Prostaglandin EP4 receptor
Prostaglandin E2 receptor 4 (EP4) is a prostaglandin receptor encoded by the PTGER4 gene in humans.
The protein encoded by this gene is a member of the G-protein coupled receptor family. This protein is one of four receptors identified for prostaglandin E2 (PGE2). This receptor can activate T-cell factor signaling. It has been shown to mediate PGE2 induced expression of early growth response 1 (EGR1), regulate the level and stability of cyclooxygenase-2 mRNA, and lead to the phosphorylation of glycogen synthase kinase-3. Knockout studies in mice suggest that this receptor may be involved in the neonatal adaptation of circulatory system, osteoporosis, as well as initiation of skin immune responses.[1]
See also
References
External links
Further reading
- Duncan AM, Anderson LL, Funk CD, et al. (1995). "Chromosomal localization of the human prostanoid receptor gene family". Genomics 25 (3): 740–2. doi:10.1016/0888-7543(95)80022-E. PMID 7759114.
- Wu H, Wu T, Hua W, Dong X, et al. (2015). "PGE2 receptor agonist misoprostol protects brain against intracerebral hemorrhage in mice.". Neurobiol Aging. 36 (3): 1439–50. doi:10.1016/j.neurobiolaging.2014.12.029. PMID 25623334.
- Regan JW, Bailey TJ, Pepperl DJ, et al. (1994). "Cloning of a novel human prostaglandin receptor with characteristics of the pharmacologically defined EP2 subtype". Mol. Pharmacol. 46 (2): 213–20. PMID 8078484.
- Bastien L, Sawyer N, Grygorczyk R, et al. (1994). "Cloning, functional expression, and characterization of the human prostaglandin E2 receptor EP2 subtype". J. Biol. Chem. 269 (16): 11873–7. PMID 8163486.
- An S, Yang J, Xia M, Goetzl EJ (1994). "Cloning and expression of the EP2 subtype of human receptors for prostaglandin E2". Biochem. Biophys. Res. Commun. 197 (1): 263–70. doi:10.1006/bbrc.1993.2470. PMID 8250933.
- Foord SM, Marks B, Stolz M, et al. (1996). "The structure of the prostaglandin EP4 receptor gene and related pseudogenes". Genomics 35 (1): 182–8. doi:10.1006/geno.1996.0337. PMID 8661119.
- Fedyk ER, Phipps RP (1996). "Prostaglandin E2 receptors of the EP2 and EP4 subtypes regulate activation and differentiation of mouse B lymphocytes to IgE-secreting cells". Proc. Natl. Acad. Sci. U.S.A. 93 (20): 10978–83. doi:10.1073/pnas.93.20.10978. PMC 38269. PMID 8855294.
- Mori K, Tanaka I, Kotani M, et al. (1996). "Gene expression of the human prostaglandin E receptor EP4 subtype: differential regulation in monocytoid and lymphoid lineage cells by phorbol ester". J. Mol. Med. 74 (6): 333–6. doi:10.1007/BF00207510. PMID 8862514.
- Mukhopadhyay P, Geoghegan TE, Patil RV, et al. (1997). "Detection of EP2, EP4, and FP receptors in human ciliary epithelial and ciliary muscle cells". Biochem. Pharmacol. 53 (9): 1249–55. doi:10.1016/S0006-2952(97)00011-7. PMID 9214685.
- Cosme R, Lublin D, Takafuji V, et al. (2000). "Prostanoids in human colonic mucosa: effects of inflammation on PGE(2) receptor expression". Hum. Immunol. 61 (7): 684–96. doi:10.1016/S0198-8859(00)00131-2. PMID 10880739.
- Desai S, April H, Nwaneshiudu C, Ashby B (2001). "Comparison of agonist-induced internalization of the human EP2 and EP4 prostaglandin receptors: role of the carboxyl terminus in EP4 receptor sequestration". Mol. Pharmacol. 58 (6): 1279–86. PMID 11093764.
- Sales KJ, Katz AA, Davis M, et al. (2001). "Cyclooxygenase-2 expression and prostaglandin E(2) synthesis are up-regulated in carcinomas of the cervix: a possible autocrine/paracrine regulation of neoplastic cell function via EP2/EP4 receptors". J. Clin. Endocrinol. Metab. 86 (5): 2243–9. doi:10.1210/jc.86.5.2243. PMC 2694306. PMID 11344234.
