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3.4.24.26: pseudolysin

This is an abbreviated version!
For detailed information about pseudolysin, go to the full flat file.

Word Map on EC 3.4.24.26

Reaction

Hydrolysis of proteins including elastin, collagen types III and IV, fibronectin and immunoglobulin A, generally with bulky hydrophobic group at P1'. Insulin B chain cleavage pattern identical to that of thermolysin, but specificity differs in other respects =

Synonyms

A2 elastase, aeruginolysin, ealastase LasB, EC 3.4.24.4, elastase, elastase B, elastolytic metalloproteinase, EPa, LasB, LasB protease, LepA, More, Neutral metalloproteinase, PAE, PASP, PE, PsE, Pseudomonas aeruginosa elastase, Pseudomonas aeruginosa neutral metalloproteinase, Pseudomonas aeruginosa small protease, Pseudomonas elastase, Pseudomonas protease

ECTree

     3 Hydrolases
         3.4 Acting on peptide bonds (peptidases)
             3.4.24 Metalloendopeptidases
                3.4.24.26 pseudolysin

Inhibitors

Inhibitors on EC 3.4.24.26 - pseudolysin

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INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
1,10-phenanthroline
1,4-dithiothreitol
-
5 mM, 0% residual activity
1-(biphenyl-4-ylmethyl)-3-hydroxy-2-methylpyridine-4(1H)-thione
-
-
2,2'-bipyridine
-
slight inhibition
2-mercaptoacetyl-L-phenyalanyl-L-leucine
-
-
2-mercaptoacetyl-L-phenylalanyl-L-leucine
prevents corneal perforation completely
2-mercaptoacetyl-Leu-Dphe
-
2-mercaptoacetyl-Leu-Phe
-
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
2-mercaptoacetylphenylalanylleucine
specific
2-mercaptoethanol
-
18.8% inhibition at 5 mM
2-[(biphenyl-4-ylsulfonyl)[2-(hydroxyamino)-2-oxoethyl]amino]-N-[2-(4-sulfamoylphenyl)ethyl]acetamide (non-preferred name)
-
-
2-[benzyl[2-(hydroxyamino)-2-oxoethyl]amino]-N-[2-(4-sulfamoylphenyl)ethyl]acetamide (non-preferred name)
-
the phenyl group of the strong binder occupies the S'2-subpocket, while a second ring system occupy the S1-subpocket in both thermolysin, EC 3.4.24.27, and pseudolysin
2-[benzyl[2-(hydroxyamino)-2-oxoethyl]amino]-N-[3-(4-phenylpiperazin-1-yl)propyl]acetamide (non-preferred name)
-
the phenyl group of the strong binder occupies the S'2-subpocket, while a second ring system occupy the S1-subpocket in both thermolysin, EC 3.4.24.27, and pseudolysin
2-[[2-(hydroxyamino)-2-oxoethyl][(4-methoxyphenyl)sulfonyl]amino]-N-[2-(4-sulfamoylphenyl)ethyl]acetamide (non-preferred name)
-
-
2-[[2-(hydroxyamino)-2-oxoethyl][(4-phenoxyphenyl)sulfonyl]amino]-N-[2-(4-sulfamoylphenyl)ethyl]acetamide (non-preferred name)
-
-
3-(2-furyl)acryloyl-glycine
-
3-(2-furyl)acryloyl-glycyl-L-phenylalanyl-L-phenylalanine
-
5-fluorouracil
-
-
ammonium chloride
extracellular elastase activity decreases if cells are cultured in the presence of ammonium chloride
anti elastase monoclonal antibody
reduces PE activity significantly
-
Aprotinin
-
markedly decreases enzymatic activity
Ba2+
-
5 mM, slightly decreases activity
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
