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Literature summary extracted from

  • Bahia, M.S.; Katare, Y.K.; Silakari, O.; Vyas, B.; Silakari, P.
    Inhibitors of microsomal prostaglandin E2 synthase-1 enzyme as emerging anti-inflammatory candidates (2014), Med. Res. Rev., 34, 825-855 .
    View publication on PubMed

Activating Compound

EC Number Activating Compound Comment Organism Structure
5.3.99.3 glutathione
-
Homo sapiens

Application

EC Number Application Comment Organism
5.3.99.3 medicine enzyme inhibition can be useful for treating pain, fever, and anorexia Homo sapiens

Cloned(Commentary)

EC Number Cloned (Comment) Organism
5.3.99.3 expressed in A-549 cells, HeLa cells, HEK-293 cells, RAW 264.7 cells, Pichia pastoris strain KM71H, and Sf9 insect cells Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
5.3.99.3 3-(4-dodecanoyl-1,5-dimethyl-3-phenyl-1H-pyrrol-2-yl)propanoic acid
-
Homo sapiens
5.3.99.3 4-(3-chlorobenzyl)-2,6-bis[4-(trifluoromethoxy)phenyl]-4H-thieno[3,2-b]pyrrole-5-carboxylic acid
-
Homo sapiens
5.3.99.3 AF3442
-
Homo sapiens
5.3.99.3 licofelone
-
Homo sapiens
5.3.99.3 Oxacillin
-
Homo sapiens
5.3.99.3 YS121 reversible and noncompetitive inhibition Homo sapiens

Localization

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

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
5.3.99.3 Prostaglandin H2 Homo sapiens
-
Prostaglandin E2
-
?

Organism

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

Source Tissue

EC Number Source Tissue Comment Organism Textmining
5.3.99.3 epididymis
-
Homo sapiens
-
5.3.99.3 epithelial cell
-
Homo sapiens
-
5.3.99.3 seminal vesicle
-
Homo sapiens
-
5.3.99.3 Sertoli cell
-
Homo sapiens
-
5.3.99.3 spermatocyte
-
Homo sapiens
-
5.3.99.3 spermatogonium
-
Homo sapiens
-
5.3.99.3 vas deferens ampulla Homo sapiens
-

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
-
?

Subunits

EC Number Subunits Comment Organism
5.3.99.3 homotrimer
-
Homo sapiens

Synonyms

EC Number Synonyms Comment Organism
5.3.99.3 microsomal prostaglandin E2 synthase-1
-
Homo sapiens
5.3.99.3 mPGES-1
-
Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
5.3.99.3 0.0034
-
pH and temperature not specified in the publication Homo sapiens YS121
5.3.99.3 0.006
-
pH and temperature not specified in the publication Homo sapiens licofelone

Expression

EC Number Organism Comment Expression
5.3.99.3 Homo sapiens the enzyme shows elevated levels in the cartilages and chondrocytes of patients suffering from osteoarthritis. The enzyme is overexpressed in 80% of several cancer cells up