGER2
Target Type
Successful
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.
BioChemical Class
GPCR rhodopsin
Target Validation
T38529
UniProt ID
P43116
Sequence
MGNASNDSQSEDCETRQWLPPGESPAISSVMFSAGVLGNLIALALLARRWRGDVGCSAGR
RSSLSLFHVLVTELVFTDLLGTCLISPVVLASYARNQTLVALAPESRACTYFAFAMTFFS
LATMLMLFAMALERYLSIGHPYFYQRRVSRSGGLAVLPVIYAVSLLFCSLPLLDYGQYVQ
YCPGTWCFIRHGRTAYLQLYATLLLLLIVSVLACNFSVILNLIRMHRRSRRSRCGPSLGS
GRGGPGARRRGERVSMAEETDHLILLAIMTITFAVCSLPFTIFAYMNETSSRKEKWDLQA
LRFLSINSIIDPWVFAILRPPVLRLMRSVLCCRISLRTQDATQTSCSTQSDASKQADL
Drugs and Mode of Action
Drug(s) Dinoprostone Drug Info Approved Medical abortion [1], [2]
Iloprost Drug Info Approved Pulmonary arterial hypertension [3], [4], [5]
Lipo-alprostadil Drug Info Approved Diabetic foot ulcer [6]
LAROPIPRANT Drug Info Phase 4 Discovery agent [7], [8]
CP-533536 Drug Info Phase 2 Osteoporosis [9], [10]
DE-117 Drug Info Phase 2 Glaucoma [11]
Taprenepag Drug Info Phase 2 Glaucoma [12], [13]
PF-4418948 Drug Info Phase 1 Endometriosis [14], [15]
PGF2alpha Drug Info Clinical trial Solid tumours [16]
ONO-8815Ly Drug Info Terminated Miscarriage [17], [18]
Agonist 11-deoxy-PGE1 Drug Info [19]
16,16-dimethyl-PGE2 Drug Info [19]
17-phenyl-omega-trinor-PGE2 Drug Info [20]
19(R)-OH-PGE2 Drug Info [20]
AH13205 Drug Info [19]
butaprost (free acid form) Drug Info [21]
carbacyclin Drug Info [22]
cicaprost Drug Info [19]
CP-533536 Drug Info [9], [23]
DE-117 Drug Info [24]
Iloprost Drug Info [25]
isocarbacyclin Drug Info [19]
Lipo-alprostadil Drug Info [6]
M&B 28767 Drug Info [20]
ONO-8815Ly Drug Info [26]
ONO-AE-248 Drug Info [27]
ONO-AE1-329 Drug Info [27]
PGD2 Drug Info [21]
PGF2alpha Drug Info [21]
Taprenepag Drug Info [28]
U46619 Drug Info [20]
Inhibitor 3-(2-((E)-3-phenylprop-1-enyl)phenyl)acrylic acid Drug Info [29]
3-(2-(4-methoxycinnamyl)phenyl)acrylic acid Drug Info [29]
3-(2-(naphthalen-2-ylmethyl)phenyl)acrylic acid Drug Info [29]
3-(2-cinnamylphenyl)acrylic acid Drug Info [29]
BUTAPROST Drug Info [30]
LAROPIPRANT Drug Info [31]
Antagonist AH6809 Drug Info [22]
Dinoprostone Drug Info [32]
PF-00212062 Drug Info [33]
PF-4418948 Drug Info [34]
TG4-155 Drug Info [35]
TG7-171 Drug Info [36]
Modulator (allosteric modulator) compound 1 Drug Info [37]
Modulator R-65 Drug Info [33]
R-99 Drug Info [33]
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 1FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 020411.
REF 2(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 32004 approvals: the demise of the blockbuster. Nat Rev Drug Discov. 2005 Feb;4(2):93-4.
REF 4(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 5Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
REF 6Emerging drugs for diabetic foot ulcers. Expert Opin Emerg Drugs. 2006 Nov;11(4):709-24.
REF 7ClinicalTrials.gov (NCT01126073) Niacin/Laropiprant and Endothelial Function. U.S. National Institutes of Health.
REF 8(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 9Discovery 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 10(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 11ClinicalTrials.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 12ClinicalTrials.gov (NCT00572455) Safety and Efficacy of PF-04217329 in Patients With Glaucoma or Elevated Eye Pressure.. U.S. National Institutes of Health.
REF 13(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 14ClinicalTrials.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 15(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 16Stereocontrolled organocatalytic synthesis of prostaglandin PGF2alpha in seven steps. Nature. 2012 Sep 13;489(7415):278-81.
REF 17(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 18Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800012532)
REF 19Ligand 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 20Molecular cloning and characterization of the four rat prostaglandin E2 prostanoid receptor subtypes. Eur J Pharmacol. 1997 Dec 11;340(2-3):227-41.
REF 21Importance of the extracellular domain for prostaglandin EP(2) receptor function. Mol Pharmacol. 1999 Sep;56(3):545-51.
REF 22The 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 23Pfizer. Product Development Pipeline. March 31 2009.
REF 24Clinical pipeline report, company report or official report of Santen Pharmaceutical.
REF 25Exploration 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 26Prostaglandin 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 27The 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 28A 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 29Bioorg 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 30Bioorg 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 31J 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 32Concurrent dinoprostone and oxytocin for labor induction in term premature rupture of membranes: a randomized controlled trial. Obstet Gynecol. 2009 May;113(5):1059-65.
REF 33(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: 341).
REF 34Clinical pipeline report, company report or official report of axonmedchem.
REF 35Small 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 36Development of second generation EP2 antagonists with high selectivity. Eur J Med Chem. 2014 Jul 23;82:521-35.
REF 37Neuroprotection by selective allosteric potentiators of the EP2 prostaglandin receptor. Proc Natl Acad Sci U S A. 2010 Feb 2;107(5):2307-12.

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