Information on EC 3.4.11.20 - aminopeptidase Ey

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The expected taxonomic range for this enzyme is: Eukaryota, Bacteria

EC NUMBER
COMMENTARY hide
3.4.11.20
-
RECOMMENDED NAME
GeneOntology No.
aminopeptidase Ey
-
REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
differs from other aminopeptidases in broad specificity for amino acids in the P1 position and the ability to hydrolyse peptides of four or five residues that contain Pro in the P1' position
show the reaction diagram
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
hydrolysis of peptide bond
-
-
exopeptidase
-
CAS REGISTRY NUMBER
COMMENTARY hide
9031-94-1
-
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
-
UniProt
Manually annotated by BRENDA team
strain FcB1
-
-
Manually annotated by BRENDA team
Xanthomonas axonopodis citri
-
-
Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
malfunction
-
inhibition caused swelling of the parasite digestive vacuole and prevented proteolysis of hemoglobin derived oligopeptides, likely starving the parasite resulting in death; inhibition is lethal to parasites early in the life cycle, prior to the onset of hemoglobin degradation
physiological function
-
synthesized as the precursor p120 form, targeted to the parasitophorous vacuole via the parasite endoplasmic reticulum/Golgi, where it is converted into the transient p96 form; p96 form is eventually redirected into the parasite to be converted into the processed p68 form that is only marginally delivered to the parasite foodvacuole
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
(S)-2-amino-4-cyclohexylbutanoyl-7-amido-4-methylcoumarin + H2O
(S)-2-amino-4-cyclohexylbutanoic acid + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
?
Ala-7-amido-4-methylcoumarin + H2O
alanine + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
?
Arg-Ala + H2O
L-Arg + L-Ala
show the reaction diagram
-
-
-
-
?
Arg-Pro-Lys-Pro + H2O
Arg + Pro-Lys-Pro
show the reaction diagram
Arg-Pro-Pro-Gly-Phe + H2O
Arg + Pro-Pro-Gly-Phe
show the reaction diagram
-
bradikinin fragment 1-5, no hydrolysis of bradikinin
-
?
Arg-Tyr-Leu-Pro-Thr + H2O
?
show the reaction diagram
-
insect neuropeptide
-
-
?
cholecystokinin octapeptide + H2O
tyrosine sulfate + Asp + Met + Gly + Trp + Met-Asp-Phe-NH2
show the reaction diagram
-
i.e. Asp-tyrosyl sulfate-Met-Gly-Trp-Met-Asp-Phe-NH2
-
-
?
Gly-p-nitroanilide + H2O
Gly + p-nitroaniline
show the reaction diagram
-
58.5% activity compared to L-Pro-p-nitroanilide
-
-
?
His-Ala + H2O
L-His + L-Ala
show the reaction diagram
-
-
-
-
?
homoargininyl-7-amido-4-methylcoumarin + H2O
homoarginine + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
?
homophenylalanyl-7-amido-4-methylcoumarin + H2O
homophenylalanine + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
?
L-Ala 4-nitroanilide + H2O
L-Ala + 4-nitroaniline
show the reaction diagram
-
-
-
-
?
L-Ala-p-nitroanilide + H2O
L-Ala + p-nitroaniline
show the reaction diagram
-
55.4% activity compared to L-Pro-p-nitroanilide
-
-
?
L-alanyl-2-naphthylamide + H2O
L-alanine + 2-naphthylamine
show the reaction diagram
-
-
-
?
L-Arg 4-nitroanilide + H2O
L-Arg + 4-nitroaniline
show the reaction diagram
-
-
-
-
?
L-arginyl-2-naphthylamide + H2O
L-arginine + 2-naphthylamine
show the reaction diagram
-
-
-
?
L-His-2-naphthylamide + H2O
L-His + 2-naphthylamine
show the reaction diagram
-
31.6% activity compared to L-Pro-p-nitroanilide
-
-
?
L-Ile-2-naphthylamide + H2O
L-Ile + 2-naphthylamine
show the reaction diagram
-
4.6% activity compared to L-Pro-p-nitroanilide
-
-
?
L-Leu 4-nitroanilide + H2O
L-Leu + 4-nitroaniline
show the reaction diagram
-
-
-
-
?
L-Leu-4-methylumbelliferyl + H2O
L-leucine + 4-methylumbelliferol
show the reaction diagram
-
-
-
-
?
L-Leu-4-nitroanilide + H2O
L-leucine + 4-nitroaniline
show the reaction diagram
-
-
-
-
?
L-Leu-7-amido-4-methyl-coumarin + H2O
L-leucine + 7-amino-4-methyl-coumarin
show the reaction diagram
-
-
-
?
L-Leu-7-amido-4-methylcoumarin + H2O
L-leucine + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
?
