Information on EC 3.4.22.51 - cruzipain

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The enzyme appears in viruses and cellular organisms

EC NUMBER
COMMENTARY hide
3.4.22.51
-
RECOMMENDED NAME
GeneOntology No.
cruzipain
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REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
broad endopeptidase specificity similar to that of cathepsin L
show the reaction diagram
-
-
-
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REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
hydrolysis
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-
hydrolysis of amide bond
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hydrolysis of peptide bond
CAS REGISTRY NUMBER
COMMENTARY hide
102227-51-0
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141588-22-9
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84399-99-5
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90371-53-2
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ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
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-
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Manually annotated by BRENDA team
strain RA
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-
Manually annotated by BRENDA team
strain Y
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-
Manually annotated by BRENDA team
strain Y486
UniProt
Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
evolution
-
the O-GlcNAc moieties constitute a common epitope between cruzipain and either myosin or other cardiac O-GlcNAc-containing proteins
malfunction
-
cruzain-deficient Trypanosoma cruzi rapidly activates host macrophages via NF-kB P65 and is unable to survive intracellularly within macrophages. No significant IL-12 expression occurs in macrophages infected with wild-type Trypanosoma cruzi and treated with lipopolysacchrides and brefeldin A, confirming impairment of macrophage activation pathways
physiological function
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
(7-[[(2S)-2-(4-[(1S)-1,2-dimethyl-1-[(morpholin-4-ylcarbonyl)amino]propyl]-1H-1,2,3-triazol-1-yl)hexanoyl]amino]-4-methyl-2-oxo-3,4-dihydro-2H-chromen-3-yl)acetic acid + H2O
(2S)-2-(4-[(1S)-1,2-dimethyl-1-[(morpholin-4-ylcarbonyl)amino]propyl]-1H-1,2,3-triazol-1-yl)hexanoic acid + 7-amino-4-methylcoumarin-3-acetic acid
show the reaction diagram
-
-
-
ir
(7-[[(2S)-2-(4-[(1S)-1,2-dimethyl-1-[(naphthalen-2-ylcarbonyl)amino]propyl]-1H-1,2,3-triazol-1-yl)hexanoyl]amino]-4-methyl-2-oxo-3,4-dihydro-2H-chromen-3-yl)acetic acid + H2O
(2S)-2-(4-[(1S)-1,2-dimethyl-1-[(naphthalen-2-ylcarbonyl)amino]propyl]-1H-1,2,3-triazol-1-yl)hexanoic acid + 7-amino-4-methylcoumarin-3-acetic acid
show the reaction diagram
-
-
-
ir
(7-[[(2S)-2-(4-[(1S)-1,2-dimethyl-1-[(phenylcarbonyl)amino]propyl]-1H-1,2,3-triazol-1-yl)hexanoyl]amino]-4-methyl-2-oxo-3,4-dihydro-2H-chromen-3-yl)acetic acid + H2O
(2S)-2-(4-[(1S)-1,2-dimethyl-1-[(phenylcarbonyl)amino]propyl]-1H-1,2,3-triazol-1-yl)hexanoic acid + 7-amino-4-methylcoumarin-3-acetic acid
show the reaction diagram
-
-
-
ir
(7-[[(2S)-2-(4-[(1S)-1,2-dimethyl-1-[(quinolin-6-ylcarbonyl)amino]propyl]-1H-1,2,3-triazol-1-yl)hexanoyl]amino]-4-methyl-2-oxo-3,4-dihydro-2H-chromen-3-yl)acetic acid + H2O
(2S)-2-(4-[(1S)-1,2-dimethyl-1-[(quinolin-6-ylcarbonyl)amino]propyl]-1H-1,2,3-triazol-1-yl)hexanoic acid + 7-amino-4-methylcoumarin-3-acetic acid
show the reaction diagram
-
-
-
ir
(7-[[(2S)-2-(4-[(1S)-1,2-dimethyl-1-[(quinolin-6-ylmethyl)amino]propyl]-1H-1,2,3-triazol-1-yl)hexanoyl]amino]-4-methyl-2-oxo-3,4-dihydro-2H-chromen-3-yl)acetic acid + H2O
(2S)-2-(4-[(1S)-1,2-dimethyl-1-[(quinolin-6-ylmethyl)amino]propyl]-1H-1,2,3-triazol-1-yl)hexanoic acid + 7-amino-4-methylcoumarin-3-acetic acid
show the reaction diagram
-
-
-
ir
(7-[[(2S)-2-(4-[(1S)-1-[(1,3-benzothiazol-6-ylcarbonyl)amino]-1,2-dimethylpropyl]-1H-1,2,3-triazol-1-yl)hexanoyl]amino]-4-methyl-2-oxo-3,4-dihydro-2H-chromen-3-yl)acetic acid + H2O
(2S)-2-(4-[(1S)-1-[(1,3-benzothiazol-6-ylcarbonyl)amino]-1,2-dimethylpropyl]-1H-1,2,3-triazol-1-yl)hexanoic acid + 7-amino-4-methylcoumarin-3-acetic acid
show the reaction diagram
-
-
-
ir
(7-[[(2S)-2-(4-[(1S)-1-[(1,3-benzothiazol-6-ylmethyl)amino]-1,2-dimethylpropyl]-1H-1,2,3-triazol-1-yl)hexanoyl]amino]-4-methyl-2-oxo-3,4-dihydro-2H-chromen-3-yl)acetic acid + H2O
(2S)-2-(4-[(1S)-1-[(1,3-benzothiazol-6-ylmethyl)amino]-1,2-dimethylpropyl]-1H-1,2,3-triazol-1-yl)hexanoic acid + 7-amino-4-methylcoumarin-3-acetic acid
show the reaction diagram
-
-
-
ir
(7-[[(2S)-2-(4-[(1S)-1-[(1-benzofuran-6-ylcarbonyl)amino]-1,2-dimethylpropyl]-1H-1,2,3-triazol-1-yl)hexanoyl]amino]-4-methyl-2-oxo-3,4-dihydro-2H-chromen-3-yl)acetic acid + H2O
(2S)-2-(4-[(1S)-1-[(1-benzofuran-6-ylcarbonyl)amino]-1,2-dimethylpropyl]-1H-1,2,3-triazol-1-yl)hexanoic acid + 7-amino-4-methylcoumarin-3-acetic acid
show the reaction diagram
-
-
-
ir
(7-[[(2S)-2-(4-[(1S)-1-[(1-benzothiophen-6-ylcarbonyl)amino]-1,2-dimethylpropyl]-1H-1,2,3-triazol-1-yl)hexanoyl]amino]-4-methyl-2-oxo-3,4-dihydro-2H-chromen-3-yl)acetic acid + H2O
