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(1-aminopropane-1,3-diyl)bis(phosphonic acid)
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(3R)-3-amino-3-phosphonopropanoic acid
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(4R)-4-amino-5-sulfanylpentanoic acid
a linear competitive inhibitor
(R)-3-amino-4-mercaptobutane-1-sulfonic acid
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i.e. EC33
(S)-3-amino-4-mercapto-butyl sulfonic acid
(S)-3-amino-4-mercapto-butylsulfonic acid
(S)-3-amino-4-mercaptobutyl sulfonic acid
2,6-diaminohexane-1-thiol
a linear competitive inhibitor
2-amino-4-methylsulfonyl butane thiol
2-mercaptoethanol
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58% inhibition at 0.01 mM, 96% at 0.1 mM
3-amino-3-[hydroxy(phenyl)phosphoryl]propanoic acid
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3-amino-4-thio-butyl sulfonate
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3-amino-4-thio-butyl sulfonic acid
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EC33, specific and selective APA inhibitor
3-[(1-amino-2-carboxyethyl)(hydroxy)phosphoryl]-2-methylpropanoic acid
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3-[[amino(carboxy)methyl](hydroxy)phosphoryl]-2-methylpropanoic acid
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4,4'-dithio [bis[(3S)-3-aminobutyl sulfonic acid]]
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i.e. RB150
4,4'-dithio[bis(3)-aminobutylsulfonic acid]
4,4'-dithio[bis(3-aminobutyl sulfonic acid)]
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RB150, a prodrug of EC33
4-amino-4-phosphonobutyric acid
a specific and selective APA inhibitor, a linear competitive inhibitor
5-amino-5-phosphonopentanoic acid
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acetic acid
inactivates at 50% w/v
Ala-PSI[PO2-CH2]-Leu-Ala
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amastin
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3% residual activity at a concentration of 0.001 mM
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amino(phosphono)acetic acid
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amino[hydroxy(methyl)phosphoryl]acetic acid
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angiotensin II
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competitive against Glu-4-methylcoumaryl-7-amide, IC50 is 0.065 mM in presence of Ca2+
angiotensin III
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competitive against Glu-4-methylcoumaryl-7-amide
aspartate hydroxamate
-
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cholecystokinin-8
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competitive against Glu-4-methylcoumaryl-7-amide, IC50 is 0.024 mM in presence of Ca2+
chromogranin A
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competitive against Glu-4-methylcoumaryl-7-amide, IC50 is 0.049 mM in presence of Ca2+
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D-glutamate phosphonic acid
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diisopropylfluorophosphate
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Glu-PSI[PO2-CH2]-Leu-Ala
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Glu-PSI[PO2-CH2]-Leu-Arg
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Glu-PSI[PO2-CH2]-Leu-Asp
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Glu-PSI[PO2-CH2]-Leu-Leu
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glutamate phosphonic acid
kallidin
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competitive against Glu-4-methylcoumaryl-7-amide
L-alpha-glutaryl-L-phenylalanine
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L-Glu
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product inhibition of enzyme Lc-PepA, 8.4% inhibition at 0.1 mM, 17.7% at 10 mM, product inhibition versus substrate L-Asp-4-nitroanilide, and 1.47% inhibition at 0.1 mM, 31.4% at 10 mM, product inhibition versus substrate L-Glu-4-nitroanilide
L-glutamate phosphinic acid
L-glutamate phosphonic acid
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leupeptin
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slight inhibition at 1 mM
methionine-thiol
a linear competitive inhibitor
Mg2+
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inhibits the activity with Glu-substrate moderately
N-(2-aminoethyl)-4-methyl-5-sulfanyl-pentanamide
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neurokinin B
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competitive against Glu-4-methylcoumaryl-7-amide,IC50 is 0.060 mM in presence of Ca2+
p-hydroxymercuribenzoate
-
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parathyroid hormone residues 69-84
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-
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pepstatin A
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slight inhibition
phenylmethylsulfonyl fluoride
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ZnCl2
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0% residual activity at a concentration of 1 mM
[Ag2(E-6-(hydroxyimino)ethyl-1,3,7-trimethyl-pteridine-2,4(1H,3H)-dione)2(CF3SO3)2(EtOH)]n x nEtOH
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compound shows cytotoxicity against both U373-MG abd NB-69 cell lines. NB-69 cells need higher concentrations of silver complexes than U373-MG cells to obtain a 50% growth inhibition. All compounds tested show apoptotic effects, with U373-MG cells being more susceptible. The silver complexes tested also show a dose-dependent inhibitory effect on aminopeptidase A activity in NB-69 and U373-MG cells, although U373-MG cells are more sensitive
