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Literature summary for 3.4.11.2 extracted from
- Aminopeptidase-N/CD13 (EC 3.4.11.2) inhibitors: chemistry, biological evaluations, and therapeutic prospects (2006), Med. Res. Rev., 26, 88-130.
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| gene mapping on chromosome 15q25-26, DNA and amino acid sequence analysis | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| (2S,3R)-3-amino-2-hydroxy-4-phenylbutanoyl-L-valine | - |
Homo sapiens |  |
| (2S,3R)-3-amino-2-hydroxy-4-phenylbutanoyl-L-valyl-L-prolyl-(trans-4-hydroxy-L-proline) | i.e. MR387A | Homo sapiens | |
| (2S,3R)-3-amino-2-hydroxy-4-phenylbutanoyl-L-valyl-L-prolyl-L-proline | i.e. MR378B | Homo sapiens | |
| 2(S)-amino-5-methylpentanal | - |
Homo sapiens | |
| 3-amino-1-hydroxypropan-2-one derivatives | - |
Homo sapiens | |
| 3-amino-2-hydroxypropionaldehyde derivatives | - |
Homo sapiens | |
| 3-amino-2-tetralone derivatives | - |
Homo sapiens | |
| 4-hydroxybestatin | - |
Homo sapiens | |
| 8-hydroxyquinoline | - |
Homo sapiens | |
| actinonin | synthetic inhibitor, complete inhibition of plasma enzyme at 0.1 mM | Homo sapiens | |
| alkyl D-cysteinats | - |
Homo sapiens | |
| alpha-thiolbestatin | - |
Homo sapiens | |
| amastatin | competitive, isolated from Streptomyces sp. strain ME98-M3, modulates blood pressure | Homo sapiens | |
| Ammonium oxalate | - |
Homo sapiens | |
| apigenin | 26% inhibition at 0.1 mM, 42% at 0.3 mM | Homo sapiens | |
| baicalein | 42% inhibition at 0.3 mM | Homo sapiens | |
| bestatin | competitive, slow-binding inhibitor, from Streptomyces olivoreticuli strain MD976-C7, modulates cell growth and maturation, overview | Homo sapiens | |
| bestatin thioamide | - |
Homo sapiens | |
| betulinic acid | pentycyclic compound, from Betula sp. and other sources, overview, modulates cell growth and maturation, overview | Homo sapiens | |
| bradykinin | - |
Homo sapiens | |
| Ca2+ | - |
Homo sapiens | |
| chelerythrine | - |
Homo sapiens | |
| Co2+ | - |
Homo sapiens | |
| curcumin | from Curcuma longa rhizome, inhibits the enzyme and the initiation of carcinogenesis, overview, modulates cell growth and maturation, overview | Homo sapiens | |
| flavone-8-acetic acid derivatives | - |
Homo sapiens | |
| KCN | - |
Homo sapiens | |
| Kelatorphan | - |
Homo sapiens | |
| L-Ala | at micromolar concentrations | Homo sapiens | |
| L-Arg | at micromolar concentrations | Homo sapiens | |
| L-Glu | at micromolar concentrations | Homo sapiens | |
| L-Met | at micromolar concentrations | Homo sapiens | |
| lapstatin | - |
Homo sapiens | |
| Leu | at micromolar concentrations | Homo sapiens | |
| leuhistin | from Bacillus letraosporus strain BM156-14F1, competitive, modulates cell growth and maturation, overview | Homo sapiens | |
| Mn2+ | - |
Homo sapiens | |
| additional information | enzyme inhibitors: chemistry, biological evaluations, and therapeutic prospects, behaviour in clinical trials, overview | Homo sapiens | |
| MR-387 A | - |
Homo sapiens | |
| Mr-387 B | - |
Homo sapiens | |
| myricetin | 48% inhibition at 0.3 mm | Homo sapiens | |
| N-hydroxy-2-(naphthalene-2-ylsulfanyl)acetamide | - |
Homo sapiens | |
| NaN3 | - |
Homo sapiens | |
| NEM | - |
Homo sapiens | |
| Ni2+ | - |
Homo sapiens | |
| PC18 | - |
Homo sapiens | |
| phebestin | frpm Streptomyces sp. strain MJ716-m3 | Homo sapiens | |
| PIQ-22 | - |
Homo sapiens | |
| Pro | at micromolar concentrations | Homo sapiens | |
| probestin | from Streptomyces azureus strain MH663-2F6, competitive, modulates cell growth and maturation, overview | Homo sapiens | |
| psammaplin A | from Psammaplysilla sp., Dysidea sp., and Throrectopsamma xana, non-competitive, modulates cell growth and maturation, overview | Homo sapiens | |
| pseudoglutamyl aminophosphinic peptides | - |
Homo sapiens | |
| puromycin | - |
Homo sapiens | |
| RB101 | - |
Homo sapiens | |
| RB120 | - |
Homo sapiens | |