benzyloxycarbonyl-L-leucine
-
benzyloxycarbonyl-L-leucyl-hydroxamate
-
benzyloxycarbonyl-L-phenylalanine
-
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
benzyloxycarbonyl-Phe-NHOH
-
Cd2+
-
5 mM, decreases activity
cetyltrimethylammonium bromide
-
0.1%, 53% residual activity
CH2ICOOH
WP_084338031.1
3 mM,88 % inhibition
ClCH2CO-HOLeu-Ala-Gly-NH2
non-competitive
ClCH2CO-N-hydroxyleucine-Ala-Gly-NH2
-
-
D-glucose
extracellular elastase activity decreases if cells are cultured in the presence of glucose
dehydroleucodine
-
-
DTT
WP_084338031.1
3 mM, 24% inhibition
elastase propeptide
-
-
Elastatinal
-
markedly decreases enzymatic activity
eriodictyol
-
-
HS-CH2-CO-Phe-Tyr-NH2
-
at 0.2 mM and 0.025 mM inhibits the degradation of the pseudolysin natural substrates nucleoside diphosphate kinase and IgG, respectively
HSAc-Leu-Phe
-
0.1 mM, inhibits 97% of the degradation of azocasein and elastin substrates by pseudolysin
HSAc-Phe-Leu
-
0.1 mM, inhibits 97% of the degradation of azocasein and elastin substrates by pseudolysin
HSCH2(DL)CH[CH2CH(CH3)2]CO-Phe-Ala-NH2
2 isomeric forms
L-cysteine
-
complete inhibition at 1.25 mM
L-phenylalanyl-L-phenylalanine
-
N-(1-carboxy-3-phenylpropyl)-phenylalanyl-alpha-asparagine
enzyme binding structure analysis, PDB ID 1U4G. The inhibitor is bound in the S1-S1’ sub-sites of pseudolysin by hydrogen bonding and hydrophobic and weak van der Waal's interactions
N-aryl mercaptoacetamide
-
-
N-mercaptoacetyl-Phe-Tyr-amide
-
-
N-[(2R)-1-(hydroxyamino)-3-methyl-1-oxobutan-2-yl]-N-[(4-phenoxyphenyl)sulfonyl]glycine
-
-
Na2 EDTA
-
complete inhibition at 10 mM
o-phenanthroline
peptides
-
containing the hydroxamic acid, N-hydroxypeptide and thiol functional groups
Phosphoramidate
-
-
phosphoramidon
phosphoryl-L-leucyl-L-phenylalanine
S-homoPhe [N-alpha-alpha]Phe-IsoAsn
L-155542, competitive
sodium dodecylsulfate
-
0.1%, 61% residual activity
sodium sulfite
WP_084338031.1
3 mM, 94% inhibition
Soybean trypsin inhibitor
-
markedly decreases enzymatic activity
-
specific polyclonal rabbit antielastase antiserum
-
-
Streptomyces metalloproteinase inhibitor
-
i.e. SMPI, molecular dynamics study of enzyme-inhibitor complex. Inhibitor interacts with pseudolysin via the rigid active side loop and several contact sites outside this loop
-
TLCK
-
markedly decreases enzymatic activity
Zincov
zinc chelator
[(biphenyl-4-ylmethyl)[2-(hydroxyamino)-2-oxoethyl]amino]acetic acid
-
-
[(biphenyl-4-ylsulfonyl)[2-(hydroxyamino)-2-oxoethyl]amino]acetic acid
-
-
[1-[2-(hydroxyamino)-2-oxoethyl]-2-[3-(4-phenylpiperazin-1-yl)propyl]hydrazinyl]acetic acid
-
-
[[(4-methoxyphenyl)sulfonyl](2-oxo-2-[[2-(4-sulfamoylphenyl)ethyl]amino]ethyl)amino]acetic acid
-
-
[[2-(hydroxyamino)-2-oxoethyl](4-nitrobenzyl)amino]acetic acid
-
-
[[2-(hydroxyamino)-2-oxoethyl](4-phenoxybenzyl)amino]acetic acid
-
-
[[2-(hydroxyamino)-2-oxoethyl][(4-methoxyphenyl)sulfonyl]amino]acetic acid
-
-
[[2-(hydroxyamino)-2-oxoethyl][(4-phenoxyphenyl)sulfonyl]amino]acetic acid
-
-
additional information
-