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(2S,3R)-3-amino-2-hydroxy-5-methyl-hexanoyl-proline
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(2S,3R)-3-amino-2-hydroxy-5-methylhexanoyl-proline
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1,2-Cylcopentanedicarboxylic acid
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acetic acid
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inhibits the enzyme in colonic tissue, but not in plasma
betulinic acid
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i.e. 3beta-hdroxy-lup-20(29)-en-28-oic acid, inhibits the enzyme and is involved in anti-angiogenesis due to further inhibition of expression and decrease in expressions of alpha1 and alpha2 integrins, hypoxia-inducible factor 1, HIF-1, and vascular endothelial cell growth factor, detailed overview
captopril
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inhibits isozyme PD I dose-dependently, but shows no inhibition of isozyme PD II at 0.1 mM
Colchicine
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colchicine has a slight inhibiting effect on prolidase activity for L-Val-L-Pro, the activity reaches its highest inhibition percentage of 59% at 2.0 mM
Cupferron
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N-Hydroxy-N-nitrosobenzeneamine ammonium salt
D,L-4-Amino-4-phosphonobutyrate
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D,L-homocysteine
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inhibits the activity at 50 mM
D,L-homocysteine-thiolactone
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inhibits the activities of isozymes prolidase I and II in a concentration-dependent manner
daunorubicin
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a cytotoxic anthracycline, inhibits the enzyme and collagen biosynthesis, inhibition mechanism might act via chelating of essential Mn2+ ions, more effective than doxorubicin, also inhibits DNA synthesis
diisopropylfluorophosphate
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87% inhibition at 1 mM
DL-Ethionine
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activates at concentrations of 1-50 mM, overview
DL-homocysteine
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slightly activates at concentrations of 1-20 mM, inhibitory at over 30 mM, overview
DL-homocysteine thiolactone
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activates at concentrations of 1-30 mM, inhibitory at over 50 mM, overview
DL-methionine
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activates at concentrations of 1-30 mM, inhibitory at over 50 mM, overview
doxorubicin
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a cytotoxic anthracycline, inhibits the enzyme and collagen biosynthesis, inhibition mechanism might act via chelating of essential Mn2+ ions, less effective than daunorubicin, also inhibits DNA synthesis
doxycyclin
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induces down-regulation of the enzyme as a post-translational event
echistatin
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treatment of cells results in inhibition of collagen production and enzyme activity and expression
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His-Pro
substrate inhibition
L-isoleucine
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inhibitory to enzyme isoform prolidase I, activating isoform prolidase II
L-leucine
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inhibitory to enzyme isoform prolidase I, activating isoform prolidase II
L-valine
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inhibitory to enzyme isoform prolidase I, activating isoform prolidase II
L-valinyl-D-boroproline
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Leu-Pro
substrate inhibition
Lys-Pro
substrate inhibition
melanin
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30% inhibition at 0.1 mg/ml, reverses inhibition of prolidase by netilmicin
N,N'-diisopropyldiamidofluorophosphate
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i.e. DDFP or mipafox
N-Benzyloxycarbonyl-L-proline
N-[N'-(2-bromoethyl)-N'-nitrosocarbamoyl]-L-proline
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netilmicin
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80% inhibition at 0.01 mM, reversible by melanin
paracetamol
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mechanism of PLD inhibition by paracetamol is noncompetitive inhibition
phenylacetyl-thioproline
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Phenylmethylsulfonylfluoride
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88.5% inhibition at 1 mM
Phosphonocarboxylates
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Pro-Pro
substrate inhibition
trans-1,2-cyclopentanedicarboxylate
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Tyr-Pro
substrate inhibition
Z-Pro
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roughly 80% inhibition at 2.53 mM
1,10-phenanthroline
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2-mercaptoethanol
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1 mM, 55% residual activity
2-mercaptoethanol
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weakly
Ag+
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Cd2+
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Co2+
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slight inhibition at 0.1-1.0 mM
Cu2+
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Cu2+
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85% inhibition at 1 mM
dithiothreitol
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EDTA
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EDTA
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1 mM, 70% residual activity
Hg2+
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Hg2+
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98% inhibition at 1 mM
iodoacetate
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Mg2+
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Mg2+
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slight inhibition at 0.1-1.0 mM
N-Benzyloxycarbonyl-L-proline
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90% inhibition after incubation of cell extracts at a 1:1 ratio of inhibitor to substrate Gly-L-Pro. Long-term incubation of fibroblasts with inhibitor causes mitochondria depolarization and increased cellular death
N-Benzyloxycarbonyl-L-proline
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50% inhibition at 5 mM
N-Benzyloxycarbonyl-L-proline
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N-Benzyloxycarbonyl-L-proline
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competitive, 60-83% inhibition levels of the enzyme from different cancer cell lines, overview
N-Benzyloxycarbonyl-L-proline
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daily injection of inhibitor for 3 weeks results in significant reduction of enzyme activity in erythrocyte. Inhibitor is not degraded in vivo
N-Benzyloxycarbonyl-L-proline
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inhibits isozyme PD I dose-dependently, but shows no inhibition of isozyme PD II at up to 1 mM
N-Benzyloxycarbonyl-L-proline
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inhibits PD I, but not PD II
N-Benzyloxycarbonyl-L-proline
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N-Benzyloxycarbonyl-L-proline
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competitive
Ni2+
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Ni2+
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Ni2+ (0.05 and 0.15mM) is a competitive inhibitor of prolidase with respect to Mn2+
NiCl2
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specific inhibition of enzyme activity in situ. Increasing concentration of Mn2+ stabilizes against Ni2+ inhibition
NiCl2
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inhibits isozye PD II much more effectively than isozyme PD I
p-chloromercuribenzoate
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p-chloromercuribenzoate
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p-chloromercuribenzoate
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p-chloromercuribenzoate
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p-chloromercuribenzoate
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p-chloromercuribenzoate
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p-chloromercuribenzoate
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p-hydroxymercuribenzoate
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p-hydroxymercuribenzoate
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p-hydroxymercuribenzoate
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p-hydroxymercuribenzoate
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Zn2+
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slightly
Zn2+
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56% inhibition at 1 mM
Zn2+
inhibitory above 0.01 mM
additional information
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effects of sulfated amino acids on enzyme-deficient erythrocytes, overview
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additional information
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carmustine does not inhibit MCF-7 cells prolidase activity
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additional information
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no significant effect by 2-mercaptoethanol at 1 mM
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additional information
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insensitive to EDTA
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additional information
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mechanism of inhibition
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