(2S)-2-(4-[(1S)-1-[(1-benzothiophen-6-ylcarbonyl)amino]-1,2-dimethylpropyl]-1H-1,2,3-triazol-1-yl)hexanoic acid + 7-amino-4-methylcoumarin-3-acetic acid
show the reaction diagram
-
-
-
ir
(7-[[(2S)-2-(4-[(1S)-1-[(1H-benzotriazol-5-ylcarbonyl)amino]-1,2-dimethylpropyl]-1H-1,2,3-triazol-1-yl)hexanoyl]amino]-4-methyl-2-oxo-3,4-dihydro-2H-chromen-3-yl)acetic acid + H2O
(2S)-2-(4-[(1S)-1-[(1H-benzotriazol-5-ylcarbonyl)amino]-1,2-dimethylpropyl]-1H-1,2,3-triazol-1-yl)hexanoic acid + 7-amino-4-methylcoumarin-3-acetic acid
show the reaction diagram
-
-
-
ir
(7-[[(2S)-2-(4-[(1S)-1-[(1H-indol-5-ylcarbonyl)amino]-1,2-dimethylpropyl]-1H-1,2,3-triazol-1-yl)hexanoyl]amino]-4-methyl-2-oxo-3,4-dihydro-2H-chromen-3-yl)acetic acid + H2O
(2S)-2-(4-[(1S)-1-[(1H-indol-5-ylcarbonyl)amino]-1,2-dimethylpropyl]-1H-1,2,3-triazol-1-yl)hexanoic acid + 7-amino-4-methylcoumarin-3-acetic acid
show the reaction diagram
-
-
-
ir
(7-[[(2S)-2-(4-[(1S)-1-[(1H-indol-6-ylcarbonyl)amino]-1,2-dimethylpropyl]-1H-1,2,3-triazol-1-yl)hexanoyl]amino]-4-methyl-2-oxo-3,4-dihydro-2H-chromen-3-yl)acetic acid + H2O
(2S)-2-(4-[(1S)-1-[(1H-indol-6-ylcarbonyl)amino]-1,2-dimethylpropyl]-1H-1,2,3-triazol-1-yl)hexanoic acid + 7-amino-4-methylcoumarin-3-acetic acid
show the reaction diagram
-
-
-
ir
(7-[[(2S)-2-(4-[(1S)-1-[(4-methoxybenzyl)amino]-1,2-dimethylpropyl]-1H-1,2,3-triazol-1-yl)hexanoyl]amino]-4-methyl-2-oxo-3,4-dihydro-2H-chromen-3-yl)acetic acid + H2O
(2S)-2-(4-[(1S)-1-[(4-methoxybenzyl)amino]-1,2-dimethylpropyl]-1H-1,2,3-triazol-1-yl)hexanoic acid + 7-amino-4-methylcoumarin-3-acetic acid
show the reaction diagram
-
-
-
ir
(7-[[(2S)-2-[4-[(1S)-1,2-dimethyl-1-[[(1-methyl-1H-indol-6-yl)carbonyl]amino]propyl]-1H-1,2,3-triazol-1-yl]hexanoyl]amino]-4-methyl-2-oxo-3,4-dihydro-2H-chromen-3-yl)acetic acid + H2O
(2S)-2-[4-[(1S)-1,2-dimethyl-1-[[(1-methyl-1H-indol-6-yl)carbonyl]amino]propyl]-1H-1,2,3-triazol-1-yl]hexanoic acid + 7-amino-4-methylcoumarin-3-acetic acid
show the reaction diagram
-
-
-
ir
(7-[[(2S)-2-[4-[(1S)-1,2-dimethyl-1-[[(2-methylphenyl)carbonyl]amino]propyl]-1H-1,2,3-triazol-1-yl]hexanoyl]amino]-4-methyl-2-oxo-3,4-dihydro-2H-chromen-3-yl)acetic acid + H2O
(2S)-2-[4-[(1S)-1,2-dimethyl-1-[[(2-methylphenyl)carbonyl]amino]propyl]-1H-1,2,3-triazol-1-yl]hexanoic acid + 7-amino-4-methylcoumarin-3-acetic acid
show the reaction diagram
-
-
-
ir
(7-[[(2S)-2-[4-[(1S)-1,2-dimethyl-1-[[(3-methylphenyl)carbonyl]amino]propyl]-1H-1,2,3-triazol-1-yl]hexanoyl]amino]-4-methyl-2-oxo-3,4-dihydro-2H-chromen-3-yl)acetic acid + H2O
(2S)-2-[4-[(1S)-1,2-dimethyl-1-[[(3-methylphenyl)carbonyl]amino]propyl]-1H-1,2,3-triazol-1-yl]hexanoic acid + 7-amino-4-methylcoumarin-3-acetic acid
show the reaction diagram
-
-
-
ir
(7-[[(2S)-2-[4-[(1S)-1,2-dimethyl-1-[[(4-methylphenyl)carbonyl]amino]propyl]-1H-1,2,3-triazol-1-yl]hexanoyl]amino]-4-methyl-2-oxo-3,4-dihydro-2H-chromen-3-yl)acetic acid + H2O
(2S)-2-[4-[(1S)-1,2-dimethyl-1-[[(4-methylphenyl)carbonyl]amino]propyl]-1H-1,2,3-triazol-1-yl]hexanoic acid + 7-amino-4-methylcoumarin-3-acetic acid
show the reaction diagram
-
-
-
ir
(7-[[(2S)-2-[4-[(1S)-1-(benzylamino)-1,2-dimethylpropyl]-1H-1,2,3-triazol-1-yl]hexanoyl]amino]-4-methyl-2-oxo-3,4-dihydro-2H-chromen-3-yl)acetic acid + H2O
(2S)-2-[4-[(1S)-1-(benzylamino)-1,2-dimethylpropyl]-1H-1,2,3-triazol-1-yl]hexanoic acid + 7-amino-4-methylcoumarin-3-acetic acid
show the reaction diagram
-
-
-
ir
(7-[[(2S)-2-[4-[(1S)-1-[[(2-methoxyphenyl)carbonyl]amino]-1,2-dimethylpropyl]-1H-1,2,3-triazol-1-yl]hexanoyl]amino]-4-methyl-2-oxo-3,4-dihydro-2H-chromen-3-yl)acetic acid + H2O
(2S)-2-[4-[(1S)-1-[[(2-methoxyphenyl)carbonyl]amino]-1,2-dimethylpropyl]-1H-1,2,3-triazol-1-yl]hexanoic acid + 7-amino-4-methylcoumarin-3-acetic acid
show the reaction diagram
-
-
-
ir
(7-[[(2S)-2-[4-[(1S)-1-[[(3-methoxyphenyl)carbonyl]amino]-1,2-dimethylpropyl]-1H-1,2,3-triazol-1-yl]hexanoyl]amino]-4-methyl-2-oxo-3,4-dihydro-2H-chromen-3-yl)acetic acid + H2O
(2S)-2-[4-[(1S)-1-[[(3-methoxyphenyl)carbonyl]amino]-1,2-dimethylpropyl]-1H-1,2,3-triazol-1-yl]hexanoic acid + 7-amino-4-methylcoumarin-3-acetic acid
show the reaction diagram
-
-
-
ir
(7-[[(2S)-2-[4-[(1S)-1-[[(4-methoxyphenyl)carbonyl]amino]-1,2-dimethylpropyl]-1H-1,2,3-triazol-1-yl]hexanoyl]amino]-4-methyl-2-oxo-3,4-dihydro-2H-chromen-3-yl)acetic acid + H2O
(2S)-2-[4-[(1S)-1-[[(4-methoxyphenyl)carbonyl]amino]-1,2-dimethylpropyl]-1H-1,2,3-triazol-1-yl]hexanoic acid + 7-amino-4-methylcoumarin-3-acetic acid
show the reaction diagram
-
-
-
ir
2-aminobenzoic acid-ALRFSKQ-N-(2,4-dinitrophenyl)ethylenediamine + H2O
?
show the reaction diagram
-
-
-
-
?
2-aminobenzoic acid-KLGFSKQ-N-(2,4-dinitrophenyl)ethylenediamine + H2O
?
show the reaction diagram
-
-
-
-
?
2-aminobenzoic acid-KLRFSKQ-N-(2,4-dinitrophenyl)ethylenediamine + H2O
?
show the reaction diagram
-
and analogues
-
-
?
2-aminobenzoic acid-peptidyl-N-(2,4-dinitrophenyl)ethylenediamine + H2O
?
show the reaction diagram
-
and derivatives, enzyme shows preference for benzyl-Cys or Arg at the P1 position and a hydrophobic non-aromatic residue at position P2
-
-
?