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[Ag2(E-6-(hydroxyimino)ethyl-1,3,7-trimethyl-pteridine-2,4(1H,3H)-dione)2(ClO4)2]n
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compound shows cytotoxicity against both U373-MG abd NB-69 cell lines. NB-69 cells need higher concentrations of silver complexes than U373-MG cells to obtain a 50% growth inhibition. All compounds tested show apoptotic effects, with U373-MG cells being more susceptible. The silver complexes tested also show a dose-dependent inhibitory effect on aminopeptidase A activity in NB-69 and U373-MG cells, although U373-MG cells are more sensitive
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[Ag2(E-6-(hydroxyimino)ethyl-1,3,7-trimethyl-pteridine-2,4(1H,3H)-dione)2(NO3)2]n
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compound shows cytotoxicity against both U373-MG abd NB-69 cell lines. NB-69 cells need higher concentrations of silver complexes than U373-MG cells to obtain a 50% growth inhibition. All compounds tested show apoptotic effects, with U373-MG cells being more susceptible. The silver complexes tested also show a dose-dependent inhibitory effect on aminopeptidase A activity in NB-69 and U373-MG cells, although U373-MG cells are more sensitive
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[[(2R,3R)-3-amino-2-sulfhydryl-5-sulfonate]pentanoyl]-D-Ile-Asp-OH
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[[(2R,3R)-3-amino-2-sulfhydryl-5-sulfonate]pentanoyl]-Ile-3-sulfoalanine-OH
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[[(2R,3R)-3-amino-2-sulfhydryl-5-sulfonate]pentanoyl]-Ile-Asp-OH
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[[(2R,3R)-3-amino-2-sulfhydryl-5-sulfonate]pentanoyl]-Ile-D-Asp-OH
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[[(2R,3R)-3-amino-2-sulfhydryl-5-sulfonate]pentanoyl]-Ile-NH2
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[[(2R,3R)-3-amino-2-sulfhydryl-5-sulfonate]pentanoyl]-Ile-OH
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[[(2R,3R)-3-amino-2-sulfhydryl-5-sulfonate]pentanoyl]-Tyr-Asp-OH
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[[(2R,3R)-3-amino-2-sulfhydryl-5-sulfonate]pentanoyl]-Tyr-homosulfoalanine-OH
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[[(2R,3R)-3-amino-5-carboxylate-2-sulfhydryl]pentanoyl]-Ile-Asp-OH
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[[(2R,3R)-3-amino-5-phosphonate-2-sulfhydryl]pentanoyl]-Ile-Asp-OH
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[[(2R,3S)-3-amino-2-sulfhydryl-5-sulfonate]pentanoyl]-Ile-Asp-OH
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[[(2R,3S)-3-amino-5-carboxylate-2-sulfhydryl]pentanoyl]-Ile-Asp-OH
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[[(2RS,3RS)-3-amino2-sulfhydryl-5-sulfamoyl]pentane]-Ile-Asp-OH
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[[(2RS,3RS)-3-amino2-sulfhydryl-5-sulfamoyl]pentanoyl]-Ile-Asp-OH
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[[(2RS,3RS)-3-amino2-sulfhydryl-5-sulfamoyl]pentanoyl]-Tyr-Asp-OH
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[[(2S,3R)-3-amino-2-sulfhydryl-5-sulfonate]pentanoyl]-D-Ile-Asp-OH
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[[(2S,3R)-3-amino-2-sulfhydryl-5-sulfonate]pentanoyl]-Ile-3-sulfoalanine-OH
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[[(2S,3R)-3-amino-2-sulfhydryl-5-sulfonate]pentanoyl]-Ile-Asp-OH
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[[(2S,3R)-3-amino-2-sulfhydryl-5-sulfonate]pentanoyl]-Ile-D-Asp-OH
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[[(2S,3R)-3-amino-2-sulfhydryl-5-sulfonate]pentanoyl]-Ile-NH2
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[[(2S,3R)-3-amino-2-sulfhydryl-5-sulfonate]pentanoyl]-Ile-OH
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[[(2S,3R)-3-amino-2-sulfhydryl-5-sulfonate]pentanoyl]-Tyr-Asp-OH
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[[(2S,3R)-3-amino-2-sulfhydryl-5-sulfonate]pentanoyl]-Tyr-homosulfoalanine-OH
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[[(2S,3R)-3-amino-5-carboxylate-2-sulfhydryl]pentanoyl]-Ile-Asp-OH
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[[(2S,3R)-3-amino-5-phosphonate-2-sulfhydryl]pentanoyl]-Ile-Asp-OH
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[[(2S,3S)-3-amino-2-sulfhydryl-5-sulfonate]pentanoyl]-Ile-Asp-OH
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[[(2S,3S)-3-amino-5-carboxylate-2-sulfhydryl]pentanoyl]-Ile-Asp-OH
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(S)-3-amino-4-mercapto-butyl sulfonic acid
i.e. EC33, a selective APA inhibitor, docking analysis in the presence of Ca2+, the ligand interacts with S1 subsite of Arg-878 in murine APA, three-dimensional structure modelling reavealing a change in the volume of the S1 subsite, which may impair the binding and/or the optimal positioning of the substrate in the active site as well as its hydrolysis, overview
(S)-3-amino-4-mercapto-butyl sulfonic acid
i.e. EC33
(S)-3-amino-4-mercapto-butylsulfonic acid
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specific and selective aminopeptidase A inhibitor
(S)-3-amino-4-mercapto-butylsulfonic acid
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specific and selective APA inhibitor
(S)-3-amino-4-mercaptobutyl sulfonic acid
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EC33, specific and selective APA inhibitor
