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Literature summary extracted from
- Different hydrolases involved in bioactivation of prodrug-type angiotensin receptor blockers: carboxymethylenebutenolidase and carboxylesterase 1 (2013), Drug Metab. Dispos., 41, 1888-1895.
KM Value [mM]
| EC Number | KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|---|
| 3.1.1.45 | additional information | - |
additional information | Michaelis-Menten kinetics | Macaca fascicularis | |
| 3.1.1.45 | additional information | - |
additional information | Michaelis-Menten kinetics | Homo sapiens | |
| 3.1.1.45 | additional information | - |
additional information | Michaelis-Menten kinetics | Mus musculus | |
| 3.1.1.45 | additional information | - |
additional information | Michaelis-Menten kinetics | Rattus norvegicus | |
| 3.1.1.45 | additional information | - |
additional information | Michaelis-Menten kinetics | Canis lupus familiaris |
Localization
| EC Number | Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|---|---|---|---|---|
| 3.1.1.45 | cytosol | - |
Macaca fascicularis | 5829 | - |
| 3.1.1.45 | cytosol | - |
Homo sapiens | 5829 | - |
| 3.1.1.45 | cytosol | - |
Mus musculus | 5829 | - |
| 3.1.1.45 | cytosol | - |
Rattus norvegicus | 5829 | - |
| 3.1.1.45 | cytosol | - |
Canis lupus familiaris | 5829 | - |
| 3.1.1.45 | microsome | - |
Macaca fascicularis | - |
- |
| 3.1.1.45 | microsome | - |
Homo sapiens | - |
- |
| 3.1.1.45 | microsome | - |
Mus musculus | - |
- |
| 3.1.1.45 | microsome | - |
Rattus norvegicus | - |
- |
| 3.1.1.45 | microsome | - |
Canis lupus familiaris | - |
- |
Natural Substrates/ Products (Substrates)
| EC Number | Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|---|
| 3.1.1.45 | azilsartan medoxomil + H2O | Macaca fascicularis | - |
azilsartan + ? | - |
? |  |
| 3.1.1.45 | azilsartan medoxomil + H2O | Homo sapiens | - |
azilsartan + ? | - |
? | |
| 3.1.1.45 | azilsartan medoxomil + H2O | Mus musculus | - |
azilsartan + ? | - |
? | |
| 3.1.1.45 | azilsartan medoxomil + H2O | Rattus norvegicus | - |
azilsartan + ? | - |
? | |
| 3.1.1.45 | azilsartan medoxomil + H2O | Canis lupus familiaris | - |
azilsartan + ? | - |
? | |
| 3.1.1.45 | azilsartan medoxomil + H2O | Rattus norvegicus Sprague-Dawley | - |
azilsartan + ? | - |
? | |
| 3.1.1.45 | candesartan cilexetil + H2O | Macaca fascicularis | - |
candesartan + ? | - |
? | |
| 3.1.1.45 | candesartan cilexetil + H2O | Homo sapiens | - |
candesartan + ? | - |
? | |
| 3.1.1.45 | candesartan cilexetil + H2O | Mus musculus | - |
candesartan + ? | - |
? | |
| 3.1.1.45 | candesartan cilexetil + H2O | Rattus norvegicus | - |
candesartan + ? | - |
? | |
| 3.1.1.45 | candesartan cilexetil + H2O | Canis lupus familiaris | - |
candesartan + ? | - |
? | |
| 3.1.1.45 | candesartan cilexetil + H2O | Rattus norvegicus Sprague-Dawley | - |
candesartan + ? | - |
? | |
| 3.1.1.45 | additional information | Macaca fascicularis | the activity with prodrug-type angiotensin II type 1 receptor blocker differs in a tissue-dependent and subcellular-dependent manner, overview | ? | - |
? | |
| 3.1.1.45 | additional information | Homo sapiens | the activity with prodrug-type angiotensin II type 1 receptor blocker differs in a tissue-dependent and subcellular-dependent manner, overview | ? | - |
? | |
| 3.1.1.45 | additional information | Mus musculus | the activity with prodrug-type angiotensin II type 1 receptor blocker differs in a tissue-dependent and subcellular-dependent manner, overview | ? | - |
? | |
| 3.1.1.45 | additional information | Rattus norvegicus | the activity with prodrug-type angiotensin II type 1 receptor blocker differs in a tissue-dependent and subcellular-dependent manner, overview | ? | - |
? | |
| 3.1.1.45 | additional information | Canis lupus familiaris | the activity with prodrug-type angiotensin II type 1 receptor blocker differs in a tissue-dependent and subcellular-dependent manner, overview | ? | - |
? | |
| 3.1.1.45 | additional information | Rattus norvegicus Sprague-Dawley | the activity with prodrug-type angiotensin II type 1 receptor blocker differs in a tissue-dependent and subcellular-dependent manner, overview | ? | - |