2-aminobenzoyl-ARF-(2,4-dinitrophenyl)-epsilon-NH2-lysine-OH + H2O
?
show the reaction diagram
-
-
-
-
?
2-aminobenzoyl-FRA-(2,4-dinitrophenyl)-epsilon-NH2-lysine-NH2 + H2O
?
show the reaction diagram
-
-
-
-
?
2-aminobenzoyl-FRA-(2,4-dinitrophenyl)-epsilon-NH2-lysine-OH + H2O
?
show the reaction diagram
-
-
-
-
?
2-aminobenzoyl-FRF-(2,4-dinitrophenyl)-epsilon-NH2-lysine-OH + H2O
?
show the reaction diagram
-
-
-
-
?
2-aminobenzoyl-LGMISLMKRPQ-N-(2,4-dinitrophenyl)ethylenediamine + H2O
?
show the reaction diagram
2-aminobenzoyl-Phe-Arg-(2,4-dinitrophenyl)-epsilon-NH2-lysine-Pro-OH + H2O
?
show the reaction diagram
-
-
-
-
?
2-aminobenzoyl-Phe-Arg-(2,4-dinitrophenyl)-epsilon-NH2-lysine-Trp-OH + H2O
?
show the reaction diagram
-
-
-
-
?
2-aminobenzoyl-RRF-(2,4-dinitrophenyl)-epsilon-NH2-lysine-OH + H2O
?
show the reaction diagram
-
-
-
-
?
Ac-Phe-Arg-7-amido-4-methylcoumarin + H2O
Ac-Phe-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
10 microM, 4 nanoM cruzain, 45 min, room temperature, pH 5.5
-
-
?
azocasein + H2O
?
show the reaction diagram
-
-
-
-
?
benzoyl-FR-4-methylcoumarin 7-amide + H2O
?
show the reaction diagram
benzoyl-HR-4-methylcoumarin 7-amide + H2O
?
show the reaction diagram
-
less susceptible substrate
-
-
?
benzoyl-PFR-4-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
benzoyl-Phe-Arg-4-methylcoumarin-7-amide + H2O
?
show the reaction diagram
-
fluorogenic substrates based on the peptide benzoyl-Phe-Arg-4-methylcoumarin-7-amide
-
-
?
benzoyl-Phe-Val-Arg-p-nitroanilide + H2O
?
show the reaction diagram
-
as active as with benzyloxycarbonyl-Arg-Arg-methoxy-beta-naphthylamide
-
-
?
benzoyl-Pro-Phe-Arg-p-nitroanilide + H2O
?
show the reaction diagram
-
41% of the activity with benzyloxycarbonyl-Arg-Arg-methoxy-beta-naphthylamide
-
-
?
benzoyl-RR-4-methylcoumarin 7-amide + H2O
?
show the reaction diagram
-
less susceptible substrate
-
-
?
benzoyl-Val-Gly-Arg-p-nitroanilide + H2O
?
show the reaction diagram
-
52% of the activity with benzyloxycarbonyl-Arg-Arg-methoxy-beta-naphthylamide
-
-
?
benzoyl-YR-4-methylcoumarin 7-amide + H2O
?
show the reaction diagram
-
-
-
-
?
benzyloxycarbonyl-Ala-Arg-Arg-methoxy-beta-naphthylamide + H2O
?
show the reaction diagram
-
36% of the activity with benzyloxycarbonyl-Arg-Arg-methoxy-beta-naphthylamide
-
-
?
benzyloxycarbonyl-Arg-Arg-methoxy-beta-naphthylamide + H2O
?
show the reaction diagram
-
-
-
-
?
benzyloxycarbonyl-Gly-Pro-Arg-p-nitroanilide + H2O
?
show the reaction diagram
-
66% of the activity with benzyloxycarbonyl-Arg-Arg-methoxy-beta-naphthylamide
-
-
?
benzyloxycarbonyl-L-Phe-L-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-L-Phe-L-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
relatively low rates of substrate hydrolysis
-
-
?
benzyloxycarbonyl-Phe-Arg-4-methylcoumarin 7-amide + H2O
?
show the reaction diagram
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Phe-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
benzyloxycarbonyl-Phe-Arg-methoxy-beta-naphthylamide + H2O
?
show the reaction diagram
-
30% of the activity with benzyloxycarbonyl-Arg-Arg-methoxy-beta-naphthylamide
-
-
?
Bovine serum albumin + H2O
?
show the reaction diagram
-
-
-
-
?
Bz-Phe-Arg-4-methylcoumaryl-7-amide + H2O
Bz-Phe-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
Bz-Pro-Phe-Arg-4-nitroanilide + H2O
Bz-Pro-Phe-Arg + 4-nitroaniline
show the reaction diagram
-
-
-
-
?
casein + H2O
?
show the reaction diagram
-
-
-
-
?
epsilon-NH2(capryl)-L-(SBzl)C-7-amido-4-methylcoumarin + H2O
?
show the reaction diagram
-
-
-
-
?
Gelatin + H2O
?
show the reaction diagram
Hemoglobin + H2O
?
show the reaction diagram
human IgG + H2O
?
show the reaction diagram
-
specific cleavage sites on human IgG subclasses by cruzipain
-
-
?
human NF-kappaB P65 + H2O
?
show the reaction diagram
-
-
-
-
?
Immunoglobulin G1 + H2O
?
show the reaction diagram
Immunoglobulin G3 + H2O
?
show the reaction diagram
insulin A + H2O
?
show the reaction diagram
-
-
-
-
?
insulin B + H2O
?
show the reaction diagram
-
-
-
-
?
KEEASSAVVGGPG + H2O
?
show the reaction diagram
-
-
-
-
?
KEEASSAVVRGPG + H2O
?
show the reaction diagram
-
-
-
-
?
Lys-Arg-primaquine + H2O
Lys-Arg + primaquine
show the reaction diagram
-
-
-
-
?
N-alpha-benzyloxy-carbonyl-L-phenylalanyl-L-alanine-(7-amido-4-methylcoumarin) + H2O
N-alpha-benzyloxy-carbonyl-L-phenylalanyl-L-alanine + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
N-alpha-benzyloxycarbonyl-L-arginyl-L-alanine-(7-amido-4-methylcoumarin) + H2O
N-alpha-benzyloxycarbonyl-L-arginyl-L-alanine + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
N-alpha-benzyloxycarbonyl-L-tyrosyl-L-alanine-(7-amido-4-methylcoumarin) + H2O
N-alpha-benzyloxycarbonyl-L-tyrosyl-L-alanine + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
N-carbobenzoxy-Arg-Arg-2-(4-methoxy)-naphthylamide + H2O
N-carbobenzoxy-Arg-Arg + 2-amino-4-methoxynaphthalene
show the reaction diagram
-
-
-
-
?
N-carbobenzoxy-Val-Val-Arg-4-nitroanilide + H2O
?
show the reaction diagram
N-tert-butoxycarbonyl-O-benzyl-Ser-Gly-Arg-p-nitroanilide + H2O
?
show the reaction diagram
-
39% of the activity with benzyloxycarbonyl-Arg-Arg-methoxy-beta-naphthylamide
-
-
?
