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Literature summary for 3.4.24.26 extracted from

  • Kessler, E.; Israel, M.; Landshman, N.; Chechick, A.; Blumberg, S.
    In vitro inhibition of Pseudomonas aeruginosa elastase by metal-chelating peptide derivatives (1982), Infect. Immun., 38, 716-723.
    View publication on PubMedView publication on EuropePMC

Application

Application Comment Organism
medicine 2-mercaptoacetyl-L-phenylalanyl-L-leucine represents a class of potent elastase inhibitors that might prove useful in the management of Pseudomonas aeruginosa infections Pseudomonas aeruginosa

Inhibitors

Inhibitors Comment Organism Structure
2-mercaptoacetyl-Leu-Dphe
-
Pseudomonas aeruginosa
2-mercaptoacetyl-Leu-Phe
-
Pseudomonas aeruginosa
2-mercaptoacetyl-Phe-Leu at 0.1 mM 96% inhibition with azocasein as substrate, 97% inhibition with elastin as substrate and 97% inhibition with cartilage as substrate, at 0.01 mM 77% inhibition with azocasein as substrate, 33% inhibition with elastin as substrate and 66% inhibition with cartilage as substrate Pseudomonas aeruginosa
benzyloxycarbonyl-Gly-NHOH at 14 mM 98% inhibition with azocasein as substrate, 95% inhibition with elastin as substrate and 95% inhibition with cartilage as substrate, at 1.4 mM 77% inhibition with azocasein as substrate, 84% inhibition with elastin as substrate and 67% inhibition with cartilage as substrate Pseudomonas aeruginosa
benzyloxycarbonyl-L-leucine
-
Pseudomonas aeruginosa
benzyloxycarbonyl-L-phenylalanine
-
Pseudomonas aeruginosa
benzyloxycarbonyl-Leu-NHOH at 5.0 mM 98% inhibition with azocasein as substrate, 100% inhibition with elastin as substrate and 94% inhibition with cartilage as substrate, at 0.5 mM 76% inhibition with azocasein as substrate, 93% inhibition with elastin as substrate and 57% inhibition with cartilage as substrate Pseudomonas aeruginosa
benzyloxycarbonyl-Phe-NHOH
-
Pseudomonas aeruginosa
Leu-Phe
-
Pseudomonas aeruginosa
Phe-Leu
-
Pseudomonas aeruginosa
phosphoryl-L-leucyl-L-phenylalanine at 0.1 mM 98% inhibition with azocasein as substrate, 94% inhibition with elastin as substrate and 98% inhibition with cartilage as substrate, at 0.01 mM 83% inhibition with azocasein as substrate, 87% inhibition with elastin as substrate and 89% inhibition with cartilage as substrate Pseudomonas aeruginosa

Molecular Weight [Da]

Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
35000
-
x * 35000, SDS-PAGE Pseudomonas aeruginosa

Organism

Organism UniProt Comment Textmining
Pseudomonas aeruginosa P14756 Habs serotype 1
-

Purification (Commentary)

Purification (Comment) Organism
-
Pseudomonas aeruginosa

Storage Stability

Storage Stability Organism
-20°C, 0.02 M Tris-hydrochloride, 0.5 mM CaCl2 (pH 7.5), 1 year, less than 10% loss of activity Pseudomonas aeruginosa

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
azocasein + H2O pH 7.5, 37°C Pseudomonas aeruginosa ?
-
?
cartilage + H2O major components proteoglycans and collagen Pseudomonas aeruginosa ?
-
?
Elastin + H2O pH 7.5, 37°C Pseudomonas aeruginosa ?
-
?
furylacryloyl-glycyl-L-leucyl-L-alanine + H2O pH 7.5, 25°C Pseudomonas aeruginosa furylacryloyl-glycine + L-leucyl-L-alanine
-
?

Subunits

Subunits Comment Organism
? x * 35000, SDS-PAGE Pseudomonas aeruginosa

Synonyms

Synonyms Comment Organism
Pseudomonas aeruginosa elastase
-
Pseudomonas aeruginosa

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0002
-
phosphoryl-L-leucyl-L-phenylalanine at pH 7.5 and 25°C, with furylacryloyl-glycyl-L-leucyl-L-alanine as substrate Pseudomonas aeruginosa
0.0002
-
2-mercaptoacetyl-Phe-Leu at pH 7.5 and 25°C, with furylacryloyl-glycyl-L-leucyl-L-alanine as substrate Pseudomonas aeruginosa
0.0015
-
2-mercaptoacetyl-Leu-Phe at pH 7.5 and 25°C, with furylacryloyl-glycyl-L-leucyl-L-alanine as substrate Pseudomonas aeruginosa
0.011
-
benzyloxycarbonyl-Leu-NHOH at pH 7.5 and 25°C, with furylacryloyl-glycyl-L-leucyl-L-alanine as substrate Pseudomonas aeruginosa
0.021
-
benzyloxycarbonyl-Phe-NHOH at pH 7.5 and 25°C, with furylacryloyl-glycyl-L-leucyl-L-alanine as substrate Pseudomonas aeruginosa
0.028
-
benzyloxycarbonyl-Gly-NHOH at pH 7.5 and 25°C, with furylacryloyl-glycyl-L-leucyl-L-alanine as substrate Pseudomonas aeruginosa
0.034
-
2-mercaptoacetyl-Leu-Dphe at pH 7.5 and 25°C, with furylacryloyl-glycyl-L-leucyl-L-alanine as substrate Pseudomonas aeruginosa
0.4
-
Phe-Leu at pH 7.5 and 25°C, with furylacryloyl-glycyl-L-leucyl-L-alanine as substrate Pseudomonas aeruginosa
1.1
-
Leu-Phe at pH 7.5 and 25°C, with furylacryloyl-glycyl-L-leucyl-L-alanine as substrate Pseudomonas aeruginosa
5
-
benzyloxycarbonyl-L-phenylalanine at pH 7.5 and 25°C, with furylacryloyl-glycyl-L-leucyl-L-alanine as substrate Pseudomonas aeruginosa
6.2
-
benzyloxycarbonyl-L-leucine at pH 7.5 and 25°C, with furylacryloyl-glycyl-L-leucyl-L-alanine as substrate Pseudomonas aeruginosa