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1,10-phenanthroline
complete inhibition of isoform LAAOII and about 30% inhibition of isoform LAAOI at 5 mM
2-aminobenzoic acid
-
three and two binding sites in isoforms L1 and L2, respectively
6-chloro-8-methoxy-6,11a-dihydro-2H-phenanthro[3,4-d][1,3]dioxole-5-carboxylic acid
derivative of aristolochic acid, significantly inhibits catalytic activity and reduces LAAO-induced cytotoxicity, interferes with the binding of LAAO to the cell membrane but does not interact with DNA. The derivative significantly reduces LAAO-induced ROS generation and cytotoxicity in HEK-293 and HepG2 cell lines
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6-hydroxy-8-methoxy-6,11a-dihydro-2H-phenanthro[3,4-d][1,3]dioxole-5-carboxylic acid
derivative of aristolochic acid, significantly inhibits catalytic activity and reduces LAAO-induced cytotoxicity, interferes with the binding of LAAO to the cell membrane but does not interact with DNA. The derivative significantly reduces LAAO-induced ROS generation and cytotoxicity in HEK-293 and HepG2 cell lines
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Al3+
strong inhibition of both isoforms at 10 mM
alpha,alpha'-dipyridyl
-
15% residual activity at 1 mM
alpha-methyl-L-tyrosine
mixed type inhibitor
alpha-Naphthol
-
12.4% inhibition at 10 mM
aristolochic acid
reversible, mixed inhibition
aromatic carboxylates
-
competitive
bathophenanthroline disulfonic acid
-
-
Butanedione
snake
-
good substrates but not poor substrates protect against inactivation
Chloropromazine
-
inhibition can be relieved by L-arginine
EMD 132338
-
inhibits platelet aggregation induced by LAAO
FAD
activates at 0.002 mM, inhibits at 0.004-0.008 mM
Gd3+
-
inhibits 17% at 10 mM
L-citrulline
pH 7.6, 30°C
L-cysteine
complete inhibition of both isoforms at 5 mM
L-methionine
pH 7.6, 30°C
L-norleucine
pH 7.6, 30°C
L-phenylalanine
pH 7.6, 30°C
La3+
-
LaCl3, La(OOCCH3)3
N-acetyl-L-tryptophan
-
about 90% inhibition at 50 nM
N-acetyl-L-tryptophan amide
-
inhibition of both isoforms L1 and L2
N-acetyltryptophan
-
inhibition of both isoforms L1 and L2
N-ethylmaleimide
-
87% residual activity at 1 mM
N-methyl-L-tyrosine
competitive inhibitor
Na+
-
sodium salts, order of effectiveness: SCN-, NO3-, Cl-, Br-, I-, F-, HCOO-, CH3COO-
NaF
-
10 mM, 85% inhibition
NaN3
-
91% residual activity at 1 mM
nordihydroguaiaretic acid
-
-
o-aminobenzoic acid
LAO inhibitor, slightly inhibiting the degradation of fibrinogen
Pepsin
10 mg/ml, complete inhibition
-
phenylhydrazine
-
complete inhibition at 1 mM (pH 5.5)
phenylmethylsulfonyl fluoride
about 20% inhibition of isoform LAAOII and about 90% inhibition of isoform LAAOI at 5 mM
proteinase K
10 mg/ml, complete inhibition
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reduced glutathione
complete inhibition of both isoforms at 5 mM
riboflavin
-
44.89% inhibition at 10 mM
Thiosemicarbazide
-
5 mM, 40% inhibition
Trypsin
10 mg/ml, complete inhibition
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tunicamycin
-
inhibits secretion of recombinant LAAO
Urea
about 50% inhibition of isoform LAAOII and about 20% inhibition of isoform LAAOI at 5 mM
2-mercaptoethanol
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2-mercaptoethanol
complete inhibition of isoform LAAOII and about 50% inhibition of isoform LAAOI at 5 mM
8-hydroxyquinoline
-
70.07% inhibition at 10 mM
8-hydroxyquinoline
-
2% residual activity at 1 mM
8-hydroxyquinoline
-
76% residual activity at 1 mM (pH 5.5)
anthranilate
-
competitive
Atebrine
-
-
benzoate
-
-
benzoate
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and derivatives
benzoic acid
-
-
benzoic acid
-
complete inhibition at 10 mM
Ca2+
-
-
Ca2+
-
CaCl2, Ca(OOCCH3)2
Ca2+
-
inhibition can be relieved by L-arginine
CaCl2
Synechococcus cedrorum PCC 6908
-
-
Cd2+
-
CdCl2
Co2+
strong inhibition of both isoforms at 10 mM
Co2+
-
88% residual activity at 1 mM
Co2+
-
67% residual activity at 1 mM (pH 5.5)
Cu2+
strong inhibition of both isoforms at 10 mM
Cu2+
-
in presence of the activator Mn2+
EDTA
-
complete inhibition at 10 mM
EDTA
about 40% inhibition of isoform LAAOII and about 10% inhibition of isoform LAAOI at 5 mM
EDTA
-
10 mM, 90% inhibition
EDTA
-
inhibits platelet aggregation induced by LAAO
EDTA
-
86% residual activity at 1 mM
EDTA
the Michaelis constant of LAAO1 decreases and the catalytic constant (Kcat/Km) value increases following pre-treatment with EDTA. EDTA pre-chelated LAAO1 is more active than the non-EDTA treated LAAO1 sample against Staphylococcus aureus ATCC 25923, MRSA clinical isolate 87-7927, and Vibrio parahaemolyticus RIMD2210001
EDTA
-
80% residual activity at 1 mM (pH 5.5)
Fe2+
strong inhibition
Fe2+
-
62% residual activity at 1 mM (pH 5.5)
Fe3+
slight inhibition
Fe3+
-
complete inhibition at 1 mM
glycine
-
29.56% inhibition at 10 mM
glycine
activity strongly decreased in glycine/NaOH-buffer, competitive inhibition, no inhibition, when 10 mM L-phenylanalnine is used as substrate
Hg2+
-
-
Hg2+
-
complete inhibition at 1 mM (pH 7.0)
HgCl
-
-
hydrazine
-
93% residual activity at 1 mM
hydrazine
-
46% residual activity at 1 mM (pH 5.5)
hydroxylamine
-
-
hydroxylamine
-
5 mM, 75% inhibition
hydroxylamine
-
12% residual activity at 1 mM
hydroxylamine
-
63% residual activity at 1 mM (pH 5.5)
iodoacetate
-
iodoacetate
-
75% residual activity at 1 mM
iodoacetic acid
-
-
iodoacetic acid
about 45% inhibition of isoform LAAOII and no inhibition of isoform LAAOI at 5 mM
iodoacetic acid
-
0.5% residual activity at 1 mM (pH 7.0)
K+
-
KCN
-
10 mM, complete inhibition
KCN
-
83% residual activity at 1 mM
KCN
-
70% residual activity at 1 mM (pH 7.0)
L-propargylglycine
-
irreversible inhibition in a dose- and time-dependent manner
L-propargylglycine
-
irreversible inhibition in a dose- and time-dependent manner
m-chlorobenzoate
-
-
m-chlorobenzoate
LAO inhibitor, does not inhibit the degradation of fibrinogen
Mg2+
slight inhibition
Mg2+
-
91% residual activity at 1 mM
Mg2+
-
78% residual activity at 1 mM (pH 5.5)
Mg2+
-
EDTA, ATP and ADP, but not AMP can overcome inhibition
Mn2+