N-tert-butoxycarbonyl-Val-Leu-Gly-Arg-p-nitroanilide + H2O
?
show the reaction diagram
-
24% of the activity with benzyloxycarbonyl-Arg-Arg-methoxy-beta-naphthylamide
-
-
?
o-aminobenzoyl-ALRFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine + H2O
?
show the reaction diagram
-
-
-
-
?
o-aminobenzoyl-HLRFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine + H2O
?
show the reaction diagram
-
-
-
-
?
o-aminobenzoyl-KARFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine + H2O
?
show the reaction diagram
-
-
-
-
?
o-aminobenzoyl-KFRFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine + H2O
?
show the reaction diagram
-
-
-
-
?
o-aminobenzoyl-KLFFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine + H2O
o-aminobenzoyl-KLF + FSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
show the reaction diagram
-
-
-
-
?
o-aminobenzoyl-KLGFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine + H2O
o-aminobenzoyl-KLG + FSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
show the reaction diagram
-
-
-
-
?
o-aminobenzoyl-KLKFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine + H2O
o-aminobenzoyl-KLK + FSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
show the reaction diagram
-
-
-
-
?
o-aminobenzoyl-KLRFAKQ-N-(2,4-dinitrophenyl)-ethylenediamine + H2O
o-aminobenzoyl-KLR + FAKQ-N-(2,4-dinitrophenyl)-ethylenediamine
show the reaction diagram
-
-
-
-
?
o-aminobenzoyl-KLRFFKQ-N-(2,4-dinitrophenyl)-ethylenediamine + H2O
o-aminobenzoyl-KLR + FFKQ-N-(2,4-dinitrophenyl)-ethylenediamine
show the reaction diagram
-
-
-
-
?
o-aminobenzoyl-KLRFPKQ-N-(2,4-dinitrophenyl)-ethylenediamine + H2O
o-aminobenzoyl-KLR + FPKQ-N-(2,4-dinitrophenyl)-ethylenediamine
show the reaction diagram
-
-
-
-
?
o-aminobenzoyl-KLRFSFQ-N-(2,4-dinitrophenyl)-ethylenediamine + H2O
o-aminobenzoyl-KLR + FSFQ-N-(2,4-dinitrophenyl)-ethylenediamine
show the reaction diagram
-
no hydrolysis is detected
-
-
?
o-aminobenzoyl-KLRFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine + H2O
o-aminobenzoyl-KLR + FSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
show the reaction diagram
-
-
-
-
?
o-aminobenzoyl-KLRFSPQ-N-(2,4-dinitrophenyl)-ethylenediamine + H2O
o-aminobenzoyl-KLR + FSPQ-N-(2,4-dinitrophenyl)-ethylenediamine
show the reaction diagram
-
-
-
-
?
o-aminobenzoyl-KLRFSRQ-N-(2,4-dinitrophenyl)-ethylenediamine + H2O
o-aminobenzoyl-KLR + FSRQ-N-(2,4-dinitrophenyl)-ethylenediamine
show the reaction diagram
-
-
-
-
?
o-aminobenzoyl-KLRLSKQ-N-(2,4-dinitrophenyl)-ethylenediamine + H2O
o-aminobenzoyl-KLR + LSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
show the reaction diagram
-
-
-
-
?
o-aminobenzoyl-KLRRSKQ-N-(2,4-dinitrophenyl)-ethylenediamine + H2O
o-aminobenzoyl-KLR + RSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
show the reaction diagram
-
-
-
-
?
o-aminobenzoyl-KPRFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine + H2O
?
show the reaction diagram
-
-
-
-
?
o-aminobenzoyl-KRRFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine + H2O
?
show the reaction diagram
-
-
-
-
?
o-aminobenzoyl-LLRFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine + H2O
?
show the reaction diagram
-
-
-
-
?
peptidyl-4-nitroanilide + H2O
?
show the reaction diagram
peptidyl-beta-naphthylamide + H2O
?
show the reaction diagram
peptidyl-methylcoumarin amide + H2O
?
show the reaction diagram
-
and derivatives, enzyme shows preference for benzyl-Cys or Arg at the P1 position and a hydrophobic non-aromatic residue at position P2
-
-
?
Phe-Ala-primaquine + H2O
Phe-Ala + primaquine
show the reaction diagram
-
-
-
-
?
Phe-Arg-AMC
?
show the reaction diagram
-
-
-
-
?
Phe-Arg-primaquine + H2O
Phe-Arg + primaquine
show the reaction diagram
-
-
-
-
?
tosyl-Gly-Pro-Arg-p-nitroanilide + H2O
?
show the reaction diagram
-
25% of the activity with benzyloxycarbonyl-Arg-Arg-methoxy-beta-naphthylamide
-
-
?
Z-Phe-Arg-7-amido-4-methylcoumarin + H2O
?
show the reaction diagram
Z-Phe-Arg-7-amido-4-methylcoumarin + H2O
Z-Phe-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
additional information
?
-
NATURAL SUBSTRATES
NATURAL PRODUCTS
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
casein + H2O
?
show the reaction diagram
-
-
-
-
-
Gelatin + H2O
?
show the reaction diagram
D0QZL7, D0QZL8, D0QZM0, D0QZM2, D0QZM5, D0QZM6, D0QZM9
-
-
-
?
Hemoglobin + H2O
?
show the reaction diagram
human NF-kappaB P65 + H2O
?
show the reaction diagram
-
-
-
-
?
Immunoglobulin G1 + H2O
?
show the reaction diagram
-
-
-
-
-
Immunoglobulin G3 + H2O
?
show the reaction diagram
-
-
-
-
-
Lys-Arg-primaquine + H2O
Lys-Arg + primaquine
show the reaction diagram
-
-
-
-
?
Phe-Ala-primaquine + H2O
Phe-Ala + primaquine
show the reaction diagram
-
-
-
-
?
Phe-Arg-primaquine + H2O
Phe-Arg + primaquine
show the reaction diagram
-
-
-
-
?
additional information
?
-
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
NaCl
-
Km increases up to 400 mM, then decreases and remains constant at 50-60% up to 1 M, kcat maximum at 300 mM
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(1E)-1-(3,4-dichlorophenyl)-2-phenylethan-1-one thiosemicarbazone
-
IC50: 80 nM
