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3.1.8.1: aryldialkylphosphatase

This is an abbreviated version!
For detailed information about aryldialkylphosphatase, go to the full flat file.

Word Map on EC 3.1.8.1

Reaction

An aryl dialkyl phosphate
+
H2O
=
dialkyl phosphate
 +
an aryl alcohol

Synonyms

A-esterase, A7Q26_23485, aminopeptidase P, AMPP, aryldialkylphosphatase, arylesterase, aryltriphosphatase, bacterial phosphotriesterase, DFPase, diisopropyl fluorophosphatase, esterase B1, esterase E4, esterase, organophosphate, esterase, paraoxon, esterase, pirimiphos-methyloxon, G3C9 rePON1, h-PON1, HAD, haloalkylphosphorus hydrolase, HDL-associated esterase/lactonase paraoxonase 1, HDL-PON1, high activity paraoxonase, high-density lipoprotein-associated esterase/lactonase, human paraoxonase 1, HuPON1, inner membrane protein YiaH, lactonase SsoPox, lactonase/phosphotriesterase, low activity paraoxonase, methyl parathion hydrolase, More, Mph, mPHP, OP hydrolase, OP-hydrolase, OP-hydrolyzing enzyme, OPA anhydrase, opd, OpdA, OpdD, OPH, OPHC2, organophosphate hydrolase, organophosphorous hydrolase, organophosphorus acid anhydrase, organophosphorus hydrolase, organophosphorus pesticide hydrolase, organophosphorus-hydrolyzing enzyme, paraoxon hydrolase, paraoxonase, paraoxonase 1, paraoxonase 1A, paraoxonase 3, paraoxonase-1, paraoxonase-2, paraoxonase1, parathion hydrolase, phosphotriesterase, phosphotriesterase homology protein, phosphotriesterase-like lactonase, PHP, pirimiphos-methyloxon esterase, PLL, PO.ase, PON, PON 1, PON-1, PON-aryl, PON-para, PON1, PON1A, PON2, PON3, POX, PTE, PTE S5, Rv0230c, SACI2140, Saci_2140, SacPox, Sb-PTE, serum paraoxonase, serum paraoxonase 1, SisLac, SisPox, Sso, SSO2522, SsoPox, type A paraoxonase, type B paraoxonase, VmoLac, Vmut2255, VmutPLL

ECTree

     3 Hydrolases
         3.1 Acting on ester bonds
             3.1.8 Phosphoric-triester hydrolases
                3.1.8.1 aryldialkylphosphatase