L-Leu-p-nitroanilide + H2O
L-Leu + p-nitroaniline
show the reaction diagram
L-leucyl-7-amido-4-methylcoumarin + H2O
L-leucine + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
L-Lys 4-nitroanilide + H2O
L-Lys + 4-nitroaniline
show the reaction diagram
-
-
-
-
?
L-Lys-p-nitroanilide + H2O
L-Lys + p-nitroaniline
show the reaction diagram
-
13% activity compared to L-Pro-p-nitroanilide
-
-
?
L-Met-p-nitroanilide + H2O
L-Met + p-nitroaniline
show the reaction diagram
-
11.5% activity compared to L-Pro-p-nitroanilide
-
-
?
L-methionyl-7-amido-4-methylcoumarin + H2O
L-methionine + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
?
L-Phe-p-nitroanilide + H2O
L-Phe + p-nitroaniline
show the reaction diagram
-
1.1% activity compared to L-Pro-p-nitroanilide
-
-
?
L-Pro-2-naphthylamide + H2O
L-Pro + 2-naphthylamine
show the reaction diagram
-
100% activity
-
-
?
L-Pro-p-nitroanilide + H2O
L-Pro + p-nitroaniline
show the reaction diagram
-
100% activity
-
-
?
L-Ser-2-naphthylamide + H2O
L-Ser + 2-naphthylamine
show the reaction diagram
-
64% activity compared to L-Pro-2-naphthylamide
-
-
?
L-Trp-2-naphthylamide + H2O
L-Trp + 2-naphthylamine
show the reaction diagram
-
15.6% activity compared to L-Pro-p-nitroanilide
-
-
?
L-Tyr-2-naphthylamide + H2O
L-Tyr + 2-naphthylamine
show the reaction diagram
-
30.3% activity compared to L-Pro-p-nitroanilide
-
-
?
L-Val-p-nitroanilide + H2O
L-Val + p-nitroaniline
show the reaction diagram
-
5.3% activity compared to L-Pro-p-nitroanilide
-
-
?
Leu 4-methylcoumarin 7-amide + H2O
?
show the reaction diagram
-
-
-
-
?
Leu 4-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
Leu-Ala + H2O
L-Leu + L-Ala
show the reaction diagram
-
-
-
-
?
Leu-enkephalin + H2O
?
show the reaction diagram
-
i.e. Tyr-Gly-Gly-Phe-Met, stepwise degradation from the N-terminus
-
-
?
Leu-Gly + H2O
L-Leu + Gly
show the reaction diagram
-
-
-
-
?
Leu-Gly-Gly + H2O
?
show the reaction diagram
-
-
-
-
?
Leu-Gly-Leu + H2O
?
show the reaction diagram
-
-
-
-
?
Leu-Gly-NH2 + H2O
?
show the reaction diagram
-
-
-
-
?
Leu-Gly-Pro + H2O
?
show the reaction diagram
-
-
-
-
?
Leu-Leu + H2O
2 L-Leu
show the reaction diagram
-
-
-
?
Leu-Leu-Tyr + H2O
Leu + Leu-Tyr
show the reaction diagram
-
-
-
-
?
Leu-NH2 + H2O
L-Leu + NH3
show the reaction diagram
-
-
-
-
?
Leu-Pro-Leu-Arg-Phe-NH2 + H2O
Leu + Pro-Leu-Arg-Phe-NH2
show the reaction diagram
-
a chicken brain pentapeptide
-
-
?
Leu-Pro-Leu-Arg-PheNH2 + H2O
Leu + Pro-Leu-Arg-PheNH2
show the reaction diagram
-
i.e. chicken brain peptide
resistant to the enzyme
?
Lys-Ala + H2O
L-Lys + L-Ala
show the reaction diagram
-
-
-
-
?
Lys-Ala-Met-Cys-Ala + H2O
?
show the reaction diagram
-
-
-
-
?
Lys-Phe-Ile-Gly-Leu-Met-NH2 + H2O
?
show the reaction diagram
-
eledoisin-related peptide, lysine, phenylalanine, isoleucine, glycine and leucine are liberated from the aminoterminus, methionine is not released from Met-NH2 of the final product
-
-
?
Met-Phe + H2O
L-Met + Phe
show the reaction diagram
-
-
-
?
N-formyl-Met-Leu-Phe(fMLP) + H2O
N-formyl-Met + Leu-Phe(fMLP)
show the reaction diagram
-
-
-
-
?
norleucyl-7-amido-4-methylcoumarin + H2O
norleucine + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
?
norvalinyl-7-amido-4-methylcoumarin + H2O
norvaline + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
?