(1E)-1-(3,4-dichlorophenyl)-3-phenylpropan-1-one thiosemicarbazone
-
IC50: 40 nM
(1E)-1-(3,4-dichlorophenyl)pentan-1-one thiosemicarbazone
-
IC50: 19 nM
(1E)-1-(3,4-dichlorophenyl)propan-1-one thiosemicarbazone
-
IC50: 30 nM
(1E)-1-(3-bromophenyl)propan-1-one thiosemicarbazone
-
IC50: 310 nM
(1E,2E)-1-(3,4-dichlorophenyl)-3-phenylprop-2-en-1-one thiosemicarbazone
-
IC50: 30 nM
(1Z)-1-(3,4-dichlorophenyl)-2-phenoxyethan-1-one thiosemicarbazone
-
IC50: 30 nM
(2(1H)-pyridinethionato-kappaS2)[2,6-bis[(mercapto-KappaS)methyl]pyridine-kappaN1] oxorhenium(V)
-
-
(2E)-1,3-bis(2,4,5-trimethoxyphenyl)prop-2-en-1-one
-
-
(2E)-1,3-di(naphthalen-2-yl)prop-2-en-1-one
-
-
(2E)-1-(1,3-benzodioxol-5-yl)-3-(1-naphthyl)-2-propen-1-one
-
-
(2E)-1-(1,3-benzodioxol-5-yl)-3-(2,6-dichlorophenyl)-2-propen-1-one
-
-
(2E)-1-(1,3-benzodioxol-5-yl)-3-(2-chlorophenyl)-2-propen-1-one
-
-
(2E)-1-(1,3-benzodioxol-5-yl)-3-(3-methoxy-4-phenoxyphenyl)prop-2-en-1-one
-
-
(2E)-1-(1,3-benzodioxol-5-yl)-3-(4-buthoxyphenyl)-2-propen-1-one
-
-
(2E)-1-(1,3-benzodioxol-5-yl)-3-(5-methylfuran-2-yl)-2-propen-1-one
-
-
(2E)-1-(1,3-benzodioxol-5-yl)-3-(thiophen-2-yl)-2-propen-1-one
-
-
(2E)-1-(2',4',5'-trimethoxyphenyl)-3-(1-naphthyl)-2-propen-1-one
-
-
(2E)-1-(2',4',5'-trimethoxyphenyl)-3-(thiophen-2-yl)-2-propen-1-one
-
-
(2E)-1-(2'-hydroxy,3'-bromo,4',6'-dimethoxyphenyl)-3-(1-naphthyl)-2-propen-1-one
-
-
(2E)-1-(2'-hydroxy-3'-bromo-4',6'-dimethoxyphenyl)-3-(4-buthoxyphenyl)-2-propen-1- one
-
-
(2E)-1-(2,4-dimethoxyphenyl)-3-(2,4,5-trimethoxyphenyl)prop-2-en-1-one
-
-
(2E)-1-(2-naphthyl)-3-(2,6-dimethoxyphenyl)-2-propen-1-one
-
-
(2E)-1-(2-naphthyl)-3-(5-methylfuran-2-yl)-2-propen-1-one
-
-
(2E)-1-(3-bromo-2-hydroxy-4,6-dimethoxyphenyl)-3-(3-nitrophenyl)prop-2-en-1-one
-
-
(2E)-1-(3-bromo-2-hydroxy-4,6-dimethoxyphenyl)-3-(4-methoxyphenyl)prop-2-en-1-one
-
-
(2E)-1-(3a,7a-dihydro-1,3-benzodioxol-5-yl)-3-(3,4,5-trimethoxyphenyl)prop-2-en-1-one
-
-
(2E)-1-(3a,7a-dihydro-1,3-benzodioxol-5-yl)-3-(3-methoxyphenyl)prop-2-en-1-one
-
-
(2E)-1-(3a,7a-dihydro-1,3-benzodioxol-5-yl)-3-(4-methoxyphenyl)prop-2-en-1-one
-
-
(2E)-1-(3a,7a-dihydro-1,3-benzodioxol-5-yl)-3-(4-methylphenyl)prop-2-en-1-one
-
-
(2E)-1-(3a,7a-dihydro-1,3-benzodioxol-5-yl)-3-phenylprop-2-en-1-one
-
-
(2E)-1-(4-hydroxy-1,3-benzodioxol-5-yl)-3-(2,4,5-trimethoxyphenyl)prop-2-en-1-one
-
-
(2E)-2-{4-[(3-oxido-2,1,3-benzoxadiazol-5-yl)methoxy]benzylidene}hydrazinecarboximidamide
-
-
(2E)-3-(1,3-benzodioxol-5-yl)-1-(2-hydroxyphenyl)prop-2-en-1-one
-
-
(2E)-3-(1,3-benzodioxol-5-yl)-1-(4-bromophenyl)prop-2-en-1-one
-
-
(2E)-3-(1,3-benzodioxol-5-yl)-1-(naphthalen-2-yl)prop-2-en-1-one
-
-
(2E)-3-(3-methoxyphenyl)-1-(2,4,5-trimethoxyphenyl)prop-2-en-1-one
-
-
(2E)-3-(4-bromophenyl)-1-(3a,7a-dihydro-1,3-benzodioxol-5-yl)prop-2-en-1-one
-
-
(2E)-3-(4-fluorophenyl)-1-(naphthalen-2-yl)prop-2-en-1-one
-
-
(2E)-3-(4-methoxyphenyl)-1-(naphthalen-2-yl)prop-2-en-1-one
-
-
(2E)-3-[4-(benzyloxy)-3-methoxyphenyl]-1-(2,4-dimethoxyphenyl)prop-2-en-1-one
-
-
(2E)-N'-(3'-bromo-4'-hydroxy-5'-methoxybenzilidene)-3,4,5-trimethoxybenzohydrazide
-
-
(2E)-N'-(4'-buthoxybenzilidene)-3,4,5-trimethoxybenzohydrazide
-
-
(2E)-N'-(4'-hydroxy-5'-methoxybenzilidene)-3,4,5-trimethoxybenzohydrazide
-
-
(2S)-2-(1-[1-[(Z)-1-chloro-2-(phenylsulfonyl)ethenyl]pentyl]-1H-1,2,3-triazol-4-yl)-3-methyl-N-(quinolin-6-ylmethyl)butan-2-amine
10 microM
(2S)-3-methyl-2-(1-[1-[(E)-2-(phenylsulfonyl)ethenyl]pentyl]-1H-1,2,3-triazol-4-yl)-N-(quinolin-6-ylmethyl)butan-2-amine
10 microM
(3-oxido-2,1,3-benzoxadiazol-5-yl)methyl (2E)-2-(4-hydroxybenzylidene)hydrazinecarbimidothioate
-
-
(3S,5R,10R)-N-benzyl-3-(2-methylpropyl)-2-oxo-10-[(E)-2-(phenylsulfonyl)ethenyl]-1,4-diazecane-5-carboxamide
(3S,5R,11R)-N-benzyl-3-(2-methylpropyl)-2-oxo-11-[(E)-2-(phenylsulfonyl)ethenyl]-1,4-diazacycloundecane-5-carboxamide
(3Z)-1H-indole-2,3-dione 3-thiosemicarbazone
-
IC50: 0.008 mM
(3Z)-5,7-dimethyl-1H-indole-2,3-dione 3-thiosemicarbazone
-
IC50: 0.016 mM
(3Z)-5-bromo-1H-indole-2,3-dione 3-thiosemicarbazone
-
IC50: 0.02 mM
(3Z)-5-chloro-1H-indole-2,3-dione 3-thiosemicarbazone
-
IC50: 0.021 mM
(3Z)-5-chloro-7-methyl-1H-indole-2,3-dione 3-thiosemicarbazone
-
IC50: 0.0105 mM
(3Z)-5-iodo-1H-indole-2,3-dione 3-thiosemicarbazone
-
IC50: 0.009 mM
(3Z)-5-methyl-1H-indole-2,3-dione 3-thiosemicarbazone
-
IC50: 0.02-0.05 mM
(3Z)-5-nitro-1H-indole-2,3-dione 3-thiosemicarbazone
-
IC50: 0.03 mM
(E)-(3,4-dichlorophenyl)(2-phenylcyclopropyl)methanone thiosemicarbazone
-
IC50: 30 nM
(E)-(3,4-dichlorophenyl)(4-methylphenyl)methanone thiosemicarbazone
-
IC50: 40 nM
(E)-cyclohexyl(3,4-dichlorophenyl)methanone thiosemicarbazone
-
IC50: 3000 nM
(E/Z)-N'-(2-chlorobenzylidene)-3-phenylquinoxaline-2-hydrazide
-
25 microM, inhibition of parasite growth
(E/Z)-N'-(2-hhenylidene)-3-phenylquinoxaline-2-hydrazide
-
25 microM, inhibition of parasite growth
(E/Z)-N'-(2-hydroxybenzylidene)-3-methylquinoxaline-2-hydrazide
-
25 microM
(E/Z)-N'-(2-hydroxybenzylidene)-3-phenylquinoxaline-2-hydrazide
-
25 microM
(E/Z)-N'-(3-chlorobenzylidene)-3-phenylquinoxaline-2-hydrazide
-
25 microM, inhibition of parasite growth
