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Literature summary for 3.1.8.1 extracted from
- Rational design of paraoxonase 1 (PON1) for the efficient hydrolysis of organophosphates (2015), Chem. Commun. (Camb.), 51, 14536-14539 .
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| gene PON1, recombinant expression of wild-type and mutant enzymes in Escherichia coli strain Origami B (DE3) | Oryctolagus cuniculus |
Protein Variants
| Protein Variants | Comment | Organism |
|---|---|---|
| H115W/T332S | site-directed mutagenesis, the mutant shows highly increased activity with diethyl-paraoxon compared to wild-type | Oryctolagus cuniculus |
| H115W/T332S/V346A | site-directed mutagenesis, the mutant shows increased activity with diethyl-paraoxon compared to wild-type | Oryctolagus cuniculus |
| H115W/V346A | site-directed mutagenesis, the mutant shows increased activity with diethyl-paraoxon compared to wild-type | Oryctolagus cuniculus |
| I74A | site-directed mutagenesis, the mutant shows highly reduced activity with diethyl-paraoxon compared to wild-type | Oryctolagus cuniculus |
| I74F | site-directed mutagenesis, the mutant shows increased activity with diethyl-paraoxon compared to wild-type | Oryctolagus cuniculus |
| I74F/H115W | site-directed mutagenesis, the mutant shows increased activity with diethyl-paraoxon compared to wild-type | Oryctolagus cuniculus |
| I74F/H115W/T332S | site-directed mutagenesis, the mutant shows very highly increased activity with diethyl-paraoxon compared to wild-type | Oryctolagus cuniculus |
| I74F/H115W/V346A | site-directed mutagenesis, the mutant shows highly increased activity with diethyl-paraoxon compared to wild-type | Oryctolagus cuniculus |
| I74F/T332S | site-directed mutagenesis, the mutant shows increased activity with diethyl-paraoxon compared to wild-type | Oryctolagus cuniculus |
| I74F/T332S/V346A | site-directed mutagenesis, the mutant shows increased activity with diethyl-paraoxon compared to wild-type | Oryctolagus cuniculus |
| I74F/V346A | site-directed mutagenesis, the mutant shows increased activity with diethyl-paraoxon compared to wild-type | Oryctolagus cuniculus |
| I74L | site-directed mutagenesis, the mutant shows unaltered activity with diethyl-paraoxon compared to wild-type | Oryctolagus cuniculus |
| I74V | site-directed mutagenesis, the mutant shows slightly reduced activity with diethyl-paraoxon compared to wild-type | Oryctolagus cuniculus |
| I74W | site-directed mutagenesis, the mutant shows unaltered activity with diethyl-paraoxon compared to wild-type | Oryctolagus cuniculus |
| L69A | site-directed mutagenesis, the mutant shows highly reduced activity with diethyl-paraoxon compared to wild-type | Oryctolagus cuniculus |
| L69I | site-directed mutagenesis, the mutant shows slightly increased activity with diethyl-paraoxon compared to wild-type | Oryctolagus cuniculus |
| T332A | site-directed mutagenesis, the mutant shows highly increased activity with diethyl-paraoxon compared to wild-type | Oryctolagus cuniculus |
| T332S | site-directed mutagenesis, the mutant shows highly increased activity with diethyl-paraoxon compared to wild-type | Oryctolagus cuniculus |
| T332S/V346A | site-directed mutagenesis, the mutant shows increased activity with diethyl-paraoxon compared to wild-type | Oryctolagus cuniculus |
| T332V | site-directed mutagenesis, almost inactive mutant | Oryctolagus cuniculus |
| V346A | site-directed mutagenesis, the mutant shows increased activity with diethyl-paraoxon compared to wild-type | Oryctolagus cuniculus |
| V346L | site-directed mutagenesis, the mutant shows highly reduced activity with diethyl-paraoxon compared to wild-type | Oryctolagus cuniculus |
| V346L | site-directed mutagenesis, the mutant shows slightly increased activity with diethyl-paraoxon compared to wild-type | Oryctolagus cuniculus |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| diethyl-paraoxon | - |
Oryctolagus cuniculus |  |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| diethyl-paraoxon + H2O | Oryctolagus cuniculus | - |
diethyl phosphate + 4-nitrophenol | - |
? | |
| dimethyl-paraoxon + H2O | Oryctolagus cuniculus | - |
dimethyl phosphate + 4-nitrophenol | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Oryctolagus cuniculus | P27170 | - |
- |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| diethyl-paraoxon + H2O | - |
Oryctolagus cuniculus | diethyl phosphate + 4-nitrophenol | - |
? | |
| dimethyl-paraoxon + H2O | - |
Oryctolagus cuniculus | dimethyl phosphate + 4-nitrophenol | - |
? | |
| additional information | molecular docking of substrates to wild-type and mutant enzymes using the crystal structure of PON1 (PDB ID 3SRG with resolution 2.19 A), overview. The enzyme also shows arylesterase activity (EC 3.1.1.2) with phenyl acetate as substrate | Oryctolagus cuniculus | ? | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| G3C9 rePON1 | - |
Oryctolagus cuniculus |
| paraoxonase 1 | - |
Oryctolagus cuniculus |
| PON1 | - |
Oryctolagus cuniculus |
Temperature Optimum [°C]
| Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|
| 35 | - |
- |
Oryctolagus cuniculus |
pH Optimum
| pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|
| 10.5 | - |
- |
Oryctolagus cuniculus |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.192 | - |
diethyl-paraoxon | pH 10.5, 25°C, recombinant mutant I74F/H115W/T332S | Oryctolagus cuniculus | |
| 0.214 | - |
diethyl-paraoxon | pH 10.5, 25°C, recombinant mutant H115W/T332S | Oryctolagus cuniculus | |
| 0.404 | - |
diethyl-paraoxon | pH 10.5, 25°C, recombinant mutant I74F/H115W | Oryctolagus cuniculus | |
| 0.727 | - |
diethyl-paraoxon | pH 10.5, 25°C, recombinant mutant V346A | Oryctolagus cuniculus | |
| 1.54 | - |
diethyl-paraoxon | pH 10.5, 25°C, recombinant mutant I74F/T332S | Oryctolagus cuniculus | |
| 1.86 | - |
diethyl-paraoxon | pH 10.5, 25°C, recombinant mutant I74F | Oryctolagus cuniculus | |
| 2.31 | - |
diethyl-paraoxon | pH 10.5, 25°C, recombinant mutant T332S | Oryctolagus cuniculus | |
| 4.49 | - |
diethyl-paraoxon | pH 10.5, 25°C, recombinant wild-type enzyme | Oryctolagus cuniculus | |
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