Pro-Phe-Gly-Lys + H2O
Pro + Phe + Gly-Lys
show the reaction diagram
-
-
-
-
?
Pro-Phe-Gly-Lys + H2O
Pro + Phe-Gly-Lys
show the reaction diagram
-
-
-
?
proctolin + H2O
?
show the reaction diagram
-
-
-
-
?
styryl-Ala-7-amido-4-methylcoumarin + H2O
styryl-alanine + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
?
tuftsin + H2O
?
show the reaction diagram
-
-
-
-
?
additional information
?
-
NATURAL SUBSTRATES
NATURAL PRODUCTS
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
N-formyl-Met-Leu-Phe(fMLP) + H2O
N-formyl-Met + Leu-Phe(fMLP)
show the reaction diagram
-
-
-
-
?
additional information
?
-
-
the enzyme functiones in regulation of hormone function and thus is involved in diverse biological processes, it offers a biodefense against the infectious microbial product N-formyl-peptide
-
-
-
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
additional information
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(2S,17S,20S,21R)-21-amino-5-(4-benzoylbenzyl)-2-[4-(hex-5-ynoylamino)butyl]-20-hydroxy-17-(naphthalen-2-ylmethyl)-4,7,16,19-tetraoxo-22-phenyl-9,12-dioxa-3,6,15,18-tetraazadocosan-1-amide
-
;
1,10-phenanthroline
1-hydroxy-2-oxo-1,2-dihydro-quinoline-3-carboxylic acid (4-phenyl-butyl)-amide
-
-
1-hydroxy-2-oxo-1,2-dihydro-quinoline-3-carboxylic acid 4-fluoro-benzylamide
-
-
2-(4-benzyl-piperidine-1-carbonyl)-4-methyl-pentanoic acid hydroxyamide
-
-
2-benzyl-3-(3,4-dihydro-1H-isoquinolin-2-yl)-N-hydroxy-3-oxo-propionamide
-
-
2-benzyl-3-(4-benzyl-piperazin-1-yl)-N-hydroxy-3-oxo-propionamide
-
-
2-benzyl-3-(4-benzyl-piperidin-1-yl)-N-hydroxy-3-oxo-propionamide
-
-
2-benzyl-N-(2,2-diphenyl-ethyl)-N'-hydroxy-malonamide
-
-
2-benzyl-N-(4-chloro-benzyl)-N'-hydroxy-malonamide
-
-
2-benzyl-N-(4-fluoro-benzyl)-N'-hydroxy-malonamide
-
-
2-benzyl-N-biphenyl-3-ylmethyl-N'-hydroxy-malonamide
-
-
2-benzyl-N-hydroxy-N'-(2-methyl-benzyl)-malonamide
-
-
2-benzyl-N-hydroxy-N'-(3-phenoxy-benzyl)-malonamide
-
-
2-benzyl-N-hydroxy-N'-(3-phenyl-propyl)-malonamide
-
-
2-benzyl-N-hydroxy-N'-(4-phenyl-butyl)-malonamide
-
-
2-benzyl-N-hydroxy-N'-indan-2-yl-malonamide
-
-
2-benzyl-N-hydroxy-N'-naphthalen-1-ylmethyl-malonamide
-
-
2-benzyl-N-hydroxy-N'-phenethyl-malonamide
-
-
2N-dibenzyl-N'-hydroxy-malonamide
-
-
3-(3,4-dihydro-1H-isoquinolin-2-yl)-N-hydroxy-3-oxo-2-(3-phenoxy-benzyl)-propionamide
-
-
3-(4-benzyl-piperidin-1-yl)-N-hydroxy-3-oxo-2-(3-phenoxybenzyl)-propionamide
-
-
bestatin
bestatin methyl ester
-
-
betaine
-
complete inhibition at 2 mM
hPhe-PSI[PO2CH2]-Phe
-
phosphinic dipeptide analog
N-(1-(4-(1H-pyrazol-1-yl)phenyl)-2-(hydroxyamino)-2-oxoethyl)-3-aminobenzamide
-
highly effective against the malaria parasites, IC50 values of 233 nM; highly effective against the malaria parasites, IC50 values of 233 nM
N-(1-(4-(1H-pyrazol-1-yl)phenyl)-2-(hydroxyamino)-2-oxoethyl)-4-aminobenzamide
-
highly effective against the malaria parasites, IC50 values of 283 nM; highly effective against the malaria parasites, IC50 values of 283 nM
N-(1-(4-(1H-pyrazol-1-yl)phenyl)-2-(hydroxyamino)-2-oxoethyl)-pivalamide
-
most effective inhibitor of isoform M1 and one of the more potent inhibitors of isoform M17 tested, the most effective compound against 3D7 malaria parasites, with an IC50 of 227 nM; most effective inhibitor of isoform M1 and one of the more potent inhibitors of isoform M17 tested, the most effective compound against 3D7 malaria parasites, with an IC50 of 227 nM
