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Literature summary for 3.4.11.2 extracted from

  • Bauvois, B.; Puiffe, M.L.; Bongui, J.B.; Paillat, S.; Monneret, C.; Dauzonne, D.
    Synthesis and biological evaluation of novel flavone-8-acetic acid derivatives as reversible inhibitors of aminopeptidase N/CD13 (2003), J. Med. Chem., 46, 3900-3913.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
overexpression in tumour cells Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
2',3-dinitro-3'-methoxy-flavone-8-acetic acid 75% inhibition at 1 mM Homo sapiens
2',3-dinitro-5'-methoxy-flavone-8-acetic acid 80% inhibition at 1 mM Homo sapiens
2',3-dinitroflavone-8-acetic acid reversible, competitive, selective, potent, and noncytotoxic inhibitor, 88% inhibition at 1 mM Homo sapiens
2'-nitro-flavone-8-acetic acid highly cytotoxic, 83% inhibition at 1 mM Homo sapiens
3,3'-dinitro-4'-methoxy-flavone-8-acetic acid 61% inhibition at 1 mM Homo sapiens
3,3'-dinitroflavone-8-acetic acid 44% inhibition at 1 mM Homo sapiens
3,4'-dinitroflavone-8-acetic acid 63% inhibition at 1 mM Homo sapiens
3-amino-2-(2-hydroxyphenyl)-4-oxo-4H-1-benzopyran-8-acetic acid methoxymethyl ester highly cytotoxic, 19% inhibition at 1 mM Homo sapiens
3-amino-flavone-8-acetic acid 33% inhibition at 1 mM Homo sapiens
3-nitro-2'-benzyloxy-flavone-8-acetic acid cytotoxic, 76% inhibition at 1 mM Homo sapiens
3-nitro-2'-carboxybenzyl-flavone-8-acetic acid cytotoxic, 77% inhibition at 1 mM Homo sapiens
3-nitro-2'-carboxymethyl-flavone-8-acetic acid slightly cytotoxic, 66% inhibition at 1 mM Homo sapiens
3-nitro-2'-chloro-flavone-8-acetic acid slightly cytotoxic, 76% inhibition at 1 mM Homo sapiens
3-nitro-2-(2-benzyloxyphenyl)-4-oxo-4H-1-benzopyran-8-acetic acid methoxymethyl ester highly cytotoxic, 32% inhibition at 1 mM Homo sapiens
3-nitro-2-(2-nitrophenyl)-4-oxo-4H-1-benzopyran-8-acetic acid methoxymethyl ester highly cytotoxic, 48% inhibition at 1 mM Homo sapiens
3-nitro-4'-methoxy-flavone-8-acetic acid cytotoxic, 64% inhibition at 1 mM Homo sapiens
3-nitro-flavone 30% inhibition at 1 mM Homo sapiens
3-nitro-flavone-8-acetaldehyde cytotoxic, 51% inhibition at 1 mM Homo sapiens
3-nitroflavone-8-acetic acid 68% inhibition at 1 mM Homo sapiens
bestatin strong inhibition, cytotoxic, 85% inhibition at 1 mM Homo sapiens
flavone 5% inhibition at 1 mM Homo sapiens
flavone-8-acetic acid 30% inhibition at 1 mM Homo sapiens
additional information
-
Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
membrane cell surface Homo sapiens 16020
-

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
additional information Homo sapiens enzyme plays a critical role in angiogenesis ?
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
U937 cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Ala-4-nitroanilide + H2O
-
Homo sapiens Ala + 4-nitroaniline
-
?
additional information enzyme plays a critical role in angiogenesis Homo sapiens ?
-
?

Synonyms

Synonyms Comment Organism
aminopeptidase N
-
Homo sapiens
aminopeptidase N/CD13
-
Homo sapiens
APN
-
Homo sapiens
APN/CD13
-
Homo sapiens
CD13
-
Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
additional information
-
additional information
-
Homo sapiens