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Literature summary for 3.4.21.B24 extracted from
- Recombinant proprotein convertase 4 (PC4) from Leishmania tarentolae expression system: purification, biochemical study and inhibitor design (2008), Protein Expr. Purif., 60, 117-126.
Activating Compound
| Activating Compound | Comment | Organism | Structure |
|---|---|---|---|
| prodomain rPC4101-116 peptide | at concentrations below 0.001 mM, it enhances PC4-activity depending on concentration (by as much as about 2fold). This activation effect is less significant for a higher substrate concentration and is not noticeable at concentrations above 0.02 mM | Rattus norvegicus |
Application
| Application | Comment | Organism |
|---|---|---|
| medicine | PC4 inhibitors may find potential therapeutic and clinical applications in male fertility | Rattus norvegicus |
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| full length and C-terminal truncated rPC4 are expressed using Leishmania tarentolae expression system | Rattus norvegicus |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| decanoyl-RVRK-chloromethyl ketone | - |
Rattus norvegicus |  |
| decanoyl-RVRR-chloromethyl ketone | - |
Rattus norvegicus | |
| prodomain rPC4101-116 peptide | strong competitive inhibition | Rattus norvegicus |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Rattus norvegicus | - |
- |
- |
Purification (Commentary)
| Purification (Comment) | Organism |
|---|---|
| recombinant | Rattus norvegicus |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| tert-butyloxycarbonyl-RVRR-7-amido-4-methylcoumarin + H2O | - |
Rattus norvegicus | tert-butyloxycarbonyl-RVRR + 7-amino-4-methylcoumarin | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| PC4 | - |
Rattus norvegicus |
| proprotein convertase 4 | - |
Rattus norvegicus |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.0038 | - |
prodomain rPC4101-116 peptide | - |
Rattus norvegicus |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.0000122 | - |
- |
Rattus norvegicus | decanoyl-RVRK-chloromethyl ketone | |
| 0.0000166 | - |
- |
Rattus norvegicus | decanoyl-RVRR-chloromethyl ketone | |
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