Any feedback?
Literature summary for 3.3.2.10 extracted from
- Epoxide hydrolases: mechanisms, inhibitor designs, and biological roles (2005), Annu. Rev. Pharmacol. Toxicol., 45, 311-333.
Application
| Application | Comment | Organism |
|---|---|---|
| medicine | the enzyme is a target for regulation of blood pressure, and inhibition of inflammation, atherosclerosis, kidney failure, and cancer progression | Homo sapiens |
| pharmacology | the enzyme is a target for inhibitor design | Mus musculus |
| pharmacology | the enzyme is a target for inhibitor design | Homo sapiens |
| pharmacology | the enzyme is a target for inhibitor design | Rattus norvegicus |
Crystallization (Commentary)
| Crystallization (Comment) | Organism |
|---|---|
- |
Homo sapiens |
| enzyme with bound inhibitor N-cyclohexyl-N'-decylurea | Mus musculus |
Protein Variants
| Protein Variants | Comment | Organism |
|---|---|---|
| H431S | mutation of His431 results in total loss of activity, the mutant can form the intermediate but cannot hydrolyze it | Mus musculus |
| Y381F | site-directed mutagenesis, mutant shows 90% reduced activity | Mus musculus |
| Y465F | site-directed mutagenesis, mutant shows 90% reduced activity | Mus musculus |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 1,3-disubstituted amides | potent and stable inhibition, Ki in the nanomolar range, mechanism | Homo sapiens |  |
| 1,3-disubstituted amides | potent and stable inhibition, Ki in the nanomolar range, mechanism | Mus musculus | |
| 1,3-disubstituted amides | potent and stable inhibition, Ki in the nanomolar range, mechanism | Rattus norvegicus | |
| 1,3-disubstituted carbamate derivatives | potent and stable inhibition, Ki in the nanomolar range, mechanism | Homo sapiens | |
| 1,3-disubstituted carbamate derivatives | potent and stable inhibition, Ki in the nanomolar range, mechanism | Mus musculus | |
| 1,3-disubstituted carbamate derivatives | potent and stable inhibition, Ki in the nanomolar range, mechanism | Rattus norvegicus | |
| 1,3-disubstituted urea derivatives | potent and stable inhibition, Ki in the nanomolar range, mechanism | Homo sapiens | |
| 1,3-disubstituted urea derivatives | potent and stable inhibition, Ki in the nanomolar range, mechanism | Mus musculus | |
| 1,3-disubstituted urea derivatives | potent and stable inhibition, Ki in the nanomolar range, mechanism | Rattus norvegicus | |
| Cd2+ | - |
Homo sapiens | |
| Cd2+ | - |
Mus musculus | |
| Cd2+ | - |
Rattus norvegicus | |
| Cu2+ | - |
Homo sapiens | |
| Cu2+ | - |
Mus musculus | |
| Cu2+ | - |
Rattus norvegicus | |
| Hg2+ | - |
Homo sapiens | |
| Hg2+ | - |
Mus musculus | |
| Hg2+ | - |
Rattus norvegicus | |
| additional information | most enzyme inhibitors do not influence the enzyme's phosphatase activity | Homo sapiens | |
| N-cyclohexyl-N'-decylurea | - |
Mus musculus | |
| Zn2+ | noncompetitive, inhibits epoxide hydrolase and phosphatase activities, allosteric mechanism | Homo sapiens | |
| Zn2+ | - |
Mus musculus | |
| Zn2+ | - |
Rattus norvegicus | |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| additional information | - |
additional information | kinetics, the hydrolysis of the intermediate is the rate-limiting step | Mus musculus | |
| additional information | - |
additional information | kinetics, the hydrolysis of the intermediate is the rate-limiting step | Homo sapiens | |
| additional information | - |
additional information | kinetics, the hydrolysis of the intermediate is the rate-limiting step | Rattus norvegicus |
Localization
| Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|---|---|---|---|
| cytosol | - |
Mus musculus | 5829 | - |
| cytosol | - |
Homo sapiens | 5829 | - |
| cytosol | - |
Rattus norvegicus | 5829 | - |
Molecular Weight [Da]
| Molecular Weight [Da] | Molecular Weight Maximum [Da] | Comment | Organism |
|---|---|---|---|
| 62500 | - |
1 * 62500 | Homo sapiens |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| additional information | Mus musculus | the enzyme is involved in regulation of blood pressure and inflammation | ? | - |