N-(4-chloro-benzyl)-N'-hydroxy-2-(3-phenoxy-benzyl)-malonamide
-
-
N-(4-chloro-benzyl)-N'-hydroxy-2-isobutyl-malonamide
-
-
N-(4-fluoro-benzyl)-N'-hydroxy-2-isobutyl-malonamide
-
-
N-(4-fluoro-benzyl)-N'-hydroxy-2-[1-phenyl-meth-(E)-ylidene]-malonamide
-
-
N-(4-fluoro-benzyl)-N'-hydroxy-2-[1-phenyl-meth-(Z)-ylidene]-malonamide
-
-
N-benzyl-N'-hydroxy-2-(3-phenoxy-benzyl)-malonamide
-
-
N-benzyl-N'-hydroxy-2-isobutyl-malonamide
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25C
N-hydroxy-2-(3-phenoxy-benzyl)-N'-(3-phenyl-propyl)-malonamide
-
-
N-hydroxy-2-(3-phenoxy-benzyl)-N'-(4-phenyl-butyl)-malonamide
-
-
N-hydroxy-2-(3-phenoxy-benzyl)-N'-(4-trifluoromethyl-benzyl)-malonamide
-
-
N-hydroxy-2-isobutyl-N'-(1,2,3,4-tetrahydro-naphthalen-1-yl)-malonamide
-
-
N-hydroxy-2-isobutyl-N'-(3-phenoxy-benzyl)-malonamide
-
-
N-hydroxy-2-isobutyl-N'-(3-phenyl-propyl)-malonamide
-
-
N-hydroxy-2-isobutyl-N'-(4-phenyl-butyl)-malonamide
-
-
N-hydroxy-2-isobutyl-N'-naphthalen-1-ylmethyl-malonamide
-
-
N-hydroxy-2-isobutyl-N'-phenethyl-malonamide
-
-
N-hydroxy-N'-(4-phenyl-butyl)-2-[1-phenyl-meth-(Z)-ylidene]-malonamide
-
-
N-[(2-[2-[(N-[(2S,3R)-3-amino-4-[4-(benzyloxy)phenyl]-2-hydroxybutanoyl]-L-alanyl)amino]ethoxy]ethoxy)acetyl]-4-benzoylphenylalanyl-N6-hex-5-ynoyl-L-lysinamide
-
;
N-[(2S,3R)-3-amino-2-hydroxy-4-(4-methoxyphenyl)butanoyl]-L-leucine
-
-
N-[(2S,3R)-3-amino-2-hydroxy-4-(naphthalen-2-yl)butanoyl]-L-leucine
-
-
N-[(2S,3R)-3-amino-2-hydroxy-4-phenylbutanoyl]-L-norleucine
-
-
N-[(2S,3R)-3-amino-2-hydroxyheptanoyl]-L-leucine
-
-
N-[(2S,3R)-3-amino-4-[4-(benzyloxy)phenyl]-2-hydroxybutanoyl]-L-leucine
-
-
N2-[(2S,3R)-3-amino-2-hydroxy-4-phenylbutanoyl]-N6-[(benzyloxy)carbonyl]-L-lysine
-
-
OF 4949-II
tert-butyl (1-(4-(1H-Pyrazol-1-yl)phenyl)-2-(hydroxyamino)-2-oxoethyl)carbamate
-
compound shows good in vitro inhibitory properties, but IC50 for parasite growth is only 783 nM, suggesting that compounds substituted with the N-Boc group are either less capable of cellular penetration or less stable than the corresponding N-acyl derivatives; compound shows good in vitro inhibitory properties, but IC50 for parasite growth is only 783 nM, suggesting that compounds substituted with the N-Boc group are either less capable of cellular penetration or less stable than the corresponding N-acyl derivatives
tosedostat
-
i.e. (2S)-([(2R)-2-[(1S)-1-hydroxy-2-(hydroxyamino)-2-oxoethyl]-4-methylpentanoyl]amino)(phenyl)ethanoic acid, crystal structure; i.e. (2S)-({(2R)-2-[(1S)-1-hydroxy-2-(hydroxyamino)-2-oxoethyl]-4-methylpentanoyl}amino)(phenyl)ethanoic acid, crystal structure
Zn2+
-
0.1 mM, 80% inhibition
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0236
4-cyclohexyl-L-butyric acid-7-amido-4-methylcoumarin
pH 7.4, 37C
0.0598
Ala-7-amido-4-methylcoumarin
pH 7.4, 37C
0.4 - 9
Arg-Ala
4.2 - 35
His-Ala
0.0277
homoargininyl-7-amido-4-methylcoumarin
pH 7.4, 37C
0.0262
homophenylalanyl-7-amido-4-methylcoumarin
pH 7.4, 37C
0.304
L-Ala 4-nitroanilide
-
pH 7.2, 37C
0.21 - 4.4
L-alanyl-2-naphthylamide
0.27
L-Arg 4-nitroanilide
-
pH 7.2, 37C
0.086 - 1.1
L-arginyl-2-naphthylamide
0.248
L-Lys 4-nitroanilide
-
pH 7.2, 37C
0.0314
L-methionyl-7-amido-4-methylcoumarin
pH 7.4, 37C
0.01 - 0.8
Leu 4-methylcoumarin 7-amide
0.64 - 10
Leu-Ala
0.95
Leu-Gly
-
pH 7.5, 30C
0.7
Leu-Gly-Gly
-
pH 7.5, 30C
0.015
Leu-Gly-Leu
-
pH 7.5, 30C
0.42
Leu-Gly-NH2
-
pH 7.5, 30C
0.2
Leu-Gly-Pro
-
pH 7.5, 30C
