Literature summary for 5.3.99.3 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.

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Cloned(Commentary)

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

Inhibitors

Inhibitors	Comment	Organism	Structure
indomethacin	-	Homo sapiens
indomethacin	-	Rattus norvegicus
MK-886	-	Homo sapiens
MK-886	-	Rattus norvegicus
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
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
SC-236	-	Homo sapiens
SC-236	-	Rattus norvegicus

Localization

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

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	-	-	-
Rattus norvegicus	-	-	-

Substrates and Products (Substrate)

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

Synonyms

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

IC50 Value

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

General Information

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

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Release 2023.1 (January 2023)