? | |
| 3.1.1.45 | olmesartan medoxomil + H2O | Macaca fascicularis | - |
olmesartan + diacetyl | - |
? | |
| 3.1.1.45 | olmesartan medoxomil + H2O | Homo sapiens | - |
olmesartan + diacetyl | - |
? | |
| 3.1.1.45 | olmesartan medoxomil + H2O | Mus musculus | - |
olmesartan + diacetyl | - |
? | |
| 3.1.1.45 | olmesartan medoxomil + H2O | Rattus norvegicus | - |
olmesartan + diacetyl | - |
? | |
| 3.1.1.45 | olmesartan medoxomil + H2O | Canis lupus familiaris | - |
olmesartan + diacetyl | - |
? | |
| 3.1.1.45 | olmesartan medoxomil + H2O | Rattus norvegicus Sprague-Dawley | - |
olmesartan + diacetyl | - |
? | |
Organism
| EC Number | Organism | UniProt | Comment | Textmining |
|---|---|---|---|---|
| 3.1.1.45 | Canis lupus familiaris | E2RF91 | male beagle dogs | - |
| 3.1.1.45 | Homo sapiens | Q96DG6 | - |
- |
| 3.1.1.45 | Macaca fascicularis | - |
male cynomolgus monkey | - |
| 3.1.1.45 | Mus musculus | Q8R1G2 | - |
- |
| 3.1.1.45 | Rattus norvegicus | Q7TP52 | - |
- |
| 3.1.1.45 | Rattus norvegicus Sprague-Dawley | Q7TP52 | - |
- |
Source Tissue
| EC Number | Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|---|
| 3.1.1.45 | intestine | - |
Macaca fascicularis | - |
| 3.1.1.45 | intestine | - |
Homo sapiens | - |
| 3.1.1.45 | intestine | - |
Mus musculus | - |
| 3.1.1.45 | intestine | - |
Rattus norvegicus | - |
| 3.1.1.45 | intestine | - |
Canis lupus familiaris | - |
| 3.1.1.45 | kidney | - |
Homo sapiens | - |
| 3.1.1.45 | kidney | - |
Mus musculus | - |
| 3.1.1.45 | kidney | - |
Rattus norvegicus | - |
| 3.1.1.45 | kidney | - |
Canis lupus familiaris | - |
| 3.1.1.45 | kidney | high enzyme activity | Macaca fascicularis | - |
| 3.1.1.45 | liver | - |
Homo sapiens | - |
| 3.1.1.45 | liver | - |
Mus musculus | - |
| 3.1.1.45 | liver | - |
Rattus norvegicus | - |
| 3.1.1.45 | liver | - |
Canis lupus familiaris | - |
| 3.1.1.45 | liver | very high enzyme activity | Macaca fascicularis | - |
| 3.1.1.45 | lung | - |
Macaca fascicularis | - |
| 3.1.1.45 | lung | - |
Homo sapiens | - |
| 3.1.1.45 | lung | - |
Mus musculus | - |
| 3.1.1.45 | lung | - |
Rattus norvegicus | - |
| 3.1.1.45 | lung | low enzyme level in the cytosol | Canis lupus familiaris | - |
Substrates and Products (Substrate)
| EC Number | Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|---|
| 3.1.1.45 | azilsartan medoxomil + H2O | - |
Macaca fascicularis | azilsartan + ? | - |
? | |
| 3.1.1.45 | azilsartan medoxomil + H2O | - |
Homo sapiens | azilsartan + ? | - |
? | |
| 3.1.1.45 | azilsartan medoxomil + H2O | - |
Mus musculus | azilsartan + ? | - |
? | |
| 3.1.1.45 | azilsartan medoxomil + H2O | - |
Rattus norvegicus | azilsartan + ? | - |
? | |
| 3.1.1.45 | azilsartan medoxomil + H2O | - |
Canis lupus familiaris | azilsartan + ? | - |
? | |
| 3.1.1.45 | azilsartan medoxomil + H2O | - |
Rattus norvegicus Sprague-Dawley | azilsartan + ? | - |
? | |
| 3.1.1.45 | candesartan cilexetil + H2O | - |
Macaca fascicularis | candesartan + ? | - |
? | |
| 3.1.1.45 | candesartan cilexetil + H2O | - |
Homo sapiens | candesartan + ? | - |
? | |
| 3.1.1.45 | candesartan cilexetil + H2O | - |
Mus musculus | candesartan + ? | - |
? | |
| 3.1.1.45 | candesartan cilexetil + H2O | - |
Rattus norvegicus | candesartan + ? | - |
? | |
| 3.1.1.45 | candesartan cilexetil + H2O | - |
Canis lupus familiaris | candesartan + ? | - |
? | |
| 3.1.1.45 | candesartan cilexetil + H2O | - |
Rattus norvegicus Sprague-Dawley | candesartan + ? | - |
? | |
| 3.1.1.45 | additional information | the activity with prodrug-type angiotensin II type 1 receptor blocker differs in a tissue-dependent and subcellular-dependent manner, overview | Macaca fascicularis | ? | - |
? | |
| 3.1.1.45 | additional information | the activity with prodrug-type angiotensin II type 1 receptor blocker differs in a tissue-dependent and subcellular-dependent manner, overview | Homo sapiens | ? | - |
? | |
| 3.1.1.45 | additional information | the activity with prodrug-type angiotensin II type 1 receptor blocker differs in a tissue-dependent and subcellular-dependent manner, overview | Mus musculus | ? | - |
? | |
