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Literature summary extracted from

  • Mbalaviele, G.; Pauley, A.M.; Shaffer, A.F.; Zweifel, B.S.; Mathialagan, S.; Mnich, S.J.; Nemirovskiy, O.V.; Carter, J.; Gierse, J.K.; Wang, J.L.; Vazquez, M.L.; Moore, W.M.; Masferrer, J.L.
    Distinction of microsomal prostaglandin E synthase-1 (mPGES-1) inhibition from cyclooxygenase-2 inhibition in cells using a novel, selective mPGES-1 inhibitor (2010), Biochem. Pharmacol., 79, 1445-1454.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
5.3.99.3 expressed in Escherichia coli BL21(DE3) cells Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
5.3.99.3 indomethacin
-
 Homo sapiens
5.3.99.3 indomethacin
-
 Rattus norvegicus
5.3.99.3 MK-886
-
 Homo sapiens
5.3.99.3 MK-886
-
 Rattus norvegicus
5.3.99.3 PF-9184 potent, competitive and reversible mPGES-1 inhibitor, i.e. N-(3',4'-dichlorobiphenyl-4-yl)-4-hydroxy-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide Homo sapiens
5.3.99.3 PF-9184 poor mPGES-1 inhibitor, i.e. N-(3',4'-dichlorobiphenyl-4-yl)-4-hydroxy-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide Rattus norvegicus
5.3.99.3 SC-236
-
 Homo sapiens
5.3.99.3 SC-236
-
 Rattus norvegicus

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
5.3.99.3 microsome
-
 Homo sapiens
-
-
5.3.99.3 microsome
-
 Rattus norvegicus
-
-

Organism

EC Number Organism UniProt Comment Textmining
5.3.99.3 Homo sapiens
-
-
-
5.3.99.3 Rattus norvegicus
-
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
5.3.99.3 Prostaglandin H2
-
 Homo sapiens Prostaglandin E2
-
 ?
5.3.99.3 Prostaglandin H2
-
 Rattus norvegicus Prostaglandin E2
-
 ?

Synonyms

EC Number Synonyms Comment Organism
5.3.99.3 microsomal prostaglandin E synthase-1
-
 Homo sapiens
5.3.99.3 microsomal prostaglandin E synthase-1
-
 Rattus norvegicus
5.3.99.3 mPGES-1
-
 Homo sapiens
5.3.99.3 mPGES-1
-
 Rattus norvegicus

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
5.3.99.3 0.0000165
-
 recombinant enzyme, in 100 mM K3PO4 buffer at pH 6.2 Homo sapiens PF-9184
5.3.99.3 0.00108
-
 in 100 mM K3PO4 buffer at pH 6.2 Rattus norvegicus PF-9184

General Information

EC Number General Information Comment Organism
5.3.99.3 physiological function the enzyme is responsible for prostaglandin E2 synthesis in inflammation-associated pathologies Homo sapiens
5.3.99.3 physiological function the enzyme is responsible for prostaglandin E2 synthesis in inflammation-associated pathologies Rattus norvegicus