(E/Z)-N'-(4-bromobenzylidene)-3-phenylquinoxaline-2-hydrazide
-
25 microM, inhibition of parasite growth
(E/Z)-N'-(4-chlorobenzylidene)-3-phenylquinoxaline-2-hydrazide
-
25 microM, inhibition of parasite growth
(E/Z)-N'-(4-dimethylaminobenzylidene)-3-phenylquinoxaline-2-hydrazide
-
25 microM, inhibition of parasite growth
(E/Z)-N'-(4-fluorobenzylidene)-3-phenylquinoxaline-2-hydrazide
-
25 microM, inhibition of parasite growth
(E/Z)-N'-(4-hydroxybenzylidene)-3-phenylquinoxaline-2-hydrazide
-
25 microM, inhibition of parasite growth
(E/Z)-N'-(4-isopropylbenzylidene)-3-phenylquinoxaline-2-hydrazide
-
25 microM, inhibition of parasite growth
(E/Z)-N'-(4-nitrobenzylidene)-3-phenylquinoxaline-2-hydrazide
-
25 microM, inhibition of parasite growth
(E/Z)-N'-(furfurylidene)-3-phenylquinoxaline-2-hydrazide
-
25 microM, inhibition of parasite growth
(E/Z)-N'-(pyridin-2-ylmethylene)-3-phenylquinoxaline-2-hydrazide
-
25 microM, inhibition of parasite growth
(E/Z)-N'-(pyridin-4-ylmethylene)-3-phenylquinoxaline-2-hydrazide
-
25 microM, inhibition of parasite growth
(E/Z)-N'-benzylidene-3-phenylquinoxaline-2-hydrazide
-
25 microM, inhibition of parasite growth
(m-bromophenyl)ethylketone thiosemicarbazone
-
-
-
(methanethiolato)[2,2'-(thio-kappaS)bis[ethanethiolato-kappaS]] oxorhenium (V)
-
-
(p-methoxyphenylthiolato-S)[2,6-bis[(mercapto-kappaS)methyl]pyridine-kappaN] oxorhenium(V)
-
-
1,10-phenanthroline
-
-
1-(2,5-dimethylbenzyl)-5-methyl-1H-indole-2,3-dione
-
IC50: 0.08 mM
1-(3-methoxybenzyl)-5-methyl-1H-indole-2,3-dione
-
IC50: 0.002 mM
1-(biphenyl-2-ylmethyl)-5-methyl-1H-indole-2,3-dione
-
IC50: 0.0028 mM
1-benzyl-5-chloro-1H-indole-2,3-dione
-
IC50: 0.09 mM
1-benzyl-5-iodo-1H-indole-2,3-dione
-
IC50: 0.09 mM
2,2-dimethyl-5-[4-(N-phenyl-N'-phenylethyl)amidinopiperazin-1-ylmethyl]-2H-benzimidazole 1,3-di-N-oxide
-
-
-
2-(N-1-phenyl-ethylidenehydrazino)-4-trifluoromethylpyrimidine
-
100 microM
2-(N-1-phenyl-ethylidenehydrazino)-5-methyl-4-trifluoro-methyl-pyrimidine
-
100 microM
2-(N-1-phenyl-ethylidenehydrazino)-6-methyl-4-trifluoro-methyl-pyrimidine
-
100 microM
2-(N-2-hydroxy-benzylidenehydrazino)-4-trifluoromethyl-pyrimidine
-
100 microM
2-(N-2-hydroxy-benzylidenehydrazino)-5-methyl-4-trifluoromethyl-pyrimidine
-
100 microM
2-(N-2-hydroxy-benzylidenehydrazino)-6-methyl-4-trifluoromethyl-pyrimidine
-
100 microM
2-(N-2-methoxy-benzylidenehydrazino)-4-trifluoromethyl-pyrimidine
-
100 microM
2-(N-2-methoxy-benzylidenehydrazino)-5-methyl-4-trifluoromethyl-pyrimidine
-
100 microM
2-(N-2-methoxy-benzylidenehydrazino)-6-methyl-4-trifluoromethyl-pyrimidine
-
100 microM, 20% inhibitory effect
2-(N-2-methyl-benzylidenehydrazino)-4-trifluoromethyl-pyrimidine
-
100 microM, 45% inhibitory effect
2-(N-2-methyl-benzylidenehydrazino)-5-methyl-4-trifluoromethyl-pyrimidine
-
100 microM
2-(N-2-methyl-benzylidenehydrazino)-6-methyl-4-trifluoromethyl-pyrimidine
-
100 microM, 45% inhibitory effect
2-(N-4-chloro-benzylidenehydrazino)-4-trifluoromethyl-pyrimidine
-
100 microM, 80% inhibitory effect
2-(N-4-chloro-benzylidenehydrazino)-5-methyl-4-trifluoro-methyl-pyrimidine
-
100 microM
2-(N-4-chloro-benzylidenehydrazino)-6-methyl-4-trifluoro-methyl-pyrimidine
-
100 microM, 60% inhibitory effect
2-(N-4-methoxy-benzylidenehydrazino)-4-trifluoromethyl-pyrimidine
-
100 microM, 40% inhibitory effect
2-(N-4-methoxy-benzylidenehydrazino)-5-methyl-4-trifluoromethyl-pyrimidine
-
100 microM
2-(N-4-methoxy-benzylidenehydrazino)-6-methyl-4-trifluoro-methyl-pyrimidine
-
100 microM
2-(N-4-methyl-benzylidenehydrazino)-4-trifluoromethyl-pyrimidine
-
100 microM, 40% inhibitory effect
2-(N-4-methyl-benzylidenehydrazino)-5-methyl-4-trifluoromethyl-pyrimidine
-
100 microM
2-(N-4-methyl-benzylidenehydrazino)-6-methyl-4-trifluoromethyl-pyrimidine
-
100 microM
2-(N-4-nitro-benzylidenehydrazino)-4-trifluoromethylpyrimidine
-
100 microM, 50% inhibitory effect
2-(N-4-nitro-benzylidenehydrazino)-5-methyl-4-trifluoromethyl-pyrimidine
-
100 microM
2-(N-4-nitro-benzylidenehydrazino)-6-methyl-4-trifluoro-methyl-pyrimidine
-
100 microM
2-(N-benzylidenehydrazino)-4-trifluoromethylpyrimidine
-
100 microM, 30% inhibitory effect
2-(N-benzylidenehydrazino)-5-methyl-4-trifluoromethyl-pyrimidine
-
100 microM
2-(N-benzylidenehydrazino)-6-methyl-4-trifluoromethyl-pyrimidine
-
100 microM
2-[(2Z)-2-[(2Z)-(3-bromobenzylidene)hydrazinylidene]-3-methyl-4-oxo-1,3-thiazolidin-5-yl]-N-methylacetamide
-
17% inhibition at 0.1 mM inhibitor and 140 nM enzyme
2-[(2Z)-2-[(2Z)-(4-chlorobenzylidene)hydrazinylidene]-3-methyl-4-oxo-1,3-thiazolidin-5-yl]-N-methylacetamide
-
7% inhibition at 0.1 mM inhibitor and 140 nM enzyme
2-[(2Z)-2-[(2Z)-(4-fluorobenzylidene)hydrazinylidene]-3-methyl-4-oxo-1,3-thiazolidin-5-yl]-N-methylacetamide
-
3% inhibition at 0.1 mM inhibitor and 140 nM enzyme
2-[(2Z)-2-[(2Z)-(4-methoxybenzylidene)hydrazinylidene]-4-oxo-1,3-thiazolidin-5-yl]-N-methylacetamide
-
22% inhibition at 0.1 mM inhibitor and 140 nM enzyme
2-[(2Z)-2-[(2Z)-benzylidenehydrazinylidene]-4-oxo-1,3-thiazolidin-5-yl]-N-methylacetamide
-
3% inhibition at 0.1 mM inhibitor and 140 nM enzyme
