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Literature summary for 3.4.11.7 extracted from
- Orally Active Aminopeptidase A Inhibitors Reduce Blood Pressure. A New Strategy for Treating Hypertension (2008), Hypertension, 51, 1318-1325.
Application
| Application | Comment | Organism |
|---|---|---|
| medicine | RB150 is the first oral active prodrug inhibiting brain but not systemic renin-angiotensin system activity, strongly reducing blood pressure several hours after a single administration | Rattus norvegicus |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| (S)-3-amino-4-mercaptobutyl sulfonic acid | EC33, specific and selective APA inhibitor | Mus musculus |  |
| (S)-3-amino-4-mercaptobutyl sulfonic acid | EC33, specific and selective APA inhibitor | Rattus norvegicus | |
| 4,4'-dithio[bis(3)-aminobutylsulfonic acid] | RB150, a prodrug of EC33 | Mus musculus | |
| 4,4'-dithio[bis(3)-aminobutylsulfonic acid] | RB150, a prodrug of EC33 | Rattus norvegicus | |
| bestatin | broad specificity for various aminopeptidases | Mus musculus | |
| bestatin | broad specificity for various aminopeptidases | Rattus norvegicus | |
Metals/Ions
| Metals/Ions | Comment | Organism | Structure |
|---|---|---|---|
| Zn2+ | - |
Mus musculus | |
| Zn2+ | - |
Rattus norvegicus | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Mus musculus | - |
- |
- |
| Rattus norvegicus | - |
hypertensive DOCA-salt rat, for the on vitro activity assay recombinant mouse APA is used | - |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| brain | - |
Rattus norvegicus | - |
Specific Activity [micromol/min/mg]
| Specific Activity Minimum [µmol/min/mg] | Specific Activity Maximum [µmol/min/mg] | Comment | Organism |
|---|---|---|---|
| 0.000686 | - |
DOCA-salt rat, 30 mg/kg RB150, 3.5 h after po | Rattus norvegicus |
| 0.00071 | - |
DOCA-salt rat, 50 mg/kg RB150, 3.5 h after po | Rattus norvegicus |
| 0.000726 | - |
DOCA-salt rat, 15 mg/kg RB150, 3.5 h after po | Rattus norvegicus |
| 0.000728 | - |
normotensive WKY rat, 15 mg/kg RB150, 3.5 h after po | Rattus norvegicus |
| 0.000752 | - |
normotensive WKY rat, 3.5 h after administration of saline po | Rattus norvegicus |
| 0.00077 | - |
normotensive Sham rat, 3.5 h after administration of saline po | Rattus norvegicus |
| 0.001083 | - |
DOCA-salt rat, 7.5 mg/kg RB150, 3.5 h after po | Rattus norvegicus |
| 0.001525 | - |
DOCA-salt rat, 3.5 h after administration of saline po | Rattus norvegicus |
| 0.001557 | - |
DOCA-salt rat, 15 mg/kg RB150, 24 h after po | Rattus norvegicus |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| angiotensin II + H2O | angiotensin II: Asp-Arg-Val-Tyr-Ile-His-Pro-Phe | Rattus norvegicus | aspartic acid + angiotensin III | angiotensin III: Arg-Val-Tyr-Ile-His-Pro-Phe | ? | |
| Glu-2-naphthylamide + H2O | synthetic substrate used in the activity assay | Mus musculus | Glu + 2-naphthylamine | - |
? | |
| Glu-2-naphthylamide + H2O | synthetic substrate used in the activity assay | Rattus norvegicus | Glu + 2-naphthylamine | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| aminopeptidase A | - |
Mus musculus |
| aminopeptidase A | - |
Rattus norvegicus |
pH Optimum
| pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|
| 7.4 | - |
activity assay | Mus musculus |
| 7.4 | - |
activity assay | Rattus norvegicus |
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