0.13 - 1.2
Leu-Leu
4.9
Leu-NH2
-
pH 7.5, 30C
0.58
Leu-Pro-Leu-Arg-PheNH2
-
-
0.43 - 8.9
Lys-Ala
0.022 - 0.38
Met-Phe
0.0165
norleucyl-7-amido-4-methylcoumarin
pH 7.4, 37C
0.0354
norvalinyl-7-amido-4-methylcoumarin
pH 7.4, 37C
0.0302
styryl-Ala-7-amido-4-methylcoumarin
pH 7.4, 37C
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.737
4-cyclohexyl-L-butyric acid-7-amido-4-methylcoumarin
Eimeria tenella
V5T9T8
pH 7.4, 37C
0.456
Ala-7-amido-4-methylcoumarin
Eimeria tenella
V5T9T8
pH 7.4, 37C
9.5 - 15
Arg-Ala
1 - 2.4
His-Ala
0.575
homoargininyl-7-amido-4-methylcoumarin
Eimeria tenella
V5T9T8
pH 7.4, 37C
0.836
homophenylalanyl-7-amido-4-methylcoumarin
Eimeria tenella
V5T9T8
pH 7.4, 37C
1.15
L-Ala 4-nitroanilide
Plasmodium falciparum
-
pH 7.2, 37C
3 - 16
L-alanyl-2-naphthylamide
1.58
L-Arg 4-nitroanilide
Plasmodium falciparum
-
pH 7.2, 37C
9.3 - 21
L-arginyl-2-naphthylamide
1.65
L-Leu 4-nitroanilide
Plasmodium falciparum
-
pH 7.2, 37C
1.55
L-Lys 4-nitroanilide
Plasmodium falciparum
-
pH 7.2, 37C
0.704
L-methionyl-7-amido-4-methylcoumarin
Eimeria tenella
V5T9T8
pH 7.4, 37C
9.3 - 12
Leu-Ala
6.5
Leu-Gly
Plasmodium falciparum
-
pH 7.5, 30C
21
Leu-Gly-Gly
Plasmodium falciparum
-
pH 7.5, 30C
4.8
Leu-Gly-Leu
Plasmodium falciparum
-
pH 7.5, 30C
21
Leu-Gly-NH2
Plasmodium falciparum
-
pH 7.5, 30C
12
Leu-Gly-Pro
Plasmodium falciparum
-
pH 7.5, 30C
1.4 - 12
Leu-Leu
12
Leu-NH2
Plasmodium falciparum
-
pH 7.5, 30C
0.1
Leu-Pro-Leu-Arg-PheNH2
Gallus gallus
-
-
27
Lys-Ala
Plasmodium falciparum
-
pH 5.5, 30C; pH 7.5, 30C
5.9 - 7.5
Met-Phe
0.71
norleucyl-7-amido-4-methylcoumarin
Eimeria tenella
V5T9T8
pH 7.4, 37C
0.658
norvalinyl-7-amido-4-methylcoumarin
Eimeria tenella
V5T9T8
pH 7.4, 37C
0.577
styryl-Ala-7-amido-4-methylcoumarin
Eimeria tenella
V5T9T8
pH 7.4, 37C
kcat/KM VALUE [1/mMs-1]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
31.3
4-cyclohexyl-L-butyric acid-7-amido-4-methylcoumarin
Eimeria tenella
V5T9T8
pH 7.4, 37C
202212
7.6
Ala-7-amido-4-methylcoumarin
Eimeria tenella
V5T9T8
pH 7.4, 37C
20648
1.7 - 23
Arg-Ala
7382
0.027 - 0.56
His-Ala
12553
20.8
homoargininyl-7-amido-4-methylcoumarin
Eimeria tenella
V5T9T8
pH 7.4, 37C
202213
31.9
homophenylalanyl-7-amido-4-methylcoumarin
Eimeria tenella
V5T9T8
pH 7.4, 37C
202211
4.24
L-Ala 4-nitroanilide
Plasmodium falciparum
-
pH 7.2, 37C
49145
3.7 - 170
L-alanyl-2-naphthylamide
18585
5.84
L-Arg 4-nitroanilide
Plasmodium falciparum
-
pH 7.2, 37C
202217
8.7 - 130
L-arginyl-2-naphthylamide
8729
5.42
L-Leu 4-nitroanilide
Plasmodium falciparum
-
pH 7.2, 37C
48302
6.24
L-Lys 4-nitroanilide
Plasmodium falciparum
-
pH 7.2, 37C
202216
22.4
L-methionyl-7-amido-4-methylcoumarin
Eimeria tenella
V5T9T8
pH 7.4, 37C
168606
1.2 - 14
Leu-Ala
3822
6.8
Leu-Gly
Plasmodium falciparum
-
pH 7.5, 30C
1721
30
Leu-Gly-Gly
Plasmodium falciparum
-
pH 7.5, 30C
4026
330
Leu-Gly-Leu
Plasmodium falciparum
-
pH 7.5, 30C
20353
49
Leu-Gly-NH2
Plasmodium falciparum
-
pH 7.5, 30C
6652
60
Leu-Gly-Pro
Plasmodium falciparum
-
pH 7.5, 30C
20354
1.2 - 97
Leu-Leu
2851
2.4
Leu-NH2
Plasmodium falciparum
-
pH 7.5, 30C
5174
3 - 65
Lys-Ala
4264
19 - 270
Met-Phe
7389
43
norleucyl-7-amido-4-methylcoumarin
Eimeria tenella
V5T9T8
pH 7.4, 37C
202210
18.6
norvalinyl-7-amido-4-methylcoumarin
Eimeria tenella
V5T9T8
pH 7.4, 37C
202215
19.1
styryl-Ala-7-amido-4-methylcoumarin
Eimeria tenella
V5T9T8
pH 7.4, 37C
202214
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.000029 - 0.00033
