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Understanding microscopic binding of human microsomal prostaglandin E synthase-1 (mPGES-1) trimer with substrate PGH2 and cofactor GSH: insights from computational alanine scanning and site-directed mutagenesis

Hamza, A.; Tong, M.; AbdulHameed, M.D.; Liu, J.; Goren, A.C.; Tai, H.H.; Zhan, C.G.; J. Phys. Chem. B 114, 5605-5616 (2010)

Data extracted from this reference:

Cloned(Commentary)
EC Number
Commentary
Organism
5.3.99.3
expressed in 293-F cells
Homo sapiens
Engineering
EC Number
Amino acid exchange
Commentary
Organism
5.3.99.3
H72A
the mutation markedly decreases the mPGES-1 activity (32%)
Homo sapiens
5.3.99.3
N74A
the mutant shows increased Km compared to the wild type enzyme
Homo sapiens
5.3.99.3
R122A
the mutant shows increased Km compared to the wild type enzyme
Homo sapiens
5.3.99.3
R70A
the mutant shows increased Km compared to the wild type enzyme
Homo sapiens
5.3.99.3
R70A/R122A
the mutant shows increased Km compared to the wild type enzyme, the double mutant of the mPGES-1 significantly reduces the binding affinity of GSH
Homo sapiens
5.3.99.3
T129V
the mutant shows increased Km compared to the wild type enzyme
Homo sapiens
5.3.99.3
Y117A
the mutant shows increased Km compared to the wild type enzyme
Homo sapiens
5.3.99.3
Y117F
the mutant still maintains full catalytic activity relative to the wild type
Homo sapiens
5.3.99.3
Y117S
the mutant shows increased Km compared to the wild type enzyme
Homo sapiens
KM Value [mM]
EC Number
KM Value [mM]
KM Value Maximum [mM]
Substrate
Commentary
Organism
Structure
5.3.99.3
0.215
-
prostaglandin H2
wild type enzyme
Homo sapiens
5.3.99.3
0.2832
-
prostaglandin H2
mutant enzyme Y117S
Homo sapiens
5.3.99.3
0.296
-
prostaglandin H2
mutant enzyme R70A
Homo sapiens
5.3.99.3
0.372
-
prostaglandin H2
mutant enzyme R122A
Homo sapiens
5.3.99.3
0.3842
-
prostaglandin H2
mutant enzyme T129V
Homo sapiens
5.3.99.3
0.4643
-
prostaglandin H2
mutant enzyme N74A
Homo sapiens
5.3.99.3
0.4737
-
prostaglandin H2
mutant enzyme R70A/R122A
Homo sapiens
5.3.99.3
0.5345
-
prostaglandin H2
mutant enzyme Y117A
Homo sapiens
Localization
EC Number
Localization
Commentary
Organism
GeneOntology No.
Textmining
5.3.99.3
microsome
-
Homo sapiens
-
-
Organism
EC Number
Organism
Primary Accession No. (UniProt)
Commentary
Textmining
5.3.99.3
Homo sapiens
O14684
-
-
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
-
705347
Homo sapiens
Prostaglandin E2
-
-
-
?
Subunits
EC Number
Subunits
Commentary
Organism
5.3.99.3
trimer
-
Homo sapiens
Cofactor
EC Number
Cofactor
Commentary
Organism
Structure
5.3.99.3
glutathione
-
Homo sapiens
Cloned(Commentary) (protein specific)
EC Number
Commentary
Organism
5.3.99.3
expressed in 293-F cells
Homo sapiens
Cofactor (protein specific)
EC Number
Cofactor
Commentary
Organism
Structure
5.3.99.3
glutathione
-
Homo sapiens
Engineering (protein specific)
EC Number
Amino acid exchange
Commentary
Organism
5.3.99.3
H72A
the mutation markedly decreases the mPGES-1 activity (32%)
Homo sapiens
5.3.99.3
N74A
the mutant shows increased Km compared to the wild type enzyme
Homo sapiens
5.3.99.3
R122A
the mutant shows increased Km compared to the wild type enzyme
Homo sapiens
5.3.99.3
R70A
the mutant shows increased Km compared to the wild type enzyme
Homo sapiens
5.3.99.3
R70A/R122A
the mutant shows increased Km compared to the wild type enzyme, the double mutant of the mPGES-1 significantly reduces the binding affinity of GSH
Homo sapiens
5.3.99.3
T129V
the mutant shows increased Km compared to the wild type enzyme
Homo sapiens
5.3.99.3
Y117A
the mutant shows increased Km compared to the wild type enzyme
Homo sapiens
5.3.99.3
Y117F
the mutant still maintains full catalytic activity relative to the wild type
Homo sapiens
5.3.99.3
Y117S
the mutant shows increased Km compared to the wild type enzyme
Homo sapiens
KM Value [mM] (protein specific)
EC Number
KM Value [mM]
KM Value Maximum [mM]
Substrate
Commentary
Organism
Structure
5.3.99.3
0.215
-
prostaglandin H2
wild type enzyme
Homo sapiens
5.3.99.3
0.2832
-
prostaglandin H2
mutant enzyme Y117S
Homo sapiens
5.3.99.3
0.296
-
prostaglandin H2
mutant enzyme R70A
Homo sapiens
5.3.99.3
0.372
-
prostaglandin H2
mutant enzyme R122A
Homo sapiens
5.3.99.3
0.3842
-
prostaglandin H2
mutant enzyme T129V
Homo sapiens
5.3.99.3
0.4643
-
prostaglandin H2
mutant enzyme N74A
Homo sapiens
5.3.99.3
0.4737
-
prostaglandin H2
mutant enzyme R70A/R122A
Homo sapiens
5.3.99.3
0.5345
-
prostaglandin H2
mutant enzyme Y117A
Homo sapiens
Localization (protein specific)
EC Number
Localization
Commentary
Organism
GeneOntology No.
Textmining
5.3.99.3
microsome
-
Homo sapiens
-
-
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
-
705347
Homo sapiens
Prostaglandin E2
-
-
-
?
Subunits (protein specific)
EC Number
Subunits
Commentary
Organism
5.3.99.3
trimer
-
Homo sapiens