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Literature summary extracted from

  • Kabeya, T.; Matsumura, W.; Iwao, T.; Hosokawa, M.; Matsunaga, T.
    Functional analysis of carboxylesterase in human induced pluripotent stem cell-derived enterocytes (2017), Biochem. Biophys. Res. Commun., 486, 143-148 .
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.1.1.1 Digitonin specifically inhibits isozyme CES1A. The metabolism of MEGX to 2,6-xylidine is inhibited by the CES1A inhibitor digitonin in Caco-2 cells Homo sapiens
3.1.1.1 telmisartan 4-nitrophenyl acetate hydrolysis in human iPS cell-derived enterocytes is significantly inhibited by the CES2A1-specific inhibitor telmisartan 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 acetylsalicylic acid + H2O Homo sapiens CES2A1-specific substrate acetate + salicylate
-
?
3.1.1.1 monoethylglycylxylidine + H2O Homo sapiens CES1A-specific substrate 2,6-xylidene + N-ethylglycine
-
?

Organism

EC Number Organism UniProt Comment Textmining
3.1.1.1 Homo sapiens
-
-
-
3.1.1.1 Homo sapiens Q6LAP9 CES1A1
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.1.1.1 Caco-2 cell
-
Homo sapiens
-
3.1.1.1 enterocyte induced pluripotent stem cell-derived enterocytes Homo sapiens
-
3.1.1.1 epithelial cell primary human intestinal epithelial cells Homo sapiens
-
3.1.1.1 additional information expression patterns of carboxylesterase isozymes CES2A1 and CES1A in Caco-2 cells differ from those in the human small intestine Homo sapiens
-
3.1.1.1 additional information expression patterns of carboxylesterase isozymes CES2A1 and CES1A in Caco-2 cells differ from those in the human small intestine. Development of a system to evaluate intestinal pharmacokinetics, CES expression and function in human induced pluripotent stem (iPS) cell-derived enterocytes are analyzed. CES2A1 mRNA and protein levels in human iPS cell-derived enterocytes are comparable to Caco-2 cells, whereas CES1A levels are lower in human iPS cell-derived enterocytes compared with Caco-2 cells. The expression and activity of CES isozymes in human iPS cell-derived enterocytes are more similar to the human small intestine compared with Caco-2 cells Homo sapiens
-
3.1.1.1 pluripotent stem cell induced pluripotent stem cell Homo sapiens
-
3.1.1.1 small intestine
-
Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.1.1.1 4-nitrophenol acetate + H2O
-
Homo sapiens 4-nitrophenol + acetate
-
?
3.1.1.1 4-nitrophenyl acetate + H2O
-
Homo sapiens 4-nitrophenol + acetate
-
?
3.1.1.1 acetylsalicylic acid + H2O CES2A1-specific substrate Homo sapiens acetate + salicylate
-
?
3.1.1.1 lidocaine + H2O the CES1A substrate lidocaine is metabolized to 2,6-xylidine via a MEGX intermediate Homo sapiens 2,6-xylidine + N,N-diethylglycine
-
?
3.1.1.1 monoethylglycylxylidine + H2O CES1A-specific substrate Homo sapiens 2,6-xylidene + N-ethylglycine
-
?
3.1.1.1 additional information the CES1A substrate lidocaine is metabolized to 2,6-xylidine via a MEGX intermediate, 2,6-xylidine production is greater with the MEGX substrate than with lidocaine Homo sapiens ?
-
?

Synonyms

EC Number Synonyms Comment Organism
3.1.1.1 CES
-
Homo sapiens
3.1.1.1 CES1A
-
Homo sapiens
3.1.1.1 CES2A1
-
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

General Information

EC Number General Information Comment Organism
3.1.1.1 additional information development of a system to evaluate intestinal pharmacokinetics, CES expression and function in human induced pluripotent stem (iPS) cell-derived enterocytes are analyzed. CES2A1 mRNA and protein levels in human iPS cell-derived enterocytes are comparable to Caco-2 cells, whereas CES1A levels are lower in human iPS cell-derived enterocytes compared with Caco-2 cells. The expression and activity of CES isozymes in human iPS cell-derived enterocytes are more similar to the human small intestine compared with Caco-2 cells Homo sapiens
3.1.1.1 physiological function human carboxylesterase (CES) is a key esterase involved in the metabolism and biotransformation of drugs. Hydrolysis activity in the human small intestine is predominantly mediated by CES2A1 rather than CES1A. In drug development studies, Caco-2 cells are commonly used as a model to predict drug absorption in the human small intestine. But the expression patterns of CES2A1 and CES1A in Caco-2 cells differ from those in the human small intestine Homo sapiens
3.1.1.1 physiological function human carboxylesterase (CES) is a key esterase involved in the metabolism and biotransformation of drugs. Hydrolysis activity in the human small intestine is predominantly mediated by CES2A1 rather than CES1A. In drug development studies, Caco-2 cells are commonly used as a model to predict drug absorption in the human small intestine. But the expression patterns of CES2A1 and CES1A in Caco-2 cells differ from those in the human small intestine. Hydrolysis levels of the CES2A1-specific substrate aspirin were similar in human iPS cell-derived enterocytes and Caco-2 cells, whereas hydrolysis of the CES1A-specific substrate monoethylglycylxylidine is observed in Caco-2 cells but not in human iPS cell-derived enterocytes Homo sapiens