Inhibitors

Inhibitors on EC 3.1.8.1 - aryldialkylphosphatase

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INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
1,10-phenanthroline
-
7% inhibition at 1 mM
1-(4-chlorophenyl)-4-(dimethylamino)butan-1-ol
-
-
1-biphenyl-4-yl-3-(dimethylamino)propan-1-one
-
-
1-hexynyl diethyl phosphate
-
rapid inactivation, reactiviation by increasing pH
1-hexynyl dimethyl phosphate
-
rapid inactivation, reactiviation by increasing pH
1-hexynyl diphenyl phosphate
-
rapid inactivation, reactiviation by increasing pH
1-myristoyl-lysophosphatidylglycerol
selective, noncompetitive inhibition of paraoxonase activity
1-palmitoyl-lysophosphatidylglycerol
selective, noncompetitive inhibition of paraoxonase activity, charge interactions, inhibition is almost completely suppressed by 1 M NaCl
1-propynyl diethyl phosphate
-
rapid inactivation, reactiviation by increasing pH
1-stearoyl-lysophosphatidylglycerol
selective, noncompetitive inhibition of paraoxonase activity
2-(4-[[2-methoxy-5-(methylsulfonyl)phenyl]carbonyl]piperazin-1-yl)ethanol
-
-
2-hydroxyquinoline
2-propanol
55% residual activity in the presence of 90% (v/v) 2-propanol, after 60 min at 70°C
4-chloromercuribenzoate
-
complete inhibition at 0.1 mM
6,7-dihydroxy-3-(2-methylphenyl)-2H-chromen-2-one
-
noncompetitive
6,7-dihydroxy-3-(3-methylphenyl)-2H-chromen-2-one
-
noncompetitive
6,7-dihydroxy-3-(4-methylphenyl)-2H-chromen-2-one
-
uncompetitive
6,7-dihydroxycoumarin
-
uncompetitive
6-palmityl-ascorbic acid
-
-
7-(4-methylbenzyl)-7H-pyrrolo[3,2-f]quinazoline-1,3-diamine
-
-
acetaminophen
-
at 37°C, 5% slightly reduces activity by 18% concentration
acetone
-
at 37°C, 1 mM reduces activity by 82%
acetonitrile
43% residual activity in the presence of 90% (v/v) acetonitrile, after 60 min at 70°C
acetyl salicylic acid
-
at 37°C, 5% slightly reduces activity by 10% concentration
ascorbate
-
0.5 mM inhibits by ca. 22%. Ascorbate/Cu2+ (0.5 mM/0.001 mM) system shows ca. 63% inactivation
atropine sulfate
-
most potent and significant inhibition, IC50 of 0.041 mg/ml
beta-mercaptoethanol
-
at 37°C, 1 mM reduces activity by 52%
bis(cyclopropylmethyl) phosphoramidate
-
paraoxon analogue with predominant active site binding mode
bis[4-(methylsulfanyl)phenyl] phosphorazidate
-
paraoxon analogue with predominant active site binding mode
Ca2+
5% inhibition at 1 mM
CdCl2
-
60.6% residual activity after 24 h in the presence of 0.02 mg/ml CdCl2
cefazolin
-
inhibits the serum and liver PON1, competitive inhibition
chloramphenicol
-
50% inhibition at 0.0309 mg/ml; inhibits the extracellular and the hepatoma cell enzyme, IC50, overview
Ciprofloxacin
-
IC50 of 0.02175 mg/ml 6 h after the drug application
citalopram
PON1 activity decreases before and after treatment with citalopram compared with control
clarithromycin
-
50% inhibition at 5.121 mg/ml; inhibits the extracellular and the hepatoma cell enzyme, IC50, overview
clindamiycin phosphate
-
IC50 of 0.2395 mg/ml 6 h after the drug application
D-penicillamine
-
20.2% residual activity after 24 h in the presence of 0.2 mg/ml D-penicillamine
dexamethasone
-
most potent and significant inhibition, IC50 of 0.014 mg/ml
dibenzyl phosphoramidate
-
paraoxon analogue with predominant active site binding mode
diclofenac sodium
-
uncompetitive inhibition
diethyl 4-methylbenzylphosphonate
the inhibitor does not bind at the active site, but binds exclusively into a well-defined surface pocket 12 A away from the active site, docking, overview
diethyl dicarbonate
6% residual activity in the presence of 5 mM diethyl dicarbonate, after 30 min at 30°C
diethyl-paraoxon
-
diethyldicarbonate
-
-
diisopropyl methyl phosphonate
-
-
diisopropylfluorophosphate
dimethyl sulfoxide
dimethylformamide
-
at 37°C, 5% completely inhibits activity
dimyristoylphosphatidic acid
0.4 mM, 81% inhibition of arylesterase activity, 64% inhibition of paraoxonase activity
dimyristoylphosphatidylethanol
0.2 mM, 20% inhibition of paraoxonase activity, no effect on arylesterase activity
dimyristoylphosphatidylglycerol
activates the arylesterase activity and inhibits paraoxonase activity
dimyristoylphosphatidylserine
no significant inhibition of both activities up to 0.030 mM, remarkable inhibition of both activities at 0.1–0.4 mM, with a greater inhibition of arylesterase activity
