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Literature summary extracted from

  • Crow, J.A.; Herring, K.L.; Xie, S.; Borazjani, A.; Potter, P.M.; Ross, M.K.
    Inhibition of carboxylesterase activity of THP1 monocytes/macrophages and recombinant human carboxylesterase 1 by oxysterols and fatty acids (2010), Biochim. Biophys. Acta, 1801, 31-41.
    View publication on PubMedView publication on EuropePMC

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.1.1.1 (10Z)-hexadecenoic acid
-
 Homo sapiens
3.1.1.1 (5Z,8Z,11Z,14Z)-eicosatetraenoic acid
-
 Homo sapiens
3.1.1.1 (6Z,9Z,12Z)-octadecatrienoic acid
-
 Homo sapiens
3.1.1.1 (9Z)-octadecenoic acid
-
 Homo sapiens
3.1.1.1 (9Z)-tetradecenoic acid
-
 Homo sapiens
3.1.1.1 (9Z,12Z)-octadecadienoic acid
-
 Homo sapiens
3.1.1.1 11,12-epoxy-(5Z,8Z,14Z)-eicosatrienoic acid
-
 Homo sapiens
3.1.1.1 14,15-epoxy-(5Z,8Z,11Z)-eicosatrienoic acid
-
 Homo sapiens
3.1.1.1 15-deoxy-DELTA12,14-prostaglandin J2
-
 Homo sapiens
3.1.1.1 22(R)-hydroxycholesterol slight inhibition of CES1, not CES2 Homo sapiens
3.1.1.1 24(S),25-epoxycholesterol inhibits only CES1, not CES2 Homo sapiens
3.1.1.1 24(S)-hydroxycholesterol slight inhibition of CES1, not CES2 Homo sapiens
3.1.1.1 25-hydroxycholesterol slight inhibition of CES1, not CES2 Homo sapiens
3.1.1.1 27-Hydroxycholesterol partially noncompetitive inhibitor of recombinant CES1, impaires intracellular CES1 activity following treatment of intact THP1 cells. No inhibition of CES2 Homo sapiens
3.1.1.1 7-oxocholesterol slight inhibition of CES1, not CES2 Homo sapiens
3.1.1.1 arachidonic acid most potent fatty acid inhibitor of recombinant CES1 acting by a noncompetitive mechanism, overview. The inhibition is reversible by bovine serum albumin Homo sapiens
3.1.1.1 benzil inhibition of CES1 in THP-1 cells Homo sapiens
3.1.1.1 bioresmethrin a pyrethroid insecticide Homo sapiens
3.1.1.1 cholesterol slight inhibition of CES1, not CES2 Homo sapiens
3.1.1.1 hexadecanoic acid
-
 Homo sapiens
3.1.1.1 additional information unsaturated fatty acids are better inhibitors of CES1 activity than saturated fatty acids, CES2 activity is unaffected by any fatty acid Homo sapiens
3.1.1.1 octadecanoic acid
-
 Homo sapiens
3.1.1.1 paraoxon inhibition of CES1 in THP-1 cells Homo sapiens
3.1.1.1 prostaglandin E2
-
 Homo sapiens
3.1.1.1 prostaglandin F2alpha
-
 Homo sapiens
3.1.1.1 tetradecanoic acid
-
 Homo sapiens
3.1.1.1 trans-permethrin a pyrethroid insecticide Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
3.1.1.1 additional information Homo sapiens xenobiotic substrates are pyrethroid insecticides ?
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
3.1.1.1 Homo sapiens
-
 isozymes CES1 and CES2
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.1.1.1 liver CES1 and CES2, S9 fraction, HL1220 and HL1274 Homo sapiens
-
3.1.1.1 macrophage CES1, no expression of CES2 Homo sapiens
-
3.1.1.1 monocyte CES1, no expression of CES2 Homo sapiens
-
3.1.1.1 THP-1 cell CES1, no expression of CES2 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.1.1.1 4-nitrophenyl valerate + H2O
-
 Homo sapiens 4-nitrophenol + valerate
-
 ?
3.1.1.1 additional information xenobiotic substrates are pyrethroid insecticides Homo sapiens ?
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.1.1.1 carboxylesterase 1
-
 Homo sapiens
3.1.1.1 CES1
-
 Homo sapiens
3.1.1.1 CES2
-
 Homo sapiens

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
3.1.1.1 37
-
 assay at Homo sapiens

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
3.1.1.1 7.4
-
 assay at Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.1.1.1 additional information
-
 additional information inhibition kinetics Homo sapiens
3.1.1.1 0.00001
-
 27-Hydroxycholesterol pH 7.4, 37°C, recombinant CES1 Homo sapiens
3.1.1.1 0.0018
-
 arachidonic acid pH 7.4, 37°C, recombinant CES1 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.1.1.1 0.000033
-
 pH 7.4, 37°C, recombinant CES1 Homo sapiens 27-Hydroxycholesterol
3.1.1.1 0.002
-
 pH 7.4, 37°C, recombinant CES1 Homo sapiens (5Z,8Z,11Z,14Z)-eicosatetraenoic acid
3.1.1.1 0.007
-
 pH 7.4, 37°C, recombinant CES1 Homo sapiens (9Z)-octadecenoic acid
3.1.1.1 0.007
-
 pH 7.4, 37°C, recombinant CES1 Homo sapiens (10Z)-hexadecenoic acid
3.1.1.1 0.0081
-
 pH 7.4, 37°C, recombinant CES1 Homo sapiens 24(S),25-epoxycholesterol
3.1.1.1 0.009
-
 pH 7.4, 37°C, recombinant CES1 Homo sapiens tetradecanoic acid
3.1.1.1 0.009
-
 pH 7.4, 37°C, recombinant CES1 Homo sapiens (9Z,12Z)-octadecadienoic acid
3.1.1.1 0.012
-
 pH 7.4, 37°C, recombinant CES1 Homo sapiens (9Z)-tetradecenoic acid
3.1.1.1 0.013
-
 pH 7.4, 37°C, recombinant CES1 Homo sapiens 15-deoxy-DELTA12,14-prostaglandin J2
3.1.1.1 0.019
-
 pH 7.4, 37°C, recombinant CES1 Homo sapiens (6Z,9Z,12Z)-octadecatrienoic acid
3.1.1.1 0.025
-
 pH 7.4, 37°C, recombinant CES1 Homo sapiens hexadecanoic acid
3.1.1.1 0.027
-
 pH 7.4, 37°C, recombinant CES1 Homo sapiens 11,12-epoxy-(5Z,8Z,14Z)-eicosatrienoic acid
3.1.1.1 0.038
-
 pH 7.4, 37°C, recombinant CES1 Homo sapiens 14,15-epoxy-(5Z,8Z,11Z)-eicosatrienoic acid
3.1.1.1 0.1
-
 pH 7.4, 37°C, recombinant CES1 Homo sapiens prostaglandin E2
3.1.1.1 0.1
-
 pH 7.4, 37°C, recombinant CES1 Homo sapiens prostaglandin F2alpha
3.1.1.1 0.1
-
 pH 7.4, 37°C, recombinant CES1 Homo sapiens octadecanoic acid