mPGES1
Target has curated data in GtoImmuPdb
Target id: 1377
Nomenclature: mPGES1
Family: Prostaglandin synthases
Annotation status:
Awaiting annotation/under development. Please contact us if you can help with annotation.
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Contents:
Gene and Protein Information  |
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| Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
| Human | - | - | PTGES | prostaglandin E synthase | ||
| Mouse | - | - | Ptges | prostaglandin E synthase | ||
| Rat | - | - | Ptges | prostaglandin E synthase | ||
| Previous and Unofficial Names |
| MGST1-L1 | PIG12 | Prostaglandin E synthase | MGST-IV | MGST1-like 1 | microsomal prostaglandin E synthase-1 | Pges |
| Database Links |
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| BRENDA | 5.3.99.3 |
| CATH/Gene3D | 1.20.120.550 |
| Ensembl Gene | ENSG00000148344 (Hs), ENSMUSG00000050737 (Mm), ENSRNOG00000006320 (Rn) |
| Entrez Gene | 9536 (Hs), 64292 (Mm), 59103 (Rn) |
| Human Protein Atlas | ENSG00000148344 (Hs) |
| KEGG Enzyme | 5.3.99.3 |
| KEGG Gene | hsa:9536 (Hs), mmu:64292 (Mm), rno:59103 (Rn) |
| OMIM | 605172 (Hs) |
| SynPHARM | 82842 (in complex with compound 30 [PMID: 15953724]) |
| UniProtKB | O14684 (Hs), Q9JM51 (Mm) |
| Wikipedia | PTGES (Hs) |
| Selected 3D Structures |
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| Enzyme Reaction |
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Download all structure-activity data for this target as a CSV file 
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| Key to terms and symbols | View all chemical structures | Click column headers to sort | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| Immunopharmacology Comments |
| Inhibition of mPGES-1 is proposed as a potentially safer alternative to COX-2 inhibition for the treatment of pain and inflammation, with a reduced risk of cardiovascular side effects [4]. Inhibition of mPGES-1 in A549 cells and mouse macrophages by compound III [PMID: 24045148] reduces PGE2 production [2]. |
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References
1. Giroux A, Boulet L, Brideau C, Chau A, Claveau D, Côté B, Ethier D, Frenette R, Gagnon M, Guay J et al.. (2009) Discovery of disubstituted phenanthrene imidazoles as potent, selective and orally active mPGES-1 inhibitors. Bioorg. Med. Chem. Lett., 19 (20): 5837-41. [PMID:19748780]
2. Leclerc P, Idborg H, Spahiu L, Larsson C, Nekhotiaeva N, Wannberg J, Stenberg P, Korotkova M, Jakobsson PJ. (2013) Characterization of a human and murine mPGES-1 inhibitor and comparison to mPGES-1 genetic deletion in mouse models of inflammation. Prostaglandins Other Lipid Mediat., 107: 26-34. [PMID:24045148]
3. Luz JG, Antonysamy S, Kuklish SL, Condon B, Lee MR, Allison D, Yu XP, Chandrasekhar S, Backer R, Zhang A et al.. (2015) Crystal Structures of mPGES-1 Inhibitor Complexes Form a Basis for the Rational Design of Potent Analgesic and Anti-Inflammatory Therapeutics. J. Med. Chem., 58 (11): 4727-37. [PMID:25961169]
4. Ozen G, Gomez I, Daci A, Deschildre C, Boubaya L, Teskin O, Uydeş-Doğan BS, Jakobsson PJ, Longrois D, Topal G et al.. (2017) Inhibition of microsomal PGE synthase-1 reduces human vascular tone by increasing PGI2 : a safer alternative to COX-2 inhibition. Br. J. Pharmacol., 174 (22): 4087-4098. [PMID:28675448]
5. Riendeau D, Aspiotis R, Ethier D, Gareau Y, Grimm EL, Guay J, Guiral S, Juteau H, Mancini JA, Méthot N et al.. (2005) Inhibitors of the inducible microsomal prostaglandin E2 synthase (mPGES-1) derived from MK-886. Bioorg. Med. Chem. Lett., 15 (14): 3352-5. [PMID:15953724]
6. Shiro T, Kakiguchi K, Takahashi H, Nagata H, Tobe M. (2013) 7-Phenyl-imidazoquinolin-4(5H)-one derivatives as selective and orally available mPGES-1 inhibitors. Bioorg. Med. Chem., 21 (11): 2868-78. [PMID:23623673]
7. Wannberg J, Alterman M, Malm J, Stenberg P, Westman J, Wallberg H. (2011) Microsomal prostaglandin e synthase-1 (mpges1) inhibitors. Patent number: WO2011023812. Assignee: Novasaid Ab. Priority date: 27/08/2009. Publication date: 03/03/2011.
How to cite this page
Prostaglandin synthases: mPGES1. Last modified on 23/11/2017. Accessed on 16/02/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=1377.