| RB129 | - |
Homo sapiens | |
| RB38A | - |
Homo sapiens | |
| SL-387 | i.e. AHPA-Val | Homo sapiens | |
| Substance P | - |
Homo sapiens | |
| Zn2+ | - |
Homo sapiens | |
Localization
| Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|---|---|---|---|
| cell surface | - |
Homo sapiens | 9986 | - |
| plasma membrane | transmembrane enzyme, anchored via its N-terminus | Homo sapiens | 5886 | - |
Metals/Ions
| Metals/Ions | Comment | Organism | Structure |
|---|---|---|---|
| Zn2+ | zinc-metallopeptidase, zinc binding motif HEXXH | Homo sapiens | |
Molecular Weight [Da]
| Molecular Weight [Da] | Molecular Weight Maximum [Da] | Comment | Organism |
|---|---|---|---|
| 160000 | - |
- |
Homo sapiens |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| kallidin + H2O | Homo sapiens | - |
? | - |
? | |
| Leu-enkephalin + H2O | Homo sapiens | - |
Leu + enkephalin | - |
? | |
| Met-enkephalin + H2O | Homo sapiens | - |
Met + enkephalin | - |
? | |
| Met-Lys-bradykinin + H2O | Homo sapiens | - |
Met + Lys + bradykinin | - |
? | |
| monocyte chemotactic protein MCP-1 + H2O | Homo sapiens | - |
? | - |
? | |
| additional information | Homo sapiens | the enzyme serves as receptor for coronaviruses, modulates bioactive peptide responses, e.g. vasopressin release, and influences immune functions and major biological processess, such as cell proliferation, secretion, invasion, and angiogenesis, overview, enzyme inhibition affects these processes, overview | ? | - |
? | |
| N-formyl-Met-Leu-Phe + H2O | Homo sapiens | - |
? | - |
? | |
| Neurokinin A + H2O | Homo sapiens | - |
? | - |
? | |
| somatostatin + H2O | Homo sapiens | - |
? | - |
? | |
| spinorphin + H2O | Homo sapiens | - |
? | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
Posttranslational Modification
| Posttranslational Modification | Comment | Organism |
|---|---|---|
| glycoprotein | the enzyme is N- and O-glycosylated, overview | Homo sapiens |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| brain | - |
Homo sapiens | - |
| carcinoma cell | - |
Homo sapiens | - |
| endothelial cell | - |
Homo sapiens | - |
| epithelial cell | - |
Homo sapiens | - |
| fibroblast | - |
Homo sapiens | - |
| leukocyte | - |
Homo sapiens | - |
| macrophage | - |
Homo sapiens | - |
| neutrophil | - |
Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| kallidin + H2O | - |
Homo sapiens | ? | - |
? | |
| Leu-enkephalin + H2O | - |
Homo sapiens | Leu + enkephalin | - |
? | |
| Met-enkephalin + H2O | - |
Homo sapiens | Met + enkephalin | - |
? | |
| Met-Lys-bradykinin + H2O | - |
Homo sapiens | Met + Lys + bradykinin | - |
? | |
| monocyte chemotactic protein MCP-1 + H2O | - |
Homo sapiens | ? | - |
? | |
| additional information | the enzyme serves as receptor for coronaviruses, modulates bioactive peptide responses, e.g. vasopressin release, and influences immune functions and major biological processess, such as cell proliferation, secretion, invasion, and angiogenesis, overview, enzyme inhibition affects these processes, overview | Homo sapiens | ? | - |
? | |
| additional information | the enzyme prefers neutral N-terminal amino acid substrates | Homo sapiens | ? | - |
? | |
| N-formyl-Met-Leu-Phe + H2O | - |
Homo sapiens | ? | - |
? | |
| Neurokinin A + H2O | - |
Homo sapiens | ? | - |
? | |
| somatostatin + H2O | - |
Homo sapiens | ? | - |
? | |
| spinorphin + H2O | - |
Homo sapiens | ? | - |
? | |
Subunits
| Subunits | Comment | Organism |
|---|---|---|
| More | structure overview, topological scheme | Homo sapiens |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| aminopeptidase-N | - |
Homo sapiens |
| APN | - |
Homo sapiens |
| CD13 | - |
Homo sapiens |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.05 | - |
IC50 is 0.05 mM | Homo sapiens | (4R)-4-(ethylamino)-2-(3-methoxypropyl)-1,1-dioxo-1,2,3,4-tetrahydro-1lambda~6~-thieno[3,2-e][1,2]thiazine-6-sulfonamide | |
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