(S)-3-amino-4-mercaptobutyl sulfonic acid
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EC33, specific and selective APA inhibitor
1,10-phenanthroline
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1,10-phenanthroline
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0% residual activity at a concentration of 1 mM
1,10-phenanthroline
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IC50 is 0.06 mM
1,10-phenanthroline
21% at 1.0 mM, complete inhibition at 10 mM
1,10-phenanthroline
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reactivation by Co2+ or Zn2+
1,10-phenanthroline
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complete inhibition at 1-10 mM
2-amino-4-methylsulfonyl butane thiol
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weak inhibitor of aminopeptidase A
2-amino-4-methylsulfonyl butane thiol
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weak inhibitor of APA
4,4'-dithio[bis(3)-aminobutylsulfonic acid]
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RB150, a prodrug of EC33
4,4'-dithio[bis(3)-aminobutylsulfonic acid]
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RB150, a prodrug of EC33
acetone
21.5% inhibition at 4.2% v/v
acetone
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37.2% inhibition at 4.2% v/v
amastatin
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amastatin
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stereoisomers and analogues
amastatin
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inhibits the enzyme and blocks the metabolism of brain angiotensin II and III
amastatin
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IC50 is 157 nM
amastatin
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inhibits the enzyme and blocks the metabolism of brain angiotensin II and III
amastatin
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inhibits APA and APN
amastatin
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inhibits the enzyme and blocks the metabolism of brain angiotensin II and III
amastatin
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an APA inhibitor, enzyme inhibition leads to increased blood pressure
amastatin
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inhibits APA and APN
amastatin
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inhibits the enzyme and blocks the metabolism of brain angiotensin II and III
angiotensin IV
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competitive feedback inhibition, negative regulatory function in absence or presence of Ca2+; IC50 is 0.010 mM
bestatin
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38% residual activity at a concentration of 0.03 mM
bestatin
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inhibits the enzyme and blocks the metabolism of brain angiotensin II and III
bestatin
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inhibits the enzyme and blocks the metabolism of brain angiotensin II and III
bestatin
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broad specificity for various aminopeptidases
bestatin
1 mM, 13% residual activity
bestatin
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inhibits the enzyme and blocks the metabolism of brain angiotensin II and III
bestatin
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broad specificity for various aminopeptidases
bestatin
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inhibits the enzyme and blocks the metabolism of brain angiotensin II and III
Ca2+
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substrate-specific inhibition, overview
Ca2+
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inhibits activity with Gln-substrate, regulatory function and influence on substrate specificity
Ca2+
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Ca2+ up- or down-regulates the enzyme activity depending on the substrate tested
Ca2+
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substrate-specific inhibition, overview
Ca2+
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Ca2+ up- or down-regulates the enzyme activity depending on the substrate tested
Ca2+
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substrate-specific inhibition, overview
Ca2+
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Ca2+ up- or down-regulates the enzyme activity depending on the substrate tested
Ca2+
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substrate-specific inhibition, overview
captopril
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-
Cd2+
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complete inhibition at 1 mM
Cd2+
complete inhibition at 1 mM
Cd2+
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complete inhibition at 1 mM
Cu2+
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complete inhibition at 1 mM
Cu2+
complete inhibition at 1 mM
Cu2+
5 mM, 3.5% residual activiy
Cu2+
-
complete inhibition at 1 mM
dimethylformamide
78.1% inhibition at 4.2% v/v
dimethylformamide
-
84.9% inhibition at 4.2% v/v
dithiothreitol
-
-
DMSO
15.1% inhibition at 4.2% v/v
DMSO
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13.9% inhibition at 4.2% v/v
DTT
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32% activity at 0.1 mM
DTT
12% inhibition at 0.1 mM
DTT
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69% inhibition at 0.001 mM, 94% at 0.1 mM
E64
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slight inhibition at 1 mM
EC33
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specific inhibition