(2S,17S,20S,21R)-21-amino-5-(4-benzoylbenzyl)-2-[4-(hex-5-ynoylamino)butyl]-20-hydroxy-17-(naphthalen-2-ylmethyl)-4,7,16,19-tetraoxo-22-phenyl-9,12-dioxa-3,6,15,18-tetraazadocosan-1-amide
0.000025 - 0.0038
bestatin
0.00048
bestatin methyl ester
-
pH 5.5, 37C; pH 7.5, 37C
0.000013
hPhe-PSI[PO2CH2]-Phe
-
pH and temperature not specified in the publication
0.000014 - 0.0055
N-(1-(4-(1H-pyrazol-1-yl)phenyl)-2-(hydroxyamino)-2-oxoethyl)-3-aminobenzamide
0.000011 - 0.0074
N-(1-(4-(1H-pyrazol-1-yl)phenyl)-2-(hydroxyamino)-2-oxoethyl)-4-aminobenzamide
0.000028 - 0.0007
N-(1-(4-(1H-pyrazol-1-yl)phenyl)-2-(hydroxyamino)-2-oxoethyl)-pivalamide
0.00026 - 0.004
N-[(2-[2-[(N-[(2S,3R)-3-amino-4-[4-(benzyloxy)phenyl]-2-hydroxybutanoyl]-L-alanyl)amino]ethoxy]ethoxy)acetyl]-4-benzoylphenylalanyl-N6-hex-5-ynoyl-L-lysinamide
0.000043
N-[(2S,3R)-3-amino-2-hydroxy-4-(4-methoxyphenyl)butanoyl]-L-leucine
-
pH 7.5, temperature not specified in the publication
0.003
N-[(2S,3R)-3-amino-2-hydroxy-4-(naphthalen-2-yl)butanoyl]-L-leucine
-
pH 7.5, temperature not specified in the publication
0.0009
N-[(2S,3R)-3-amino-2-hydroxy-4-phenylbutanoyl]-L-norleucine
-
pH 7.5, temperature not specified in the publication
0.0053
N-[(2S,3R)-3-amino-2-hydroxyheptanoyl]-L-leucine
-
pH 7.5, temperature not specified in the publication
0.00049
N-[(2S,3R)-3-amino-4-[4-(benzyloxy)phenyl]-2-hydroxybutanoyl]-L-leucine
-
pH 7.5, temperature not specified in the publication
0.00145
N2-[(2S,3R)-3-amino-2-hydroxy-4-phenylbutanoyl]-N6-[(benzyloxy)carbonyl]-L-lysine
-
pH 7.5, temperature not specified in the publication
0.00003 - 0.0008
tert-butyl (1-(4-(1H-Pyrazol-1-yl)phenyl)-2-(hydroxyamino)-2-oxoethyl)carbamate
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.01
1-hydroxy-2-oxo-1,2-dihydro-quinoline-3-carboxylic acid (4-phenyl-butyl)-amide
Plasmodium falciparum
-
IC50 above 0.01 mM, in Tris-HCl buffer (25 mM, pH 7.4), at 25C
0.01
1-hydroxy-2-oxo-1,2-dihydro-quinoline-3-carboxylic acid 4-fluoro-benzylamide
Plasmodium falciparum
-
IC50 above 0.01 mM, in Tris-HCl buffer (25 mM, pH 7.4), at 25C
0.000406
2-(4-benzyl-piperidine-1-carbonyl)-4-methyl-pentanoic acid hydroxyamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25C
0.000253
2-benzyl-3-(3,4-dihydro-1H-isoquinolin-2-yl)-N-hydroxy-3-oxo-propionamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25C
0.00176
2-benzyl-3-(4-benzyl-piperazin-1-yl)-N-hydroxy-3-oxo-propionamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25C
0.000206
2-benzyl-3-(4-benzyl-piperidin-1-yl)-N-hydroxy-3-oxo-propionamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25C
0.005363
2-benzyl-N-(2,2-diphenyl-ethyl)-N'-hydroxy-malonamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25C
0.00017
2-benzyl-N-(4-chloro-benzyl)-N'-hydroxy-malonamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25C
0.000027
2-benzyl-N-(4-fluoro-benzyl)-N'-hydroxy-malonamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25C
0.001168
2-benzyl-N-biphenyl-3-ylmethyl-N'-hydroxy-malonamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25C
0.000041
2-benzyl-N-hydroxy-N'-(2-methyl-benzyl)-malonamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25C
0.002515
2-benzyl-N-hydroxy-N'-(3-phenoxy-benzyl)-malonamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25C
0.000125
2-benzyl-N-hydroxy-N'-(3-phenyl-propyl)-malonamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25C
0.000046