? | |
| additional information | Homo sapiens | the enzyme is involved in regulation of blood pressure and inflammation | ? | - |
? | |
| additional information | Rattus norvegicus | the enzyme is involved in regulation of blood pressure and inflammation | ? | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
| Mus musculus | - |
- |
- |
| Rattus norvegicus | - |
- |
- |
Reaction
| Reaction | Comment | Organism | Reaction ID |
|---|---|---|---|
| an epoxide + H2O = a glycol | two step mechanism with formation of of a hydroxyl-alkyl-enzyme intermediate, catalytic triad is Asp333-His523-Asp495 with polarizing residues Tyr381 and Tyr465, catalytic cycle | Mus musculus | |
| an epoxide + H2O = a glycol | two step mechanism with formation of of a hydroxyl-alkyl-enzyme intermediate, the catalytic triad is Asp333-His523-Asp495, catalytic cycle | Rattus norvegicus | |
| an epoxide + H2O = a glycol | two step mechanism with formation of of a hydroxyl-alkyl-enzyme intermediate, the catalytic triad is Asp334-His523-Asp495 with polarizing residues Tyr382 and Tyr465, catalytic cycle | Homo sapiens |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| kidney | - |
Mus musculus | - |
| kidney | - |
Homo sapiens | - |
| kidney | - |
Rattus norvegicus | - |
| liver | - |
Mus musculus | - |
| liver | - |
Homo sapiens | - |
| liver | - |
Rattus norvegicus | - |
| additional information | wide tissue distribution | Mus musculus | - |
| additional information | wide tissue distribution | Homo sapiens | - |
| additional information | wide tissue distribution | Rattus norvegicus | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| chalcone oxides + H2O | - |
Mus musculus | ? | - |
? | |
| chalcone oxides + H2O | - |
Homo sapiens | ? | - |
? | |
| chalcone oxides + H2O | - |
Rattus norvegicus | ? | - |
? | |
| additional information | the enzyme is involved in regulation of blood pressure and inflammation | Mus musculus | ? | - |
? | |
| additional information | the enzyme is involved in regulation of blood pressure and inflammation | Homo sapiens | ? | - |
? | |
| additional information | the enzyme is involved in regulation of blood pressure and inflammation | Rattus norvegicus | ? | - |
? | |
| additional information | sEH prefers gem-di-, trans-di-, cis-di-, tri-, and tetra-substituted epoxides | Mus musculus | ? | - |
? | |
| additional information | sEH prefers gem-di-, trans-di-, cis-di-, tri-, and tetra-substituted epoxides | Rattus norvegicus | ? | - |
? | |
| additional information | the enzyme also shows phosphatase activity, EC 3.1.3.76, sEH prefers gem-di-, trans-di-, cis-di-, tri-, and tetra-substituted epoxides | Homo sapiens | ? | - |
? | |
| stearic acid epoxide + H2O | - |
Homo sapiens | ? | - |
? | |
Subunits
| Subunits | Comment | Organism |
|---|---|---|
| monomer | 1 * 62500 | Homo sapiens |
| More | quarternary structure | Mus musculus |
| More | quarternary structure | Rattus norvegicus |
| More | quarternary structure, monomers interact in a head-to-tail manner, the enzyme contains the DXDX(T/V) motif | Homo sapiens |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| EPXH1 | - |
Homo sapiens |
| EPXH2 | - |
Homo sapiens |
| More | the enzyme belongs to the alpha/beta-hydrolase fold family of proteins | Mus musculus |
| More | the enzyme belongs to the alpha/beta-hydrolase fold family of proteins | Homo sapiens |
| More | the enzyme belongs to the alpha/beta-hydrolase fold family of proteins | Rattus norvegicus |
| SEH | - |
Mus musculus |
| SEH | - |
Homo sapiens |
| SEH | - |
Rattus norvegicus |
pH Optimum
| pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|
| 7 | 7.5 | - |
Homo sapiens |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.02 | - |
Zn2+ | - |
Homo sapiens | |
Use of this online version of BRENDA is free under the CC BY 4.0 license. See terms of use for full details.
Release 2023.1 (January 2023)
Legal
Curated at
Member of
