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Literature summary extracted from

  • Uejima, Y.; Kokubo, M.; Oshida, J.; Kawabata, H.; Kato, Y.; Fujii, K.
    5-Methyl-4H-3,1-benzoxazin-4-one derivatives: specific inhibitors of human leukocyte elastase (1993), J. Pharmacol. Exp. Ther., 265, 516-523.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.21.37 7-(4-chlorophenylsulfonyl-L-glutamyl)amino-5-methyl-2-iso-propylamino-4H-3,1-benzoxazin-4-one TEI-5624, strong, highly specific inhibitor, prevents degradation of insoluble elastin by elastase, prevents pulmonary hemorrhage in animal model Cricetulus griseus
3.4.21.37 7-(4-chlorophenylsulfonyl-L-glutamyl)amino-5-methyl-2-iso-propylamino-4H-3,1-benzoxazin-4-one TEI-5624, strong, highly specific inhibitor, prevents degradation of insoluble elastin by elastase Homo sapiens
3.4.21.37 7-(4-chlorophenylsulfonyl-L-lysyl)amino-5-methyl-2-iso-propylamino-4H-3,1-benzoxazin-4-one TEI-6344, strong, highly specific inhibitor, prevents degradation of insoluble elastin by elastase, prevents pulmonary hemorrhage in animal model Cricetulus griseus
3.4.21.37 7-(4-chlorophenylsulfonyl-L-lysyl)amino-5-methyl-2-iso-propylamino-4H-3,1-benzoxazin-4-one TEI-6344, strong, highly specific inhibitor, prevents degradation of insoluble elastin by elastase Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
3.4.21.37 Elastin + H2O Cricetulus griseus involved in lung defense against bacterial infection, due to the ability of the enzyme to cleave cell surface proteins, body cells might also be damaged ? protein cleaved at at least one location ?
3.4.21.37 Elastin + H2O Homo sapiens involved in lung defense against bacterial infection, due to the ability of the enzyme to cleave cell surface proteins, body cells might also be damaged ? protein cleaved at at least one location ?

Organism

EC Number Organism UniProt Comment Textmining
3.4.21.37 Cricetulus griseus
-
 with induced pulmonary hemorrhage
-
3.4.21.37 Homo sapiens
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.4.21.37 lung
-
 Cricetulus griseus
-
3.4.21.37 lung
-
 Homo sapiens
-
3.4.21.37 sputum
-
 Cricetulus griseus
-
3.4.21.37 sputum
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.4.21.37 Elastin + H2O
-
 Cricetulus griseus ?
-
 ?
3.4.21.37 Elastin + H2O
-
 Homo sapiens ?
-
 ?
3.4.21.37 Elastin + H2O involved in lung defense against bacterial infection, due to the ability of the enzyme to cleave cell surface proteins, body cells might also be damaged Cricetulus griseus ? protein cleaved at at least one location ?
3.4.21.37 Elastin + H2O involved in lung defense against bacterial infection, due to the ability of the enzyme to cleave cell surface proteins, body cells might also be damaged Homo sapiens ? protein cleaved at at least one location ?
3.4.21.37 methoxysuccinyl-Ala-Ala-Pro-Val-4-nitroanilide + H2O
-
 Cricetulus griseus methoxysuccinyl-Ala-Ala-Pro-Val + 4-nitroaniline
-
 ?
3.4.21.37 methoxysuccinyl-Ala-Ala-Pro-Val-4-nitroanilide + H2O
-
 Homo sapiens methoxysuccinyl-Ala-Ala-Pro-Val + 4-nitroaniline
-
 ?

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.4.21.37 0.000007
-
 7-(4-chlorophenylsulfonyl-L-glutamyl)amino-5-methyl-2-iso-propylamino-4H-3,1-benzoxazin-4-one pH 7.5, 37°C Cricetulus griseus
3.4.21.37 0.000007
-
 7-(4-chlorophenylsulfonyl-L-glutamyl)amino-5-methyl-2-iso-propylamino-4H-3,1-benzoxazin-4-one pH 7.5, 37°C Homo sapiens
3.4.21.37 0.000016
-
 7-(4-chlorophenylsulfonyl-L-lysyl)amino-5-methyl-2-iso-propylamino-4H-3,1-benzoxazin-4-one pH 7.5, 37°C Cricetulus griseus
3.4.21.37 0.000016
-
 7-(4-chlorophenylsulfonyl-L-lysyl)amino-5-methyl-2-iso-propylamino-4H-3,1-benzoxazin-4-one pH 7.5, 37°C Homo sapiens