BRENDA - Enzyme Database show

Distinction of microsomal prostaglandin E synthase-1 (mPGES-1) inhibition from cyclooxygenase-2 inhibition in cells using a novel, selective mPGES-1 inhibitor

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.; Biochem. Pharmacol. 79, 1445-1454 (2010)

Data extracted from this reference:

Cloned(Commentary)
EC Number
Commentary
Organism
5.3.99.3
expressed in Escherichia coli BL21(DE3) cells
Homo sapiens
Inhibitors
EC Number
Inhibitors
Commentary
Organism
Structure
5.3.99.3
indomethacin
-
Homo sapiens
5.3.99.3
indomethacin
-
Rattus norvegicus
5.3.99.3
MK-886
-
Rattus norvegicus
5.3.99.3
MK-886
-
Homo sapiens
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
Commentary
Organism
GeneOntology No.
Textmining
5.3.99.3
microsome
-
Homo sapiens
-
-
5.3.99.3
microsome
-
Rattus norvegicus
-
-
Organism
EC Number
Organism
Primary Accession No. (UniProt)
Commentary
Textmining
5.3.99.3
Homo sapiens
-
-
-
5.3.99.3
Rattus norvegicus
-
-
-
Substrates and Products (Substrate)
EC Number
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
5.3.99.3
Prostaglandin H2
-
702165
Homo sapiens
Prostaglandin E2
-
-
-
?
5.3.99.3
Prostaglandin H2
-
702165
Rattus norvegicus
Prostaglandin E2
-
-
-
?
IC50 Value
EC Number
IC50 Value
IC50 Value Maximum
Commentary
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
Cloned(Commentary) (protein specific)
EC Number
Commentary
Organism
5.3.99.3
expressed in Escherichia coli BL21(DE3) cells
Homo sapiens
IC50 Value (protein specific)
EC Number
IC50 Value
IC50 Value Maximum
Commentary
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
Inhibitors (protein specific)
EC Number
Inhibitors
Commentary
Organism
Structure
5.3.99.3
indomethacin
-
Homo sapiens
5.3.99.3
indomethacin
-
Rattus norvegicus
5.3.99.3
MK-886
-
Rattus norvegicus
5.3.99.3
MK-886
-
Homo sapiens
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 (protein specific)
EC Number
Localization
Commentary
Organism
GeneOntology No.
Textmining
5.3.99.3
microsome
-
Homo sapiens
-
-
5.3.99.3
microsome
-
Rattus norvegicus
-
-
Substrates and Products (Substrate) (protein specific)
EC Number
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
5.3.99.3
Prostaglandin H2
-
702165
Homo sapiens
Prostaglandin E2
-
-
-
?
5.3.99.3
Prostaglandin H2
-
702165
Rattus norvegicus
Prostaglandin E2
-
-
-
?
General Information
EC Number
General Information
Commentary
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
General Information (protein specific)
EC Number
General Information
Commentary
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