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Literature summary for 3.1.1.1 extracted from

  • Ross, M.K.; Borazjani, A.; Edwards, C.C.; Potter, P.M.
    Hydrolytic metabolism of pyrethroids by human and other mammalian carboxylesterases (2006), Biochem. Pharmacol., 71, 657-669.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
2-chloro-3,4-dimethoxybenzil blocks hydrolysis of trans-permethrin by isoform hCE2 36 times more efficiently than hCE1 Homo sapiens
2-chloro-3,4-dimethoxybenzil blocks hydrolysis of trans-permethrin by isoform hCE2 36 times more efficiently than hCE1 Oryctolagus cuniculus
2-chloro-3,4-dimethoxybenzil blocks hydrolysis of trans-permethrin by isoform hCE2 36 times more efficiently than hCE1 Rattus norvegicus

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.00672
-
bioresmethrin isoform hCE1, pH 7.4, 37°C Homo sapiens
0.00757
-
(1RS)-trans-permethrin isoform hCE2, pH 7.4, 37°C Homo sapiens
0.0086
-
(1RS)-cis-permethrin isoform hCE2, pH 7.4, 37°C Homo sapiens
0.0098
-
(1RS)-trans-permethrin isoform hCE1, pH 7.4, 37°C Homo sapiens
0.0238
-
(1RS)-cis-permethrin isoform hCE1, pH 7.4, 37°C Homo sapiens
1.93
-
(1RS)-cis-permethrin hydrolase A, pH 7.4, 37°C Rattus norvegicus
1.96
-
(1RS)-trans-permethrin pH 7.4, 37°C Oryctolagus cuniculus
4.96
-
(1RS)-cis-permethrin hydrolase B, pH 7.4, 37°C Rattus norvegicus
6.74
-
(1RS)-trans-permethrin hydrolase A, pH 7.4, 37°C Rattus norvegicus
9.8
-
(1RS)-trans-permethrin hydrolase B, pH 7.4, 37°C Rattus norvegicus
16.7
-
(1RS)-cis-permethrin pH 7.4, 37°C Oryctolagus cuniculus
25.75
-
bioresmethrin pH 7.4, 37°C Oryctolagus cuniculus

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
isoforms hCE1 and hCE2
-
Oryctolagus cuniculus
-
-
-
Rattus norvegicus
-
hydrolases A and B
-

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
19.05
-
isoform hCE2, substrate 4-nitrophenyl acetate, pH 7.4, 37°C Homo sapiens
36.14
-
isoform hCE1, substrate 4-nitrophenyl acetate, pH 7.4, 37°C Homo sapiens
86.41
-
substrate 4-nitrophenyl acetate, pH 7.4, 37°C Oryctolagus cuniculus
90.1
-
isoform hCE2, substrate 4-nitrophenyl valerate, pH 7.4, 37°C Homo sapiens
113.2
-
isoform hCE1, substrate 4-nitrophenyl valerate, pH 7.4, 37°C Homo sapiens
126
-
substrate 4-nitrophenyl valerate, pH 7.4, 37°C Oryctolagus cuniculus
293.1
-
isoform hCE1, substrate 4-nitrophenyl butanoate, pH 7.4, 37°C Homo sapiens
315.2
-
isoform hCE2, substrate 4-nitrophenyl butanoate, pH 7.4, 37°C Homo sapiens
374
-
substrate 4-nitrophenyl butanoate, pH 7.4, 37°C Oryctolagus cuniculus

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
(1R)-bioresmethrin + H2O
-
Oryctolagus cuniculus ?
-
?
(1R)-bioresmethrin + H2O substrate for isoform hCE1, not for hCE2 Homo sapiens ?
-
?
(1RS)-cis-permethrin + H2O
-
Rattus norvegicus cis-dichlorochrysamthemic acid + 3-phenoxybenzyl alcohol
-
?
(1RS)-cis-permethrin + H2O
-
Oryctolagus cuniculus cis-dichlorochrysamthemic acid + 3-phenoxybenzyl alcohol
-
?
(1RS)-cis-permethrin + H2O isoforms hCE1 and hCE2 hydrolyze trans-permethrin 8- and 28fold more efficiently than cis-permethrin, resp. Homo sapiens cis-dichlorochrysamthemic acid + 3-phenoxybenzyl alcohol
-
?
(1RS)-trans-permethrin + H2O
-
Rattus norvegicus trans-dichlorochrysamthemic acid + 3-phenoxybenzyl alcohol
-
?
(1RS)-trans-permethrin + H2O
-
Oryctolagus cuniculus trans-dichlorochrysamthemic acid + 3-phenoxybenzyl alcohol
-
?
(1RS)-trans-permethrin + H2O isoforms hCE1 and hCE2 hydrolyze trans-permethrin 8- and 28fold more efficiently than cis-permethrin, resp. Homo sapiens trans-dichlorochrysamthemic acid + 3-phenoxybenzyl alcohol
-
?
4-nitrophenyl acetate + H2O
-
Homo sapiens 4-nitrophenol + acetate
-
?
4-nitrophenyl acetate + H2O
-
Oryctolagus cuniculus 4-nitrophenol + acetate
-
?
4-nitrophenyl butanoate + H2O
-
Homo sapiens 4-nitrophenol + butanoate
-
?
4-nitrophenyl butanoate + H2O
-
Oryctolagus cuniculus 4-nitrophenol + butanoate
-
?
4-nitrophenyl valerate + H2O
-
Homo sapiens 4-nitrophenol + valerate
-
?
4-nitrophenyl valerate + H2O
-
Oryctolagus cuniculus 4-nitrophenol + valerate
-
?
bioresmethrin + H2O
-
Homo sapiens ?
-
?
bioresmethrin + H2O
-
Oryctolagus cuniculus ?
-
?

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.0008
-
(1RS)-trans-permethrin isoform hCE2, pH 7.4, 37°C Homo sapiens
0.0028
-
(1RS)-trans-permethrin isoform hCE1, pH 7.4, 37°C Homo sapiens
0.004
-
(1RS)-cis-permethrin hydrolase A, pH 7.4, 37°C Rattus norvegicus
0.0053
-
(1RS)-cis-permethrin hydrolase B, pH 7.4, 37°C Rattus norvegicus
0.016
-
(1RS)-trans-permethrin pH 7.4, 37°C Oryctolagus cuniculus
0.025
-
(1RS)-trans-permethrin hydrolase B, pH 7.4, 37°C Rattus norvegicus
0.028
-
(1RS)-cis-permethrin isoform hCE2, pH 7.4, 37°C Homo sapiens
0.034
-
bioresmethrin isoform hCE1, pH 7.4, 37°C Homo sapiens
0.036
-
(1RS)-trans-permethrin hydrolase A, pH 7.4, 37°C Rattus norvegicus
0.05
-
(1RS)-cis-permethrin pH 7.4, 37°C Oryctolagus cuniculus
0.056
-
(1RS)-cis-permethrin isoform hCE1, pH 7.4, 37°C Homo sapiens
0.11
-
bioresmethrin pH 7.4, 37°C Oryctolagus cuniculus