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Literature summary for 3.1.1.1 extracted from
- Functional analysis of carboxylesterase in human induced pluripotent stem cell-derived enterocytes (2017), Biochem. Biophys. Res. Commun., 486, 143-148 .
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 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 |  |
| 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)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| acetylsalicylic acid + H2O | Homo sapiens | CES2A1-specific substrate | acetate + salicylate | - |
? | |
| monoethylglycylxylidine + H2O | Homo sapiens | CES1A-specific substrate | 2,6-xylidene + N-ethylglycine | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
| Homo sapiens | Q6LAP9 | CES1A1 | - |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| Caco-2 cell | - |
Homo sapiens | - |
| enterocyte | induced pluripotent stem cell-derived enterocytes | Homo sapiens | - |
| epithelial cell | primary human intestinal epithelial cells | Homo sapiens | - |
| additional information | expression patterns of carboxylesterase isozymes CES2A1 and CES1A in Caco-2 cells differ from those in the human small intestine | Homo sapiens | - |
| 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 | - |
| pluripotent stem cell | induced pluripotent stem cell | Homo sapiens | - |
| small intestine | - |
Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| 4-nitrophenol acetate + H2O | - |
Homo sapiens | 4-nitrophenol + acetate | - |
? | |
| 4-nitrophenyl acetate + H2O | - |
Homo sapiens | 4-nitrophenol + acetate | - |
? | |
| acetylsalicylic acid + H2O | CES2A1-specific substrate | Homo sapiens | acetate + salicylate | - |
? | |
| lidocaine + H2O | the CES1A substrate lidocaine is metabolized to 2,6-xylidine via a MEGX intermediate | Homo sapiens | 2,6-xylidine + N,N-diethylglycine | - |
? | |
| monoethylglycylxylidine + H2O | CES1A-specific substrate | Homo sapiens | 2,6-xylidene + N-ethylglycine | - |
? | |
| 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
| Synonyms | Comment | Organism |
|---|---|---|
| CES | - |
Homo sapiens |
| CES1A | - |
Homo sapiens |
| CES2A1 | - |
Homo sapiens |
Temperature Optimum [°C]
| Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|
| 37 | - |
assay at | Homo sapiens |
pH Optimum
| pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|
| 7.4 | - |
assay at | Homo sapiens |
General Information
| General Information | Comment | Organism |
|---|---|---|
| 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 |
| 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 |
| 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 |
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