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Literature summary for 3.5.3.15 extracted from
- Profiling protein arginine deiminase 4 (PAD4): a novel screen to identify PAD4 inhibitors (2008), Bioorg. Med. Chem., 16, 739-745.
Application
| Application | Comment | Organism |
|---|---|---|
| drug development | PAD4 is a leading target for the development of a rheumatoid arthritis pharmaceutical | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 5-aminosalicylic acid | - |
Homo sapiens |  |
| Azathioprine | - |
Homo sapiens | |
| azithromycin | - |
Homo sapiens | |
| clindamycin | - |
Homo sapiens | |
| leflunomide | - |
Homo sapiens | |
| methotrexate | - |
Homo sapiens | |
| minocycline | a mixed type inhibitor | Homo sapiens | |
| additional information | PAD4 inhibitor screening based on a PAD4-targeted activity-based protein profiling reagent, denoted rhodamine-conjugated F-amidine, RFA, rapid competitive assay method development, overview | Homo sapiens | |
| streptomycin | a competitive inhibitor of PAD4 | Homo sapiens | |
| sulfamethoxazole | - |
Homo sapiens | |
| sulfapyridine | - |
Homo sapiens | |
| trimethoprim | - |
Homo sapiens | |
Metals/Ions
| Metals/Ions | Comment | Organism | Structure |
|---|---|---|---|
| Ca2+ | - |
Homo sapiens | |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| protein-L-arginine + H2O | Homo sapiens | - |
protein-L-citrulline + NH3 | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| protein-L-arginine + H2O | - |
Homo sapiens | protein-L-citrulline + NH3 | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| PAD4 | - |
Homo sapiens |
| protein arginine deiminase 4 | - |
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 |
|---|---|---|---|
| 7.6 | - |
assay at | Homo sapiens |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| additional information | - |
additional information | inhibition kinetics | Homo sapiens |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 1.8 | - |
pH 7.6, 37°C, recombinant PAD4 | Homo sapiens | streptomycin | |
| 2.4 | - |
pH 7.6, 37°C, recombinant PAD4 | Homo sapiens | leflunomide | |
| 5.1 | - |
pH 7.6, 37°C, recombinant PAD4 | Homo sapiens | clindamycin | |
| 7.5 | - |
pH 7.6, 37°C, recombinant PAD4 | Homo sapiens | trimethoprim | |
| 8.1 | - |
pH 7.6, 37°C, recombinant PAD4 | Homo sapiens | Azathioprine | |
| 10 | - |
above, pH 7.6, 37°C, recombinant PAD4 | Homo sapiens | methotrexate | |
| 10 | - |
above, pH 7.6, 37°C, recombinant PAD4 | Homo sapiens | 5-aminosalicylic acid | |
| 10 | - |
above, pH 7.6, 37°C, recombinant PAD4 | Homo sapiens | sulfamethoxazole | |
| 10 | - |
above, pH 7.6, 37°C, recombinant PAD4 | Homo sapiens | sulfapyridine | |
| 10 | - |
above, pH 7.6, 37°C, recombinant PAD4 | Homo sapiens | azithromycin | |
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