2-[(2Z)-2-[(2Z)-[1-(3-bromophenyl)ethylidene]hydrazinylidene]-3-methyl-4-oxo-1,3-thiazolidin-5-yl]-N-methylacetamide
-
22% inhibition at 0.1 mM inhibitor and 140 nM enzyme
2-[(benzofuroxan-5-yl)methylene]-1-(2-hydroxybenzylidene)hydrazine
-
-
2-[(benzofuroxan-5-yl)methylene]-1-(4-hydroxybenzylidene)hydrazine
-
-
2-[(benzofuroxan-5-yl)methylene]-1-(5-bromo-2-hydroxybenzylidene)hydrazine
-
-
3,4,5-trimethoxy-N'-[(E)-(4-nitrophenyl)methylidene]benzohydrazide
-
-
3,4,5-trimethoxy-N'-[(E)-naphthalen-1-ylmethylidene]benzohydrazide
-
-
3-(4-[(1S)-1,2-dimethyl-1-[(quinolin-6-ylmethyl)amino]propyl]-1H-1,2,3-triazol-1-yl)-1-(2,3,5,6-tetrafluorophenoxy)heptan-2-one
10 microM
3-(4-[(1S)-1,2-dimethyl-1-[(quinolin-6-ylmethyl)amino]propyl]-1H-1,2,3-triazol-1-yl)-2-oxoheptyl 2,6-bis(trifluoromethyl)benzoate
10 microM
3-(4-[(1S)-1,2-dimethyl-1-[(quinolin-6-ylmethyl)amino]propyl]-1H-1,2,3-triazol-1-yl)-2-oxoheptyl 2,6-dimethylbenzoate
10 microM
3-(4-[(1S)-1-[(1,3-benzothiazol-6-ylmethyl)amino]-1,2-dimethylpropyl]-1H-1,2,3-triazol-1-yl)-1-(2,3,5,6-tetrafluorophenoxy)heptan-2-one
10 microM
3-(4-[(1S)-1-[(1,3-benzothiazol-6-ylmethyl)amino]-1,2-dimethylpropyl]-1H-1,2,3-triazol-1-yl)-2-oxoheptyl 2,6-bis(trifluoromethyl)benzoate
10 microM
4-(benzofuroxan-5-ylmethyloxy)benzaldehyde amidinohydrazone
-
-
4-(benzofuroxan-5-ylmethyloxy)benzaldehyde semicarbazone
-
0.1 mM, 36% of inhibition
4-(benzofuroxan-5-ylmethyloxy)benzaldehyde thiosemicarbazone
-
-
5-chloro-1-(4-chlorobenzyl)-1H-indole-2,3-dione
-
IC50: 0.006 mM
5-fluoro-1H-indole-2,3-dione
-
IC50: 0.03 mM
5-[4-(N,N'-diphenyl)amidinopiperazin-1-ylmethyl]benzo[1,2-c]1,2,5-oxadiazole N-oxide
-
-
-
5-[4-(N-benzyl-N'-phenyl)amidinopiperazin-1-ylmethyl]-2,2-dimethyl-2H-benzimidazole 1,3-di-N-oxide
-
-
-
5-[4-(N-benzyl-N'-phenyl)amidinopiperazin-1-ylmethyl]benzo[1,2-c]1,2,5-oxadiazole N-oxide
-
-
-
5-[4-(N-furyl-N'-phenyl)amidinopiperazin-1-ylmethyl]-2,2-dimethyl-2H-benzimidazole 1,3-di-N-oxide
-
-
-
5-[4-(N-furyl-N'-phenyl)amidinopiperazin-1-ylmethyl]benzo[1,2-c]1,2,5-oxadiazole N-oxide
-
-
-
5-[4-(N-phenyl-N'-phenylethyl)amidinopiperazin-1-yl methyl]benzo[1,2-c]1,2,5-oxadiazole N-oxide
-
-
-
6-[(E)-2-(phenylsulfonyl)ethenyl]-2,1,3-benzoxadiazole 1-oxide
-
-
aceto[2,6-bis[(butylthio-jS)methyl]phenyl-kappaC]-,(SP-4-3)-palladium(II)
-
-
alpha2-Macroglobulin
-
40% inhibition at a 1:1 ratio of cruzipain and alpha2-macroglobulin
-
Amphotericin B
-
-
antipain
-
-
azocasein
-
substrate inhibition
-
benznidazole
-
presents 80% inhibitory activity against amastigotes in LLC-MK2 cell culture infected with amastigote and trypomastigote forms of the parasite, leads to parasite recrudescence in trypomastigotes on the 15th day at 0.01 mM
benzofuroxan-5-carboxaldehyde thiosemicarbazone
-
0.1 mM, 7% of inhibition
benzyl 5-chloro-2,3-dioxoindoline-1-carboxylate
-
IC50: 0.08 mM
benzyloxycarbonyl-Phe-Ala-fluoromethylketone
-
-
benzyloxycarbonyl-Phe-Arg-aminomethyl coumarin
-
substrate inhibition
biotin-Phe-Ala-fluoromethylketone
-
-
captopril
-
-
chagasin mutant delta T31-T32
-
-
-
chagasin mutant P30A
-
-
-
chagasin mutant T31A
-
-
-
chagasin mutant T31A/T32A
-
-
-
chagasin mutant T31S
-
-
-
chagasin mutant T31V
-
-
-
chagasin mutant T31Y
-
-
-
chagasin mutant T32A
-
-
-
chagasin mutant T32E
-
-
-
chagasin mutant T32S
-
-
-
chagasin mutant T32V
-
-
-
chagasin mutant T32Y
-
-
-
chagasin mutant W93A
-
-
-
chagasin mutant Y89F
-
-
-
chagasin mutant Y89S
-
-
-
chicken cystatin
-
-
-
chloro[2,2'-(thio-kappaS)bis[ethanethiolato-kappaS]] oxorhenium(V)
-
-
chymostatin
-
-
Cystatin
-
-
-
diaceto[2-[(2-pyridinyl-kappaN)methyl]-phenyl-kappaC]Au(III)-,(SP-4-3)
-
-
guanidine hydrochloride
-
activates at low concentrations but inhibits above 2 M
heparan sulfate
-
-
Human cystatin C
-
-
-
hydroxymethylnitrofurazone
-
presents 100% inhibitory activity against amastigotes in LLC-MK2 cell culture infected with amastigote and trypomastigote forms of the parasite, leads to complete inhibtiion in trypomastigotes at 0.005 mM
iodoacetamide
-
-
K11777
-
the chemotherapeutical drug targets the major cysteine protease cruzain and disrupts amastigote intracellular development. The mechanism of drug resistance, in primary epimastigotes, is due to secretion of inactive, unprocessed cruzain
KSCN
-
activates at low concentrations but inhibits above 1 M
L-kininogen
-
L-trans-epoxysuccinylleucylamido(4-guanidino)butane
leupeptin
methyl (2E)-[(2Z)-2-[(2Z)-(4-chlorobenzylidene)hydrazinylidene]-3-methyl-4-oxo-1,3-thiazolidin-5-ylidene]ethanoate
-
75% inhibition at 0.1 mM inhibitor and 140 nM enzyme
methyl (2E)-[(2Z)-2-[(2Z)-(4-methoxybenzylidene)hydrazinylidene]-3-methyl-4-oxo-1,3-thiazolidin-5-ylidene]ethanoate
-
71% inhibition at 0.1 mM inhibitor and 140 nM enzyme
methyl (2E)-[(2Z)-2-[(2Z)-(4-methoxybenzylidene)hydrazinylidene]-4-oxo-1,3-thiazolidin-5-ylidene]ethanoate
-
7% inhibition at 0.1 mM inhibitor and 140 nM enzyme
methyl (2E)-[(2Z)-3-methyl-4-oxo-2-[(2Z)-[4-(trifluoromethyl)benzylidene]hydrazinylidene]-1,3-thiazolidin-5-ylidene]ethanoate
-
65% inhibition at 0.1 mM inhibitor and 140 nM enzyme
N'-(furan-2-ylmethyl)-N-phenylpiperazine-1-carboximidamide
-