EC33
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highly selective APA inhibitor
EC33
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highly selective APA inhibitor
EC33
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highly selective APA inhibitor
EC33
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specific inhibition
EC33
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highly selective APA inhibitor
EDTA
-
-
EDTA
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7% residual activity at a concentration of 5 mM
EDTA
-
83.5% activity at 5 mM
EDTA
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reactivation by Co2+
EDTA
complete inhibition at 1.0 mM
EDTA
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reactivation by Co2+
EDTA
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complete inhibition at 1.0 mM
EDTA
10 mM, 3.7% residual activiy
EDTA
activity is reduced to 14% after incubating with 10 mM EDTA
EGTA
-
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ethanol
16.3% inhibition at 4.2% v/v
ethanol
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25.7% inhibition at 4.2% v/v
glutamate phosphonate
0.001 mM, activity of wild-type enzyme is completely abolished
glutamate phosphonate
specific aminopeptidase A inhibitor
glutamate phosphonic acid
-
glutamate phosphonic acid
-
-
Hg2+
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complete inhibition at 1 mM
Hg2+
complete inhibition at 1 mM
Hg2+
-
complete inhibition at 1 mM
imidazole
34% inhibition at 40 mM
imidazole
-
21% inhibition at 40 mM
L-Asp
39.5% inhibition at 10 mM, no inhibition at 0.1-1.0 mM, product inhibition versus substrate L-Asp-4-nitroanilide, and 33.8% inhibition at 10 mM and no inhibition at 0.1-1.0 mM, product inhibition versus substrate L-Glu-4-nitroanilide
L-Asp
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21.8% inhibition at 10 mM and no inhibition at 0.1-1.0 mM, product inhibition versus substrate L-Asp-4-nitroanilide, and 24.0% inhibition at 10 mM and no inhibition at 0.1-1.0 mM, product inhibition versus substrate L-Glu-4-nitroanilide
L-glutamate phosphinic acid
-
-
L-glutamate phosphinic acid
-
-
methionine thiol
-
-
Mn2+
-
inhibits the activity with Glu-substrate moderately
Mn2+
5 mM, 15% residual activiy
Ni2+
-
complete inhibition at 1 mM
Ni2+
complete inhibition at 1 mM
Ni2+
-
complete inhibition at 1 mM
o-phenanthroline
-
47.1% activity at 2 mM
o-phenanthroline
activity is reduced to 8.3% after incubating with 20 mM o-phenanthroline
PMSF
35% inhibition at 10 mM
PMSF
-
32% inhibition at 10 mM
RB150
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selective and specific prodrug of the enzyme inhibitor EC33, inhibits the enzyme given i.v. to rats
RB150
selective and specific prodrug of the enzyme inhibitor EC33, inhibits the enzyme given i.v. to rats
RB150
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selective and specific prodrug of the enzyme inhibitor EC33, inhibits the enzyme given i.v. to mice
RB150
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selective and specific prodrug of the enzyme inhibitor EC33, inhibits the enzyme given i.v. to rats
SDS
73% at 1.0 mM, complete inhibition at 10 mM
SDS
-
63% at 1.0 mM, 97% inhibition at 10 mM
Zn2+
-
complete inhibition at 1 mM
Zn2+
-
68.3% activity at 0.4 mM
Zn2+
-
zinc-metallopeptidase, inhibits the activity with Glu- and Gln-substrates
Zn2+
complete inhibition at 1 mM
Zn2+
Zn2+ abolishes enzyme activity at a concentration of 1 mM
Zn2+
-
complete inhibition at 1 mM
additional information
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inhibitory effects of peptide hormones on enzyme activity in presence or absence of Ca2+, overview, no or poor inhibition by 4-(amidinophenyl)-methanesulfonyl fluoride, pepstatin, and bestatin
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additional information
enzyme Lb-PepA is not product-inhibited by L-Glu. Lb-PepA activity decreases significantly with metal salt concentrations above the optimum concentrations determined. Poor inhibition at 1.0 mM 2-mercaptoethanol, no inhibition by pepstatin A at 0.1-10 mM
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additional information
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enzyme Lb-PepA is not product-inhibited by L-Glu. Lb-PepA activity decreases significantly with metal salt concentrations above the optimum concentrations determined. Poor inhibition at 1.0 mM 2-mercaptoethanol, no inhibition by pepstatin A at 0.1-10 mM
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additional information
enzyme Lb-PepA is not product inhibited by glutamic acid
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additional information
no enzyme inhibition by leptin, but reduction of enzyme level in blood, although not in kidney
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additional information
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no enzyme inhibition by leptin, but reduction of enzyme level in blood, although not in kidney
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additional information
ligand docking study and molecular dynamics simulations with wild-type and mutant enzymes, overview
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additional information
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ligand docking study and molecular dynamics simulations with wild-type and mutant enzymes, overview
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