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1-ethyl-3-(3-dimethylaminopropyl)-carbodiimide
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-
2-Pyrrolidinone
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1 mM inhibits by 44%
4-(2-aminoethyl)-benzenesulfonylfluoride
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-
5,5'-dithiobis(2-nitrobenzoic acid)
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activity is restored by 2-mercaptoethanol
Acid thyroliberin
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competitive inhibition of thyroliberin hydrolysis
Anorexogenic peptide
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competitive inhibition of thyroliberin hydrolysis
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bestatin
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inhibits soluble PAP-I in the hippocampus by 14.8% and in the hypothalamus by 14.4%. Inhibition of membrane-bound PAP-I in the hypothalamus by 8.8%
bradykinin-potentiating peptide 5a
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competitive inhibition of thyroliberin hydrolysis
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Chelating agents
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strong
Dithiobisnitrobenzoate
-
-
E64
0.1 mM, 15% inhibition
Eledoisin
-
competitive inhibition of thyroliberin hydrolysis
formic acid ethyl ester
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-
iodoacetic acid
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0.1 mM completely inhibits
L-trans-epoxysuccinyl-leucylamide-(4-guanido)-butane
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i.e. E-64, partial
Luliberin
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competitive inhibition of thyroliberin hydrolysis
luteinizing hormone releasing hormone 1-5
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-
Luteinizing hormone-releasing hormone
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inhibits hydrolysis of thyrotropin-releasing hormone
Nalpha-benzyloxycarbonyl-L-pyroglutamyl chloromethylketone
natural oligosaccharide gum from Hakea gibbosa
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effective non-competitive inhibitor. The natural gum may be a promising additive not only for its sustained-release and mucoadhesive properties, but also for its ability to slow the enzymatic degradation of therapeutic polypeptides incorporated in dosage forms
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neurotensin
-
competitive inhibition of thyroliberin hydrolysis
p-chloromercuribenzoate
1 mM, activity is completely lost
p-hydroxymercuribenzoate
-
-
peptidic calpain inhibitor
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i.e. EP-475, partial
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phenylmethylsulfonyl fluoride
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1 mM inhibits by 53.4%
pyroglutamic acid-Ala
-
competitive inhibitor
pyroglutamic acid-His-Pro-NH2
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thyrotropin-releasing hormone, relative highest affinity, competitive inhibitor
pyroglutamic acid-Val
-
competitive inhibitor
pyroglutamyl-His methyl ester
-
inhibits hydrolysis of thyrotropin-releasing hormone
pyroglutamyl-L-dopa-Pro-NH2
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inhibits hydrolysis of thyrotropin-releasing hormone
1,10-phenanthroline
-
-
2-Iodoacetamide
-
-
2-Pyrrolidone
-
-
2-Pyrrolidone
-
competitive
8-hydroxyquinoline
-
-
amastatin
-
-
amastatin
-
inhibits soluble PAP-I in the hippocampus by 12.5% and in the hypothalamus by 13.8%. Does not inhibit membrane-bound PAP-I
Ca2+
-
weak inhibition
Ca2+
1 mM, 20% inhibition
Cd2+
-
-
Co2+
-
Cu2+
-
-
Cu2+
1 mM, 96% inhibition
Cu2+
-
1 mM inhibits by 91.3%
Cu2+
-
strong, even at 0.5 mM
DTT
-
weak
EDTA
-
-
EDTA
-
95% stimulation at pH 8.0, no effect at pH 6.5
EGTA
-
-
Fe3+
-
weak inhibition
Hg2+
-
HgCl2
iodoacetamide
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weak
iodoacetamide
-
0.1 mM strongly inhibits by 98.3%
iodoacetate
-
-
N-ethylmaleimide
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0.1 mM strongly inhibits by 98.1%
N-ethylmaleimide
1 mM, activity is completely lost
Nalpha-benzyloxycarbonyl-L-pyroglutamyl chloromethylketone
-
-
Nalpha-benzyloxycarbonyl-L-pyroglutamyl chloromethylketone
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inactive towards the D-isomer
NEM
-
-
Ni2+
-
NiSO4, weak
Ni2+
0.1 mM, 98% inhibition
Ni2+
-
1 mM inhibits by 99%, 0.1 mM inhibits by 48%
PCMB
-
-
PCMB
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reversible reactivation by mercaptoethanol
PMSF
-
-
puromycin
-
-
puromycin
-
inhibits soluble PAP-I in the hippocampus by 15.5% and in the hypothalamus by 42.5%. Inhibition of membrane-bound PAP-I in the hippcampus by 11.5%
Sodium tetrathionate
-
-
Zn2+
-
-
Zn2+
1 mM, 98% inhibition
Zn2+
-
1 mM inhibits by 80.2%
Zn2+
-
inhibits soluble PAP-1 in the hippocampus and hypothalamus, does not inhibit membrane-bound PAP-I
Zn2+
-
strong, even at 0.5 mM
additional information
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postive linear correlation between pKi and the carbon chain length for a homologous series of n-alkanols up to C5
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additional information
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Ca2+, Mg2+, Na+, Li+, pepstatin A, 1,10-phenanthroline, benzamidine, bestatin and trans-epoxysuccinyl-L-leucylamido-(4-guanidino)butane have no or little inhibitory effect
-
additional information
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not inhibited by phenyl methyl sulphonyl fluoride. 28% reduced activity of soluble PAP-I and 40-45% reduced activity of membrane-bound PAP-I in both the hippocampus and hypothalamus of streptozotocin-diabetic rats. Changes can be mitigated by concomitant treatment with insulin
-
3.4.19.3 pyroglutamyl-peptidase I
results (
results (
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