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1.14.99.1: prostaglandin-endoperoxide synthase

This is an abbreviated version!
For detailed information about prostaglandin-endoperoxide synthase, go to the full flat file.

Word Map on EC 1.14.99.1

Reaction

arachidonate
+
reduced acceptor
 + 2 O2 =
prostaglandin H2
 +
acceptor
 +
H2O

Synonyms

(PG)H synthase, COX, COX-1, COX-2, COX1, Cox2, cyclooxygenase, cyclooxygenase 1, cyclooxygenase 2, cyclooxygenase-1, cyclooxygenase-1b, cyclooxygenase-2, cycloxigenase-2, fatty acid cyclooxygenase, hPGHS-1, hPGHS-2, oPGHS-1, PG G/H synthase 2, PG H synthase, PG synthetase, PG-endoperoxide synthase 2, PG-endoperoxide synthetase, PGH-synthase, PGHS, PGHS isoform-1, PGHS-1, PGHS-2, PHS, PHS-1, PHS-2, prostagladin-H synthase, prostaglandin endoperoxide H synthase, prostaglandin endoperoxide H synthase 1, prostaglandin endoperoxide H synthase 2, prostaglandin endoperoxide H synthase-1, prostaglandin endoperoxide H2 synthase-2, prostaglandin endoperoxide synthase, prostaglandin endoperoxide synthase 2, prostaglandin endoperoxide synthase-1, prostaglandin endoperoxide synthase-2, prostaglandin endoperoxide synthetase, prostaglandin G/H synthase, prostaglandin G/H synthase-2, prostaglandin H synthase, prostaglandin H synthase-1, prostaglandin H synthase-2, prostaglandin H2 synthase, prostaglandin H2 synthase-1, prostaglandin synthase, prostaglandin synthase-2, prostaglandin synthetase, prostaglandin-endoperoxide synthase, prostaglandin-endoperoxide synthase 1, prostaglandin-endoperoxide synthase 2, prostaglandin-H-synthase, prostaglandin-H-synthase 1, prostaglandin-H-synthase 2, PTGS 2, PTGS-1, PTGS-2, PTGS1, PTGS2, putative cyclooxygenase-3, synthase, prostaglandin, tPGHS-1, tPGHS-2

ECTree

     1 Oxidoreductases
         1.14 Acting on paired donors, with incorporation or reduction of molecular oxygen
             1.14.99 Miscellaneous
                1.14.99.1 prostaglandin-endoperoxide synthase

Engineering

Engineering on EC 1.14.99.1 - prostaglandin-endoperoxide synthase

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PROTEIN VARIANTS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
C299S/C526S
-
mutant, relative activity: 70%
cyclooxygenase-1bdeltaG
-
mutant, in which the frame shift in the splice variant human cyclooxygenase-1b is corrected
E488G
-
site-directed mutagenesis, the mutant shows reduced sensitivity to the cyclooxygenase inhibitor nimesulide compared to the wild-type enzyme. The activity with eicosapentaenoate is altered
F59C
-
mutant, relative activity: 50%
F66C
-
mutant, relative activity: 50%
F84C
-
mutant, relative activity: 50%
G587R
-
site-directed mutagenesis, the mutant shows reduced sensitivity to the cyclooxygenase inhibitor nimesulide compared to the wild-type enzyme. The activity with eicosapentaenoate is not affected
G83C
-
mutant, relative activity: 35%
H75C
-
mutant, relative activity: 70%
I63C
-
mutant, relative activity: 70%
I77C
-
mutant, relative activity: 60%
K211A
-
complete abolition of activity
K211A/K215A
-
complete abolition of activity
K211A/K215A/K222A
-
complete abolition of activity
K211A/K222A
-
complete abolition of activity
K211E
-
complete abolition of activity
K211E/K215E
-
complete abolition of activity
K211E/K215E/K222E
-
complete abolition of activity
K211E/K222E
-
complete abolition of activity
K215A
-
does not impair PGHS activity
K215A/K222A
-
significant reduction of 27% of the activity
K215E
-
does not impair PGHS activity
K215E/K222E
-
significant reduction of 58% of the activity
K222A
-
no significant reduction of activity
K222E
-
no significant reduction of activity
K64C
-
mutant, relative activity: 70%
L60C
-
mutant, relative activity: 70%
L65C
-
mutant, relative activity: 70%
L67C
-
mutant, relative activity: 40%
L78C
-
mutant, relative activity: 30%
N382A
-
mutation has little effect on the cyclooxygenase specific activity or activation efficiency but almost doubles the cyclooxygenase catalytic output before self-inactivation
N382D
-
mutation has little effect on the cyclooxygenase specific activity or activation efficiency but almost doubles the cyclooxygenase catalytic output before self-inactivation
N382L
-
mutation has little effect on the cyclooxygenase specific activity or activation efficiency but almost doubles the cyclooxygenase catalytic output before self-inactivation
N72C
-
mutant, relative activity: 60%
N86C
-
mutant, relative activity: 50%
N89C
-
mutant, relative activity: 30%
N90C
-
mutant, relative activity: 20%
R228H
-
site-directed mutagenesis, the mutant shows reduced sensitivity to the cyclooxygenase inhibitor nimesulide compared to the wild-type enzyme. The activity with eicosapentaenoate is not affected
R62C
-
mutant, relative activity: 50%
S516M
-
mutation mimics acetylation of Ser516, mutant still sensitive to most inhibitors, not: diclofenac, meclofenamic acid
T61C
-
mutant, relative activity: 60%
T73C
-
mutant, relative activity: 40%
V511A
-
site-directed mutagenesis, the mutant shows reduced sensitivity to the cyclooxygenase inhibitor nimesulide compared to the wild-type enzyme. The activity with eicosapentaenoate altered
V74C
-
mutant, relative activity: 60%
V87C
-
mutant, relative activity: 30%
V88C
-
mutant, relative activity: 30%
W85C
-
mutant, relative activity: 10%
Y148F
-
mutant enzyme has cyclooxygenase activity comparable to that of the native enzyme
Y148F/Y348F/Y385F/Y404F/Y504F
-
no cyclooxygenase activity detected
Y148F/Y348F/Y404F/Y504F
-
mutant enzyme has specific cyclooxygenase activity approximately half that of native enzyme. Modest increase in cyclooxygenase self-inactivation rate, 2.3fold
Y348F
Y348F/Y504F
-
mutant
Y385F
-
no cyclooxygenase activity detected
Y404F
-
mutant enzyme has cyclooxygenase activity comparable to that of the native enzyme. Modest increase in cyclooxygenase self-inactivation rate, 2.3fold
Y504F
Y76C
-
mutant, relative activity: 70%
L531A
site-directed mutagenesis, the mutant shows reduced Vmax and Km with arachidonate compared to the wild-type COX-2
L531F
site-directed mutagenesis, the mutant shows reduced Vmax and Km with arachidonate compared to the wild-type COX-2
L531P
site-directed mutagenesis, the mutant shows reduced Vmax and Km with arachidonate compared to the wild-type COX-2
L531T
site-directed mutagenesis, the mutant shows reduced Vmax and Km with arachidonate compared to the wild-type COX-2
N580A
site-directed mutagenesis, crystal structure determination with bound substrates, overview
Arg120Glu
-
Arg120 important for interaction with substrate and with inhibitors containing a free carboxylic acid moiety
Cys313Ser
-
cyclooxygenase and peroxidase activity reduced by 80-90%, no significant effect on inhibition, dimer formation, glycosylation
Cys540Ser
-
cyclooxygenase and peroxidase activity reduced by 80-90%, no significant effect on inhibition, dimer formation, glycosylation