2-benzyl-N-hydroxy-N'-(4-phenyl-butyl)-malonamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25C
0.001931
2-benzyl-N-hydroxy-N'-indan-2-yl-malonamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25C
0.000107
2-benzyl-N-hydroxy-N'-naphthalen-1-ylmethyl-malonamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25C
0.001011
2-benzyl-N-hydroxy-N'-phenethyl-malonamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25C
0.000125
2N-dibenzyl-N'-hydroxy-malonamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25C
0.000966
3-(3,4-dihydro-1H-isoquinolin-2-yl)-N-hydroxy-3-oxo-2-(3-phenoxy-benzyl)-propionamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25C
0.000248
3-(4-benzyl-piperidin-1-yl)-N-hydroxy-3-oxo-2-(3-phenoxybenzyl)-propionamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25C
0.00013
N-(4-chloro-benzyl)-N'-hydroxy-2-(3-phenoxy-benzyl)-malonamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25C
0.000904
N-(4-chloro-benzyl)-N'-hydroxy-2-isobutyl-malonamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25C
0.003896
N-(4-fluoro-benzyl)-N'-hydroxy-2-isobutyl-malonamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25C
0.00033
N-(4-fluoro-benzyl)-N'-hydroxy-2-[1-phenyl-meth-(E)-ylidene]-malonamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25C
0.000006
N-(4-fluoro-benzyl)-N'-hydroxy-2-[1-phenyl-meth-(Z)-ylidene]-malonamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25C
0.000164
N-benzyl-N'-hydroxy-2-(3-phenoxy-benzyl)-malonamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25C
0.000495
N-benzyl-N'-hydroxy-2-isobutyl-malonamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25C
0.000527
N-hydroxy-2-(3-phenoxy-benzyl)-N'-(3-phenyl-propyl)-malonamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25C
0.000225
N-hydroxy-2-(3-phenoxy-benzyl)-N'-(4-phenyl-butyl)-malonamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25C
0.000231
N-hydroxy-2-(3-phenoxy-benzyl)-N'-(4-trifluoromethyl-benzyl)-malonamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25C
0.000109
N-hydroxy-2-isobutyl-N'-(1,2,3,4-tetrahydro-naphthalen-1-yl)-malonamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25C
0.000045
N-hydroxy-2-isobutyl-N'-(3-phenoxy-benzyl)-malonamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25C
0.00079
N-hydroxy-2-isobutyl-N'-(3-phenyl-propyl)-malonamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25C
0.001149
N-hydroxy-2-isobutyl-N'-(4-phenyl-butyl)-malonamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25C
0.000091
N-hydroxy-2-isobutyl-N'-naphthalen-1-ylmethyl-malonamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25C
0.000885
N-hydroxy-2-isobutyl-N'-phenethyl-malonamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25C
0.000013
N-hydroxy-N'-(4-phenyl-butyl)-2-[1-phenyl-meth-(Z)-ylidene]-malonamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25C
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
3083
-
purified enzyme
additional information
-
-
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
6.5
-
plasma enzyme
7.8
-
granule enzyme
pH RANGE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
5.5 - 9.5
-
pure native enzyme, substrate L-Leu-7-amido-4-methylcoumarin
pI VALUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
2.8
-
isoelectric focusing, holoenzyme
4.4
-
isoelectric focusing, asialo enzyme form
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY hide
GeneOntology No.