slight inhibition
Mn2+
-
92% residual activity at 1 mM
Mn2+
-
63% residual activity at 1 mM (pH 5.5)
NH4+
-
inhibition of amino acid oxidase activity, no inhibition of L-hydroxy acid oxidase activity
NH4+
-
inhibition of amino acid oxidase activity, no inhibition of L-hydroxy acid oxidase activity
NH4+
-
inhibition of amino acid oxidase activity, no inhibition of L-hydroxy acid oxidase activity
Ni2+
strong inhibition of both isoforms at 10 mM
Ni2+
-
90% residual activity at 1 mM
Ni2+
-
55% residual activity at 1 mM (pH 5.5)
o-phenanthroline
-
84% residual activity at 1 mM
o-phenanthroline
-
15% residual activity at 1 mM (pH 5.5)
p-chloromercuribenzoate
-
-
p-chloromercuribenzoate
-
-
quinine sulfate
-
-
SDS
-
-
Semicarbazide
-
70% residual activity at 1 mM
Semicarbazide
-
32% residual activity at 1 mM (pH 5.5)
Sodium azide
-
49.63% inhibition at 10 mM
Zn2+
-
-
Zn2+
strong inhibition of both isoforms at 10 mM
Zn2+
-
55% residual activity at 1 mM
Zn2+
-
24% residual activity at 1 mM (pH 5.5)
additional information
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no inhibition by caspase III inhibitor benzyloxycarbonyl-Asp(OMe)-fluoromethylketone
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additional information
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antiparasite effects are inhibited by catalase
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additional information
catalase inhibits dose-dependent parasite killing
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additional information
catalase inhibits dose-dependent parasite killing
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additional information
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is inactivated by freezing or low pH. Bactericidal, antitumoral, trypanocidal, edematogenic, platelet-aggregating activities, and apoptotic DNA fragmentation in HL-60 cells are inhibited by catalase
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additional information
not inhibitory: Ca2+, Mg2+ and Mn2+, PMSF, EDTA and glutamic acid
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additional information
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catalase (1.5 micromol) at various concentrations of leucine does not completely inhibit cell death caused by LAAO (1.2 micromol) in leucine auxotrophic strain
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additional information
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not inhibitory: EDTA
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additional information
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substrate inhibition
-
additional information
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good substrates, not poor substrates are inhibitors; substrate inhibition
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additional information
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insensitive to KCN at 1 mM; substrate inhibition
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additional information
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substrate inhibition
-
additional information
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LAAO is not inhibited by carbon monoxide releasing molecule CORM-2 nor by EDTA
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additional information
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initial uncompetitive inhibition of L1 followed by mixed inhibition at higher concentrations suggesting the existence of two different inhibitor-binding sites distinct from the substrate-binding site. In the case of L2, initial linear competitive inhibition followed by mixed inhibition suggesting the existence of two nonoverlapping inhibitor-binding sites, one of which is the substrate-binding site
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additional information
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naturally occuring inhibitors
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additional information
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LAAO has no activity on platelets in platelet-rich plasma. Catalase inhibits the platelet aggregation and platelet protein phosphorylation induced by LAAO
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additional information
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the antibacterial and anti-aggregating activity of LAAO is abolished by catalase
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additional information
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substrate inhibition
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additional information
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antimicrobial activity can be partially inhibited by catalase
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additional information
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catalase almost completely abolishs the antibacterial activity of SSAP, indicating that H2O2 is the mediator of the activity of SSAP
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additional information
catalase almost completely abolishs the antibacterial activity of SSAP, indicating that H2O2 is the mediator of the activity of SSAP
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additional information
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antibacterial activity of SSAP is completely abolished by addition of catalase
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additional information
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antibacterial activities are completely abolished by catalase
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additional information
snake
-
not: 5,5-dithiobis-(2-nitrobenzoic acid), trinitrobenzene sulfonic acid
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additional information
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inhibition by cations increases in alkaline pH, inhibition by anions increases in acidic pH
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