| 3.1.1.45 | additional information | the activity with prodrug-type angiotensin II type 1 receptor blocker differs in a tissue-dependent and subcellular-dependent manner, overview | Rattus norvegicus | ? | - |
? | |
| 3.1.1.45 | additional information | the activity with prodrug-type angiotensin II type 1 receptor blocker differs in a tissue-dependent and subcellular-dependent manner, overview | Canis lupus familiaris | ? | - |
? | |
| 3.1.1.45 | additional information | the activity with prodrug-type angiotensin II type 1 receptor blocker differs in a tissue-dependent and subcellular-dependent manner, overview | Rattus norvegicus Sprague-Dawley | ? | - |
? | |
| 3.1.1.45 | olmesartan medoxomil + H2O | - |
Macaca fascicularis | olmesartan + diacetyl | - |
? | |
| 3.1.1.45 | olmesartan medoxomil + H2O | - |
Homo sapiens | olmesartan + diacetyl | - |
? | |
| 3.1.1.45 | olmesartan medoxomil + H2O | - |
Mus musculus | olmesartan + diacetyl | - |
? | |
| 3.1.1.45 | olmesartan medoxomil + H2O | - |
Rattus norvegicus | olmesartan + diacetyl | - |
? | |
| 3.1.1.45 | olmesartan medoxomil + H2O | - |
Canis lupus familiaris | olmesartan + diacetyl | - |
? | |
| 3.1.1.45 | olmesartan medoxomil + H2O | - |
Rattus norvegicus Sprague-Dawley | olmesartan + diacetyl | - |
? | |
Synonyms
| EC Number | Synonyms | Comment | Organism |
|---|---|---|---|
| 3.1.1.45 | CMBL | - |
Macaca fascicularis |
| 3.1.1.45 | CMBL | - |
Homo sapiens |
| 3.1.1.45 | CMBL | - |
Mus musculus |
| 3.1.1.45 | CMBL | - |
Rattus norvegicus |
| 3.1.1.45 | CMBL | - |
Canis lupus familiaris |
Temperature Optimum [°C]
| EC Number | Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|---|
| 3.1.1.45 | 37 | - |
assay at | Macaca fascicularis |
| 3.1.1.45 | 37 | - |
assay at | Homo sapiens |
| 3.1.1.45 | 37 | - |
assay at | Mus musculus |
| 3.1.1.45 | 37 | - |
assay at | Rattus norvegicus |
| 3.1.1.45 | 37 | - |
assay at | Canis lupus familiaris |
pH Optimum
| EC Number | pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|---|
| 3.1.1.45 | 7.4 | - |
assay at | Macaca fascicularis |
| 3.1.1.45 | 7.4 | - |
assay at | Homo sapiens |
| 3.1.1.45 | 7.4 | - |
assay at | Mus musculus |
| 3.1.1.45 | 7.4 | - |
assay at | Rattus norvegicus |
| 3.1.1.45 | 7.4 | - |
assay at | Canis lupus familiaris |
General Information
| EC Number | General Information | Comment | Organism |
|---|---|---|---|
| 3.1.1.45 | physiological function | the carboxymethylenebutenolidase homologue is the enzyme responsible for bioactivation of olmesartan medoxomil, prodrug-type angiotensin II type 1 receptor blocker, and also of other prodrug-type angiotensin II type 1 receptor blockers, candesartan cilexetil and azilsartan medoxomil | Mus musculus |
| 3.1.1.45 | physiological function | the carboxymethylenebutenolidase homologue is the enzyme responsible in humans for bioactivation of olmesartan medoxomil, prodrug-type angiotensin II type 1 receptor blocker, and also of other prodrug-type angiotensin II type 1 receptor blockers, candesartan cilexetil and azilsartan medoxomil | Macaca fascicularis |
| 3.1.1.45 | physiological function | the carboxymethylenebutenolidase homologue is the enzyme responsible in humans for bioactivation of olmesartan medoxomil, prodrug-type angiotensin II type 1 receptor blocker, and also of other prodrug-type angiotensin II type 1 receptor blockers, candesartan cilexetil and azilsartan medoxomil | Homo sapiens |
| 3.1.1.45 | physiological function | the carboxymethylenebutenolidase homologue is the enzyme responsible in humans for bioactivation of olmesartan medoxomil, prodrug-type angiotensin II type 1 receptor blocker, and also of other prodrug-type angiotensin II type 1 receptor blockers, candesartan cilexetil and azilsartan medoxomil | Rattus norvegicus |
| 3.1.1.45 | physiological function | the carboxymethylenebutenolidase homologue is the enzyme responsible in humans for bioactivation of olmesartan medoxomil, prodrug-type angiotensin II type 1 receptor blocker, and also of other prodrug-type angiotensin II type 1 receptor blockers, candesartan cilexetil and azilsartan medoxomil | Canis lupus familiaris |
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