LITERATURE
SOURCE
-
plasma of egg yolk
-
Manually annotated by BRENDA team
-
intraerythroytic parasite
Manually annotated by BRENDA team
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
37000
-
4 * 37000, SDS-PAGE, His-tagged enzyme
37250
-
4 * 37250, dynamic light scattering, His-tagged enzyme
106130
-
x * 106130, calculated for recombinant protein including His-tag
120000
-
x * 120000, x * complex of 68000 and 35000 (generated by proteolytic cleveage within the loop sequence containing Leu-796 without N-terminal extension (residue 1-194))
148000
-
His-tagged enzyme, SDS-PAGE
149000
-
His-tagged enzyme, dynamic light scattering
150000
-
2 * 150000
300000
-
low angle laser light scattering-HPLC
343000
-
gel filtration
360000
-
plasma enzyme, gel filtration
700000
-
granule enzyme, gel filtration
SUBUNITS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
homohexamer
tetramer
-
4 * 37000, SDS-PAGE, His-tagged enzyme; 4 * 37250, dynamic light scattering, His-tagged enzyme
additional information
-
the native enzyme contains 14% alpha helix and 68% beta-sheet, while the apoenzyme contains only 6% alpha helix, and 70% beta-sheet, tertiary structure
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
glycoprotein
-
-
proteolytic modification
isoform APN1 is synthesized as a 120-kDa precursor and cleaved into 96-, 68-, and 38-kDa forms during sporulation
Crystallization/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
hanging drop vapour diffusion method
-
in complex with inhibitor tosedostat. The inhibitor occupies the enzymes' putative product egress channels in addition to the substrate binding pockets. Inhibitor adopts different binding poses when bound to isoforms M1, and M17; in complex with inhibitor tosedostat. The inhibitor occupies the enzymes' putative product egress channels in addition to the substrate binding pockets. Inhibitor adopts different binding poses when bound to isoforms M1, and M17
-
pH STABILITY
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
5 - 8.5
-
at least 90% activity after 60 min
717834
TEMPERATURE STABILITY
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
30
-
10 min, pH 7.5, plasma enzyme stable
60
-
10 min, pH 7.5, 20% loss of plasma enzyme activity, activation of granule enzyme
70
-
10 min, pH 7.5, complete loss of activity of plasma enzyme, 60% loss of activity of granule enzyme
Purification/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
amino acid residue 192-1085 as His-tagged protein: immobilized metal ion affinity chromatography (Ni2+), His-tag removed, gel filtration; from a modified parasite line expressing an enzyme with a C-terminal hemagglutinin tag: ion exchange chromatography, gel filtration
-
enzyme form from egg yolk plasma fraction and from granule fraction
-
Hi-Trap Ni2+-chelating column chromatography
-
immobilized metal ion affinity chromatography (Ni2+), gel filtration
-
p68 form, immobilized metal ion affinity chromatography (Ni2+)
-
to homogeneity
-
Cloned/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
amino acid residue 192-1085 expressed in Escherichia coli; His-tagged protein (amino acid residue 79-605) expressed in Escherichia coli
-
expressed in Escherichia coli
-
expressed in Escherichia coli BL21 (DE3) pLysS cells
-
expression in Escherichia coli
-
expression in Escherichia coli; expression in Escherichia coli
-
gene apdE, DNA and amino acid sequence determination and analysis
-
His-tagged p68 form expressed in Escherichia coli BL21(DE3)
-
His-tagged truncated form expressed in Escherichia coli Rosetta2 BL21(DE3)
-
EXPRESSION
ORGANISM
UNIPROT
LITERATURE
isoform APN1 is present during the intracellular life cycle stages in both the parasite cytoplasm and the parasite nucleus
p120 form is expressed in ring stages at least 12 hours before p68 is detected
-
ENGINEERING
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
additional information