eserine
92% residual activity in the presence of 5 mM eserine, after 30 min at 30°C
ethanol
ethynyl diethyl phosphate
-
rapid inactivation, reactiviation by increasing pH
etomidate
non-competitive inhibitor, PON1 is significantly inhibited by 0.3 mg/kg etomidate for up to 5 min following intravenous administration
Fe2+
-
ascorbate/Fe2+ (0.5 mM/0.002 mM) system shows ca. 27% inactivation after 30 min
Fe3+
-
88% inhibition at 1 mM
fensulfothion
furosemid
-
most potent and significant inhibition, IC50 of 0.235 mg/ml
gentamicin sulfate
gentamycin sulfate
-
inhibits the serum and liver PON1, noncompetitive inhibition
indomethacin
-
competitive inhibition
iodoacetic acid
kanamycin sulfate
-
at 37°C, 0.6 mg/ml reduces activity by 50%
Ketamine
uncompetitive inhibitor, PON1 is significantly inhibited by 1 mg/kg ketamine for up to 5 min following intravenous administration
Ketoprofen
-
noncompetitive inhibition
lincomycine
-
uncompetitive inhibition, weakest inhibitor
lornoxicam
-
uncompetitive inhibition, strongest inhibitor
lysophosphatidylinositol
inhibition of paraoxonase
metamizole sodium
-
IC50 of 26.777 mg/ml
methanol
48% residual activity in the presence of 90% (v/v) methanol, after 60 min at 70°C
methylphosphonic acid
possibly inhibits the enzyme, substrate inhibition
NaCl
76% residual activity in the presence of 2 M NaCl, after 60 min at 70°C
NEM
-
complete inhibition at 0.1 mM
NiCl2
is a non-competitive inhibitor of Co-PTE
nitrilotriacetic acid
-
nitrite
1 mM nitrite inhibits 23% of PON-1 activity, while 6 mM represses 85% of the enzyme activity, the inhibition of PON-1 activity by nitrite is significantly reduced by tryptophan, reduced glutathione, and catalase additions
O,O-dicyclopentylphosphoroamidate
-
substrate analogue, competitive inhibition, binding structure, direct coordination of the phosphoryl oxygen by the active site catalytic calcium ion, overview
o-phenanthroline
-
inactivation
Oxytocin
-
IC50 of 507.72 mg/ml
p-chloromercuribenzoate
23% residual activity in the presence of 5 mM p-chloromercuribenzoate, after 30 min at 30°C
p-hydroxymercuribenzoate
petroleum ether
-
petroleum ether slightly reduces the activity down to 78%
-
phenyl acetate
-
Phenylglyoxal
97% residual activity in the presence of 5 mM phenylglyoxal, after 30 min at 30°C
phenylmethylsulfonyl fluoride
23% residual activity in the presence of 5 mM phenylmethylsulfonyl fluoride, after 30 min at 30°C
phosphatidylinositol
enhances arylesterase activity, but slightly decreases paraoxonase activity
phosphatidylserine
-
-
propofol
competitive inhibitor, PON1 is significantly inhibited by 2 mg/kg propofol for up to 5 min following intravenous administration
rifamycin SV
-
IC50 of 0.00265 mg/ml 6 h after the drug application
SDS
about half of the activity is retained at 1% SDS after incubation for 60 min at 70°C, the addition of 5% SDS completely eliminates the enzyme activity at 70°C
sodium ampicillin
Sodium dodecyl sulfate
-
at 37°C, 5% completely inhibits activity
sodium hypochlorite
-
at 1 mM and in the presence of PBS buffer causes approximately 49% decrease in activity
streptomycin sulfate
-
at 37°C, 0.6 mg/ml reduces activity by 50%
sulfadoxine-trimethoprim
-
IC50 of 15.636 mg/ml
tenoxicam
-
competitive inhibition
toldimfos sodium
-
IC50 of 11.08 mg/ml
Toluene
-
toluene slightly reduces the activity down to 74%
Triton X-100
11% residual activity in the presence of 5% (v/v) Tween 80, after 60 min at 70°C
Tween 80
21% residual activity in the presence of 5% (v/v) Tween 80, after 60 min at 70°C
Urea
88% residual activity in the presence of 8 M urea, after 60 min at 70°C
xylene
-
xylene decreases the enzyme activity by more than 75%
ZnCl2
induces a non-competitive partial inhibition of Zn2+-PTE and Co2+-PTE at pH 8.5. Inhibition of hydrolysis of O,O-(3-chloro-4-methyl-2-oxo-2H-chromen-7-yl)ethylmethylphosphonate is one order of magnitude higher than for paraoxon. Inhibition results from interactions with colloidal Zn(OH)2 formed in alkaline buffer that alters the catalytic machinery. ZnCl2 has an inhibitory effect when a protein environment stabilizes PTE. Adding ZnCl2 to the enzyme stabilized by beta-lactoglobulin results in 10% and 20% decrease in activity for Co-PTE and Zn-PTE, respectively
additional information
-