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Literature summary for 3.4.21.37 extracted from

  • Mulchande, J.; Oliveira, R.; Carrasco, M.; Gouveia, L.; Guedes, R.C.; Iley, J.; Moreira, R.
    4-Oxo-beta-lactams (azetidine-2,4-diones) are potent and selective inhibitors of human leukocyte elastase (2010), J. Med. Chem., 53, 241-253.
    View publication on PubMed
Search for more literature for 3.4.21.37

Inhibitors

Inhibitors Comment Organism Structure
1-(2-((1-methyl-1H-imidazol-2-ylthio)methyl)phenyl)-3,3-diethylazetidine-2,4-dione
-
 Homo sapiens
1-(2-((5-phenyl-1,3,4-oxadiazol-2-ylthio)methyl)phenyl)-3,3-diethylazetidine-2,4-dione
-
 Homo sapiens
1-(2-((benzo[d]oxazol-2-ylthio)methyl)phenyl)-3,3-diethylazetidine-2,4-dione
-
 Homo sapiens
1-(2-((benzo[d]thiazol-2-ylthio)methyl)phenyl)-3,3-diethylazetidine-2,4-dione
-
 Homo sapiens
1-(4-((5-phenyl-1,3,4-oxadiazol-2-ylthio)methyl)phenyl)-3,3-diethylazetidine-2,4-dione
-
 Homo sapiens
1-(4-((benzo[d]oxazol-2-ylthio)methyl)phenyl)-3,3-diethylazetidine-2,4-dione
-
 Homo sapiens
1-(4-((benzo[d]thiazol-2-ylthio)methyl)phenyl)-3,3-diethylazetidine-2,4-dione
-
 Homo sapiens
1-(4-chlorophenyl)-3,3-diethylazetidine-2,4-dione
-
 Homo sapiens
1-(4-chlorophenyl)-3,3-dimethylazetidine-2,4-dione
-
 Homo sapiens
1-(6-((benzo[d]thiazol-2-ylthio)methyl)pyridin-3-yl)-3,3-diethylazetidine-2,4-dione
-
 Homo sapiens
1-benzyl-3,3-dimethylazetidine-2,4-dione
-
 Homo sapiens
2-(4-(3,3-diethyl-2,4-dioxoazetidin-1-yl)benzylthio)benzo[d ]-oxazole-6-carboxylic acid
-
 Homo sapiens
3,3-diethyl-1-(4-((phenylthio)methyl)phenyl)azetidine-2,4-dione
-
 Homo sapiens
3,3-diethyl-1-(4-methoxyphenyl)azetidine-2,4-dione
-
 Homo sapiens
3,3-diethyl-1-(4-methylphenyl)azetidine-2,4-dione
-
 Homo sapiens
3,3-diethyl-1-(6-methylpyridin-3-yl)azetidine-2,4-dione
-
 Homo sapiens
3,3-diethyl-1-(naphthalen-1-yl)azetidine-2,4-dione
-
 Homo sapiens
3,3-diethyl-1-(pyridin-3-yl)azetidine-2,4-dione
-
 Homo sapiens
3,3-diethyl-1-o-tolylazetidine-2,4-dione
-
 Homo sapiens
3,3-diethyl-1-phenylazetidine-2,4-dione
-
 Homo sapiens
3,3-diethyl-1-[4-(naphthalen-2-yloxy)phenyl]azetidine-2,4-dione
-
 Homo sapiens
3,3-dimethyl-1-phenylazetidine-2,4-dione
-
 Homo sapiens
3-benzyl-3-ethyl-1-phenylazetidine-2,4-dione
-
 Homo sapiens
3-benzyl-3-methyl-1-phenylazetidine-2,4-dione
-
 Homo sapiens
3-ethyl-3-isobutyl-1-phenylazetidine-2,4-dione
-
 Homo sapiens
4-(3,3-diethyl-2,4-dioxoazetidin-1-yl)benzonitrile
-
 Homo sapiens
ethyl [4-(3,3-diethyl-2,4-dioxoazetidin-1-yl)phenyl]acetate
-
 Homo sapiens
additional information 4-oxo-beta-lactams are selective and potent inhibitors of leukocyte elastase, 4-oxo-beta-lactams containing a heteroarylthiomethyl group on the para position of an N1-aryl moiety afforded highly potent and selective inhibition of the enzyme, even at a very low inhibitor to enzyme ratio, structure-activity relationship analysis, inhibition mechanisms, molecular modelling, overview Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
extracellular the enzyme is stored in and secreted from neutrophils Homo sapiens
-
-

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
neutrophil
-
 Homo sapiens
-
plasma
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
N-methoxysuccinyl-Ala-Ala-Pro-Val-4-nitroanilide + H2O
-
 Homo sapiens N-methoxysuccinyl-Ala-Ala-Pro-Val + 4-nitroaniline
-
 ?

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
 assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
 assay at Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
additional information
-
 additional information detailed inhibition kinetics of 4-oxo-beta-lactams, overview Homo sapiens

General Information

General Information Comment Organism
physiological function leukocyte elastase is a serine protease stored in and secreted from neutrophils that plays a determinant role in the pathogenesis of several lung diseases Homo sapiens