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Literature summary for 3.4.22.34 extracted from

  • Martinez, M.; Diaz-Mendoza, M.; Carrillo, L.; Diaz, I.
    Carboxy terminal extended phytocystatins are bifunctional inhibitors of papain and legumain cysteine proteinases (2007), FEBS Lett., 581, 2914-2918.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
FaCPI-1 strawberry cystatin, phytocystatin of Fragaria sp. Hordeum vulgare
HvCPI-4 cystatin HvCPI-4 of Hordeum vulgare Hordeum vulgare
HvCPI-4-deltaT143-Cterm C-terminal extended part of cystatin HvCPI-4 Hordeum vulgare
HvCPI-4-deltaT151-Cterm C-terminal extended part of cystatin HvCPI-4 Hordeum vulgare
HvCPI-4-Q86P cystatin HvCPI-4 of Hordeum vulgare, mutant Q86P Hordeum vulgare
additional information inhibitory activity of the phytocystatins HvCPI-4 of Hordeum vulgare and FaCPI-1 of Fragaria sp. measured by the inhibition of legumain proteinase activity, ability of HvCPI-4 and FaCPI-1 to inhibit human legumain in vitro demonstrated Homo sapiens
additional information inhibitory activity measured by the inhibition of legumain proteinase activity, phytocystatins that are able to inhibit human legumain also inhibit the barley legumain proteinase activities in developing roots, endogenous barley legumain activities inhibited by iodoacetamide, no inhibition by the non-legumain inhibitors leupeptin and E64 observed; inhibitory effects against endogenous legumain activity in barley protein extracts tested, inhibitory activity measured by the inhibition of legumain-like proteinase activity, phytocystatins able to inhibit human legumain also inhibit the barley legumain proteinase activities in developing endosperms, endogenous barley legumain activities inhibited by iodoacetamide, no inhibition by the non-legumain inhibitors leupeptin and E64 observed Hordeum vulgare

Organism

Organism UniProt Comment Textmining
Homo sapiens Q99538 Homo sapiens
-
Hordeum vulgare
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legumain activity in barley protein extracts analyzed
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Source Tissue

Source Tissue Comment Organism Textmining
commercial preparation inhibitory effects by phytocystatins against commercial human legumain analyzed Homo sapiens
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endosperm developing endosperms of 18 days after flowering, inhibitory effects by cystatins against endogenous legumain activity in barley protein extracts analyzed Hordeum vulgare
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root collected from plants germinated at 22°C in the dark for 7 days Hordeum vulgare
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Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
additional information
-
ability of carboxy-terminal extensions and mutants of phytocystatin to inhibit endogenous legumain activity present in barley protein extracts analyzed, inhibitory activity measured by the inhibition of legumain proteinase activity, assay described Hordeum vulgare
additional information
-
ability of carboxy-terminal extensions and mutants of phytocystatin to inhibit in vitro human legumain shown, inhibitory activity measured by the inhibition of legumain proteinase activity, assay described Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
benzyloxycarbonyl-Ala-Ala-Asn-4-methylcoumarin-7-amide + H2O inhibitory activity of cystatin variants of Hordeum vulgare against endogenous legumain activity in protein extracts of Hordeum vulgare analyzed Hordeum vulgare benzyloxycarbonyl-Ala-Ala-Asn + 7-amino-4-methylcoumarin
-
?
benzyloxycarbonyl-Ala-Ala-Asn-4-methylcoumarin-7-amide + H2O inhibitory activity of cystatin variants of Hordeum vulgare against endogenous legumain activity in protein extracts of roots of Hordeum vulgare analyzed Hordeum vulgare benzyloxycarbonyl-Ala-Ala-Asn + 7-amino-4-methylcoumarin
-
?
benzyloxycarbonyl-Ala-Ala-Asn-4-methylcoumarin-7-amide + H2O inhibitory activity of phytocystatin variants of Hordeum vulgare tested against commercial human legumain Homo sapiens benzyloxycarbonyl-Ala-Ala-Asn + 7-amino-4-methylcoumarin
-
?

Synonyms

Synonyms Comment Organism
AEP
-
Hordeum vulgare
AEP
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Homo sapiens
asparagine endopeptidase
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Hordeum vulgare
asparagine endopeptidase
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Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00013
-
HvCPI-4-Q86P mutant Q86P of HvCPI-4, inhibitor concentrations between 25 and 500 nM used, incubation with 10 microgram of a soluble endosperm protein extract, at 25°C and pH 6 for 10 min Hordeum vulgare
0.00013
-
HvCPI-4-Q86P mutant Q86P of HvCPI-4, inhibitor concentrations between 25 and 500 nM used, incubation with 5 microgram of a soluble root protein extract, at 25°C and pH 6 for 10 min Hordeum vulgare
0.00019
-
HvCPI-4 inhibitor concentrations between 25 and 500 nM used, incubation with 10 microgram of a soluble endosperm protein extract, at 25°C and pH 6 for 10 min Hordeum vulgare
0.00019
-
HvCPI-4-deltaT143-Cterm inhibitor concentrations between 25 and 500 nM used, incubation with 10 microgram of a soluble endosperm protein extract, at 25°C and pH 6 for 10 min Hordeum vulgare
0.00019
-
HvCPI-4 inhibitor concentrations between 25 and 500 nM used, incubation with 5 microgram of a soluble root protein extract, at 25°C and pH 6 for 10 min Hordeum vulgare
0.00019
-
HvCPI-4-deltaT143-Cterm inhibitor concentrations between 25 and 500 nM used, incubation with 5 microgram of a soluble root protein extract, at 25°C and pH 6 for 10 min Hordeum vulgare
0.00029
-
HvCPI-4-deltaT151-Cterm inhibitor concentrations between 25 and 500 nM used, incubation with 10 microgram of a soluble endosperm protein extract, at 25°C and pH 6 for 10 min Hordeum vulgare
0.00029
-
HvCPI-4-deltaT151-Cterm inhibitor concentrations between 25 and 500 nM used, incubation with 5 microgram of a soluble root protein extract, at 25°C and pH 6 for 10 min Hordeum vulgare
0.00076
-
FaCPI-1 inhibitor concentrations between 25 and 500 nM used, incubation with 10 microgram of a soluble endosperm protein extract, at 25°C and pH 6 for 10 min Hordeum vulgare
0.00076
-
FaCPI-1 inhibitor concentrations between 25 and 500 nM used, incubation with 5 microgram of a soluble root protein extract, at 25°C and pH 6 for 10 min Hordeum vulgare

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
additional information
-
inhibitory doses for 50% proteinase activity inhibition higher for root legumain activity than for endosperm one Hordeum vulgare additional information
0.018
-
endosperm Hordeum vulgare HvCPI-4-deltaT143-Cterm
0.02
-
endosperm Hordeum vulgare FaCPI-1
0.022
-
endosperm Hordeum vulgare HvCPI-4-deltaT151-Cterm
0.033
-
endosperm Hordeum vulgare HvCPI-4-Q86P
0.038
-
endosperm Hordeum vulgare HvCPI-4
0.068
-
root extract Hordeum vulgare HvCPI-4-deltaT143-Cterm
0.091
-
root extract Hordeum vulgare HvCPI-4-deltaT151-Cterm
0.11
-
root extract Hordeum vulgare HvCPI-4-Q86P
0.12
-
root extract Hordeum vulgare HvCPI-4
0.2
-
root extract Hordeum vulgare FaCPI-1