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Literature summary for 3.4.21.37 extracted from

  • Sommerhoff, C.P.; Krell, R.D.; Williams, J.L.; Gomes, B.C.; Strimpler, A.M.; Nadel, J.A.
    Inhibition of human neutrophil elastase by ICI 200,355 (1991), Eur. J. Pharmacol., 193, 153-158.
    View publication on PubMed
Search for more literature for 3.4.21.37

Inhibitors

Inhibitors Comment Organism Structure
4-(4-bromophenylsulfonylcarbamoyl)benzoyl-L-valyl-L-proline 1 (RS)-(1-trifluoroacetyl-2-methylpropyl)amide ICI 200,355, reversible, tight, and potent inhibitor, prevents the ongoing destruction of insoluble elastin by elastase, IC50: 16 nM, 4fold excess of inhibitor over enzyme causes 83% inhibition Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
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, involved in the onset of emphysema, acute respiratory distress syndrome, and rheumatoid arthritis ? protein cleaved at at least one location ?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
neutrophil enzyme released from neutrophils during phagocytosis and upon cell death Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Elastin + H2O
-
 Homo sapiens ?
-
 ?
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, involved in the onset of emphysema, acute respiratory distress syndrome, and rheumatoid arthritis Homo sapiens ? protein cleaved at at least one location ?
methoxysuccinyl-Ala-Ala-Pro-Val-4-nitroanilide + H2O
-
 Homo sapiens methoxysuccinyl-Ala-Ala-Pro-Val + 4-nitroaniline
-
 ?

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0000006
-
 4-(4-bromophenylsulfonylcarbamoyl)benzoyl-L-valyl-L-proline 1 (RS)-(1-trifluoroacetyl-2-methylpropyl)amide
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000016
-
 ICI 200,355, reversible, tight, and potent inhibitor, prevents the ongoing destruction of insoluble elastin by elastase, IC50: 16 nM, 4fold excess of inhibitor over enzyme causes 83% inhibition Homo sapiens 4-(4-bromophenylsulfonylcarbamoyl)benzoyl-L-valyl-L-proline 1 (RS)-(1-trifluoroacetyl-2-methylpropyl)amide