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Literature summary for 3.4.11.1 extracted from
- The most potent organophosphorus inhibitors of leucine aminopeptidase. Structure-based design, chemistry, and activity (2003), J. Med. Chem., 46, 2641-2655.
Application
| Application | Comment | Organism |
|---|---|---|
| medicine | enzyme is a target for inhibitor design | Sus scrofa |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 2-[[(1-amino-3-methylbutyl)hydroxyphosphinyl]methyl]-4-methylpentanoic acid | (R)-isomer and 1:1 ratio of the 2 diastereomers | Sus scrofa |  |
| 2-[[(1-amino-4-phenylbutyl)hydroxyphosphinyl]methyl]-3-(4-hydroxyphenyl)propionic acid | - |
Sus scrofa | |
| 2-[[(1-amino-4-phenylbutyl)hydroxyphosphinyl]methyl]-3-phenylpropionic acid | - |
Sus scrofa | |
| 2-[[(1-amino-4-phenylbutyl)hydroxyphosphinyl]methyl]-4-methylpentanoic acid | - |
Sus scrofa | |
| 3-[(1-amino-3-methylbutyl)hydroxyphosphinyl]-propionic acid | - |
Sus scrofa | |
| additional information | computational inhibitor design | Sus scrofa | |
| N-[(1-hydroxy-3-methylbutyl)oxyphosphinyl]glycine dilithium salt | - |
Sus scrofa | |
Localization
| Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|---|---|---|---|
| cytosol | - |
Sus scrofa | 5829 | - |
Metals/Ions
| Metals/Ions | Comment | Organism | Structure |
|---|---|---|---|
| Zn2+ | zinc-containing metallopeptidase | Sus scrofa | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Sus scrofa | - |
- |
- |
Reaction
| Reaction | Comment | Organism | Reaction ID |
|---|---|---|---|
| release of an N-terminal amino acid, Xaa-/-Yaa-, in which Xaa is preferably Leu, but may be other amino acids including Pro although not Arg or Lys, and Yaa may be Pro. Amino acid amides and methyl esters are also readily hydrolysed, but rates on arylamides are exceedingly low | exopeptidase | Sus scrofa |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| commercial preparation | - |
Sus scrofa | - |
| kidney | - |
Sus scrofa | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| L-Leu-4-nitroanilide + H2O | - |
Sus scrofa | L-Leu + 4-nitroaniline | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| LAP | - |
Sus scrofa |
| leucine aminopeptidase | - |
Sus scrofa |
Temperature Optimum [°C]
| Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|
| 25 | - |
assay at | Sus scrofa |
pH Optimum
| pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|
| 8.4 | - |
assay at | Sus scrofa |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.000065 | - |
2-[[(1-amino-3-methylbutyl)hydroxyphosphinyl]methyl]-4-methylpentanoic acid | pH 8.4, 25°C, 1:1 ratio of the 2 diastereomers | Sus scrofa | |
| 0.000066 | - |
2-[[(1-amino-4-phenylbutyl)hydroxyphosphinyl]methyl]-3-phenylpropionic acid | pH 8.4, 25°C | Sus scrofa | |
| 0.000067 | - |
2-[[(1-amino-4-phenylbutyl)hydroxyphosphinyl]methyl]-3-(4-hydroxyphenyl)propionic acid | pH 8.4, 25°C | Sus scrofa | |
| 0.000074 | - |
2-[[(1-amino-4-phenylbutyl)hydroxyphosphinyl]methyl]-4-methylpentanoic acid | pH 8.4, 25°C | Sus scrofa | |
| 0.00011 | - |
2-[[(1-amino-3-methylbutyl)hydroxyphosphinyl]methyl]-4-methylpentanoic acid | pH 8.4, 25°C, (R)-isomer | Sus scrofa | |
| 0.00033 | - |
3-[(1-amino-3-methylbutyl)hydroxyphosphinyl]-propionic acid | pH 8.4, 25°C | Sus scrofa | |
| 0.00488 | - |
N-[(1-hydroxy-3-methylbutyl)oxyphosphinyl]glycine dilithium salt | pH 8.4, 25°C | Sus scrofa | |
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