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Literature summary for 3.1.1.45 extracted from
- Interindividual variability of carboxymethylenebutenolidase homolog, a novel olmesartan medoxomil hydrolase, in the human liver and intestine (2013), Drug Metab. Dispos., 41, 1156-1162.
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| recombinant expression of tagged mutant enzymes, semiquantitative tissue-specific expression analysis of wild-type and mutant enzymes | Homo sapiens |
Protein Variants
| Protein Variants | Comment | Organism |
|---|---|---|
| A150T | site-directed mutagenesis, the mutant shows slightly higher Vmax with olmesartan medoxomil compared to the wild-type enzyme | Homo sapiens |
| Y155C | site-directed mutagenesis, the enzyme mutant is caused by a single nucleotide polymorphism rs35489000 and shows 50% reduced olmesartan medoxomil-hydrolase activity, slightly higher Km, and lower Vmax compared to the wild-type protein | Homo sapiens |
Localization
| Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|---|---|---|---|
| cytosol | - |
Homo sapiens | 5829 | - |
| microsome | - |
Homo sapiens | - |
- |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| olmesartan medoxomil + H2O | Homo sapiens | - |
olmesartan + diacetyl | - |
? |  |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | Q96DG6 | - |
- |
Purification (Commentary)
| Purification (Comment) | Organism |
|---|---|
| subcellular fractionation from liver and intestine, recombinant tagged mutant enzymes by affinity chromatography | Homo sapiens |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| colon | - |
Homo sapiens | - |
| duodenum | high enzyme activity | Homo sapiens | - |
| intestine | Tthe protein and activity are highly distributed in the proximal region (duodenum and jejunum) and decrease to the distal region of the intestine, high 16fold interindividual variability in both the protein and activity in the intestinal segments from the duodenum to colon. The interindividual variability in the duodenum and jejunum was relatively small, i.e. 3.0fold and 2.4fold, respectively | Homo sapiens | - |
| jejunum | high enzyme activity | Homo sapiens | - |
| liver | - |
Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| olmesartan medoxomil + H2O | - |
Homo sapiens | olmesartan + diacetyl | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| carboxymethylenebutenolidase homolog | - |
Homo sapiens |
| CMBL | - |
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 |
|---|---|---|
| physiological function | the carboxymethylenebutenolidase homologue is the enzyme responsible in humans for bioactivation of olmesartan medoxomil, prodrug-type angiotensin II type 1 receptor blocker | Homo sapiens |
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Release 2023.1 (January 2023)
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