- Faour WH, He Y, He QW, et al. (2001). "Prostaglandin E(2) regulates the level and stability of cyclooxygenase-2 mRNA through activation of p38 mitogen-activated protein kinase in interleukin-1 beta-treated human synovial fibroblasts". J. Biol. Chem. 276 (34): 31720–31. doi:10.1074/jbc.M104036200. PMID 11423555.
- Desai S, Ashby B (2001). "Agonist-induced internalization and mitogen-activated protein kinase activation of the human prostaglandin EP4 receptor". FEBS Lett. 501 (2–3): 156–60. doi:10.1016/S0014-5793(01)02640-0. PMID 11470276.
- Slipetz D, Buchanan S, Mackereth C, et al. (2001). "Sequestration and phosphorylation of the prostaglandin E2 EP4 receptor: dependence on the C-terminal tail". Biochem. Pharmacol. 62 (8): 997–1012. doi:10.1016/S0006-2952(01)00742-0. PMID 11597569.
- Fujino H, West KA, Regan JW (2002). "Phosphorylation of glycogen synthase kinase-3 and stimulation of T-cell factor signaling following activation of EP2 and EP4 prostanoid receptors by prostaglandin E2". J. Biol. Chem. 277 (4): 2614–9. doi:10.1074/jbc.M109440200. PMID 11706038.
- Mutoh M, Watanabe K, Kitamura T, et al. (2002). "Involvement of prostaglandin E receptor subtype EP(4) in colon carcinogenesis". Cancer Res. 62 (1): 28–32. PMID 11782353.
- Kvirkvelia N, Vojnovic I, Warner TD, et al. (2002). "Placentally derived prostaglandin E2 acts via the EP4 receptor to inhibit IL-2-dependent proliferation of CTLL-2 T cells". Clin. Exp. Immunol. 127 (2): 263–9. doi:10.1046/j.1365-2249.2002.01718.x. PMC 1906325. PMID 11876748.
- Asano T, Shoda J, Ueda T, et al. (2002). "Expressions of cyclooxygenase-2 and prostaglandin E-receptors in carcinoma of the gallbladder: crucial role of arachidonate metabolism in tumor growth and progression". Clin. Cancer Res. 8 (4): 1157–67. PMID 11948128.
- Kyveris A, Maruscak E, Senchyna M (2002). "Optimization of RNA isolation from human ocular tissues and analysis of prostanoid receptor mRNA expression using RT-PCR". Mol. Vis. 8: 51–8. PMID 11951086.
- Scandella E, Men Y, Gillessen S, et al. (2002). "Prostaglandin E2 is a key factor for CCR7 surface expression and migration of monocyte-derived dendritic cells". Blood 100 (4): 1354–61. doi:10.1182/blood-2001-11-0017. PMID 12149218.
This article incorporates text from the United States National Library of Medicine, which is in the public domain.
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| Receptor (ligands) | DP (D2) | | |
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- Antagonists: ADC-3680
- AZD-1981
- Bay U3405
- Fevipiprant
- MK-1029
- MK-7246
- OC-459
- OC000459
- QAV-680
- Ramatroban
- Setipiprant
- TM30089
- Vidupiprant
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| EP (E2) | |
- Antagonists: AH-6809
- ONO-8130
- SC-19220
- SC-51089
- SC-51322
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- Antagonists: AH-6809
- PF-04418948
- TG 4-155
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- Antagonists: GW-627368
- L-161982
- ONO-AE3-208
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| Unsorted | |
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| FP (F2α) | |
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| IP (I2) | |
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| TP (TXA2) | |
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| Unsorted |
- Arbaprostil
- Ataprost
- Ciprostene
- Clinprost
- Cobiprostone
- Delprostenate
- Deprostil
- Dimoxaprost
- Doxaprost
- Ecraprost
- Eganoprost
- Enisoprost
- Eptaloprost
- Esuberaprost
- Etiproston
- Fenprostalene
- Flunoprost
- Froxiprost
- Lanproston
- Limaprost
- Luprostiol
- Meteneprost
- Mexiprostil
- Naxaprostene
- Nileprost
- Nocloprost
- Ornoprostil
- Oxoprostol
- Penprostene
- Pimilprost
- Piriprost
- Posaraprost
- Prostalene
- Rioprostil
- Rivenprost
- Rosaprostol
- Spiriprostil
- Tiaprost
- Tilsuprost
- Tiprostanide
- Trimoprostil
- Viprostol
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| Enzyme (inhibitors) | |
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| Others | |
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| See also: Leukotrienergics |
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