Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 3.1.1.1 extracted from

  • Wang, J.; Williams, E.T.; Bourgea, J.; Wong, Y.N.; Patten, C.J.
    Characterization of recombinant human carboxylesterases: fluorescein diacetate as a probe substrate for human carboxylesterase 2 (2011), Drug Metab. Dispos., 39, 1329-1333.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
expressed in baculovirus-infected High Five insect cells Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
bis(4-nitrophenyl)phosphate potent inhibitor Homo sapiens
loperamide inhibitor of isoform CES2 Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.00194
-
fluorescein diacetate isoform CES1-b, in 0.1 M potassium phosphate buffer, pH 7.4, at 37°C Homo sapiens
0.00431
-
fluorescein diacetate isoform CES1-c, in 0.1 M potassium phosphate buffer, pH 7.4, at 37°C Homo sapiens
0.00482
-
fluorescein diacetate isoform CES2, in 0.1 M potassium phosphate buffer, pH 7.4, at 37°C Homo sapiens
0.173
-
4-nitrophenyl acetate isoform CES2, in 0.1 M potassium phosphate buffer, pH 7.4, at 37°C Homo sapiens
0.208
-
4-nitrophenyl acetate isoform CES1-b, in 0.1 M potassium phosphate buffer, pH 7.4, at 37°C Homo sapiens
0.441
-
4-nitrophenyl acetate isoform CES1-c, in 0.1 M potassium phosphate buffer, pH 7.4, at 37°C Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
microsome
-
Homo sapiens
-
-

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
liver CES1-b is the predominant form in human liver Homo sapiens
-
small intestine
-
Homo sapiens
-

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
0.099
-
isoform CES2, using methyl 4-nitrobenzoate as substrate, in 0.1 M potassium phosphate buffer, pH 7.4, at 37°C Homo sapiens
0.281
-
isoform CES1-c, fluorescein diacetate as substrate, in 0.1 M potassium phosphate buffer, pH 7.4, at 37°C Homo sapiens
0.357
-
isoform CES1-b, using fluorescein diacetate as substrate, in 0.1 M potassium phosphate buffer, pH 7.4, at 37°C Homo sapiens
0.68
-
isoform CES1-c, methyl 4-nitrobenzoate as substrate, in 0.1 M potassium phosphate buffer, pH 7.4, at 37°C Homo sapiens
0.682
-
isoform CES2, using 4-nitrophenyl acetate as substrate, in 0.1 M potassium phosphate buffer, pH 7.4, at 37°C Homo sapiens
0.957
-
isoform CES1-b, using methyl 4-nitrobenzoate as substrate, in 0.1 M potassium phosphate buffer, pH 7.4, at 37°C Homo sapiens
1.4
-
isoform CES1-c, using 4-nitrophenyl acetate as substrate, in 0.1 M potassium phosphate buffer, pH 7.4, at 37°C Homo sapiens
1.43
-
isoform CES1-b, using 4-nitrophenyl acetate as substrate, in 0.1 M potassium phosphate buffer, pH 7.4, at 37°C Homo sapiens
13.8
-
isoform CES2, using fluorescein diacetate as substrate, in 0.1 M potassium phosphate buffer, pH 7.4, at 37°C Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
4-nitrophenyl acetate + H2O substrate for both isoform CES1 and CES2 Homo sapiens 4-nitrophenol + acetate
-
?
fluorescein diacetate + H2O specific probe substrate for isoform CES2 Homo sapiens ?
-
?
methyl 4-nitrobenzoate + H2O specific substrate for isoform ES1 Homo sapiens 4-nitrobenzoate + methanol
-
?

Synonyms

Synonyms Comment Organism
carboxylesterase 2
-
Homo sapiens
CES1 isoform Homo sapiens
CES1-b carboxylesterase 1 form b Homo sapiens
CES1-c carboxylesterase 1 form c Homo sapiens
CES2 isoform Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000104
-
isoform CES2, in 0.1 M potassium phosphate buffer, pH 7.4, at 37°C Homo sapiens bis(4-nitrophenyl)phosphate
0.0000236
-
isoform CES1-b, in 0.1 M potassium phosphate buffer, pH 7.4, at 37°C Homo sapiens bis(4-nitrophenyl)phosphate
0.000287
-
isoform CES2, in 0.1 M potassium phosphate buffer, pH 7.4, at 37°C Homo sapiens loperamide
0.000788
-
isoform CES1-c, in 0.1 M potassium phosphate buffer, pH 7.4, at 37°C Homo sapiens bis(4-nitrophenyl)phosphate
0.1
-
IC50 above 0.1 mM, isoform CES1-b, in 0.1 M potassium phosphate buffer, pH 7.4, at 37°C Homo sapiens loperamide
0.1
-
IC50 above 0.1 mM, isoform CES1-c, in 0.1 M potassium phosphate buffer, pH 7.4, at 37°C Homo sapiens loperamide