10% inhibition at 0.1 mM, at pH 5.3, temperature not specified in the publication
N'-benzyl-N-phenylpiperazine-1-carboximidamide
-
5.4% inhibition at 0.1 mM, at pH 5.3, temperature not specified in the publication
N'-[(E)-(2,6-dichlorophenyl)methylidene]-3,4,5-trimethoxybenzohydrazide
-
-
N'-[(E)-(4-bromophenyl)methylidene]-3,4,5-trimethoxybenzohydrazide
-
-
N,N'-diphenylpiperazine-1-carboximidamide
-
6.3% inhibition at 0.1 mM, at pH 5.3, temperature not specified in the publication
N-carbobenzoxy-FA-diazomethylketone
-
inhibition in vivo
N-carbobenzoxy-FF-diazomethylketone
-
inhibition in vivo
N-carbobenzoxy-FK-acyloxymethylketone
-
inhibition in vivo
N-carbobenzoxy-VVR-4-nitroanilide
-
strong substrate inhibition
N-methyl-2-[(2Z)-3-methyl-4-oxo-2-[(2Z)-[4-(trifluoromethyl)benzylidene]hydrazinylidene]-1,3-thiazolidin-5-yl]acetamide
-
27% inhibition at 0.1 mM inhibitor and 140 nM enzyme
N-methyl-2-[(2Z)-4-oxo-2-[(2Z)-(2-sulfanylbenzylidene)hydrazinylidene]-1,3-thiazolidin-5-yl]acetamide
-
27% inhibition at 0.1 mM inhibitor and 140 nM enzyme
N-phenyl benzofuroxan-5-carboxaldehyde thiosemicarbazone
-
-
N-phenyl-N'-(2-phenylethyl)piperazine-1-carboximidamide
-
3.2% inhibition at 0.1 mM, at pH 5.3, temperature not specified in the publication
N4-allyl benzofuroxan-5-carboxaldehyde thiosemicarbazone
-
0.1 mM, 36% of inhibition
Nalpha-[(2R,3E)-2-benzyl-4-(phenylsulfonyl)but-3-enoyl]-N-(morpholin-4-ylcarbonyl)-L-phenylalaninamide
-
-
Nalpha-[(2R,3E)-2-benzyl-4-(phenylsulfonyl)but-3-enoyl]-N-[(4-methylpiperazin-1-yl)carbonyl]-L-phenylalaninamide
nifurtimox
-
25 microM
nitrofurazone
-
a 5-nitro-2-furfurylidenesemicarbazone, presents 90% inhibitory activity against amastigotes in LLC-MK2 cell culture infected with amastigote and trypomastigote forms of the parasite, leads to parasite recrudescence in trypomastigotes on the 15th day at 0.005 mM
pregnancy zone protein
-
50% inhibition at a 1:1 ratio of cruzipain and pregnancy zone protein
-
primaquine
-
active against cruzipain, design of selective prodrugs Lys-Arg-primaquine, Phe-Ala-primaquine, and Phe-Arg-primaquine to be cleaved by the enzyme in vivo and selectively inhibiting it, overview
propeptide of cruzipain
-
PCZ, is also a good inhibitor of brucipain from Trypanosoma brucei. The propeptide of cruzipain does not inhibit human cathepsins S, K or B or papain at the tested concentrations, and moderately inhibits human cathepsin V. Human cathepsin F is very efficiently inhibited (Ki of 32 picomol/L)
-
Stefin A
-
-
-
Stefin B
-
-
-
trans-epoxysuccinyl-L-leucylamido-(4-guanidino)butane
Triton X-100
-
non-specific inhibition in the presence of 0.02% (v/v) Triton X-100
Urea
-
70% inhibition at 5 M
[(2Z)-2-[(2Z)-(2-fluorobenzylidene)hydrazinylidene]-4-oxo-1,3-thiazolidin-5-yl]acetic acid
-
6% inhibition at 0.1 mM inhibitor and 140 nM enzyme
[(2Z)-2-[(2Z)-(4-chlorobenzylidene)hydrazinylidene]-4-oxo-1,3-thiazolidin-5-yl]acetic acid
-
11% inhibition at 0.1 mM inhibitor and 140 nM enzyme
[(2Z)-2-[(2Z)-(4-methoxybenzylidene)hydrazinylidene]-4-oxo-1,3-thiazolidin-5-yl]acetic acid
-
38% inhibition at 0.1 mM inhibitor and 140 nM enzyme
[(2Z)-2-[(2Z)-(4-nitrobenzylidene)hydrazinylidene]-4-oxo-1,3-thiazolidin-5-yl]acetic acid
-
4% inhibition at 0.1 mM inhibitor and 140 nM enzyme
[(2Z)-4-oxo-2-[(2Z)-(thiophen-2-ylmethylidene)hydrazinylidene]-1,3-thiazolidin-5-yl]acetic acid
-
34% inhibition at 0.1 mM inhibitor and 140 nM enzyme
[(S)-1-carboxy-2-phenylethyl]-carbamoyl-L-Arg-L-Val-arginal
-
-
additional information
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
2-mercaptoethanol
activates
dithiothreitol
activates
guanidine hydrochloride
-
activates at low concentrations but inhibits above 2 M
heparan sulfate
-
6-fold increased catalytic efficiency
KSCN
-
activates at low concentrations but inhibits above 1 M
L-cysteine
activates
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0003 - 0.001
2-aminobenzoic acid-KLRFSKQ-N-(2,4-dinitrophenyl)ethylenediamine
0.019
2-aminobenzoyl-ARF-(2,4-dinitrophenyl)-epsilon-NH2-lysine-OH
-
37°C, pH 5.5
0.0013
2-aminobenzoyl-FRA-(2,4-dinitrophenyl)-epsilon-NH2-lysine-NH2
-
37°C, pH 5.5
0.0035
2-aminobenzoyl-FRA-(2,4-dinitrophenyl)-epsilon-NH2-lysine-OH
-
37°C, pH 5.5
0.0039
2-aminobenzoyl-FRF-(2,4-dinitrophenyl)-epsilon-NH2-lysine-OH
-
37°C, pH 5.5
0.000065 - 0.00012
2-aminobenzoyl-LGMISLMKRPQ-N-(2,4-dinitrophenyl)ethylenediamine
0.0036
2-aminobenzoyl-Phe-Arg-(2,4-dinitrophenyl)-epsilon-NH2-lysine-Pro-OH
-
37°C, pH 5.5
0.0023
2-aminobenzoyl-Phe-Arg-(2,4-dinitrophenyl)-epsilon-NH2-lysine-Trp-OH
-
37°C, pH 5.5
0.00095
2-aminobenzoyl-RRF-(2,4-dinitrophenyl)-epsilon-NH2-lysine-OH
-
37°C, pH 5.5
0.001
Ac-Phe-Arg-7-amido-4-methylcoumarin
-
-
0.028 - 0.029
azocasein
-
0.0006 - 0.015
benzoyl-FR-aminomethyl coumarin
0.043
benzoyl-HR-aminomethyl coumarin
-
pH 6.3, 37°C
0.066
benzoyl-PFR-4-nitroanilide
-
-
0.0119
benzoyl-RR-aminomethyl coumarin
-
pH 6.3, 37°C
0.001
benzoyl-YR-aminomethyl coumarin
-
-
0.0011
benzyloxycarbonyl-FR-aminomethyl coumarin
-
pH 6.3, 37°C
0.0008 - 0.0032
benzyloxycarbonyl-Phe-Arg-aminomethyl coumarin
0.0058
epsilon-NH2(capryl)-L-(SBzl)C-7-amido-4-methylcoumarin
-
-
0.0021
N-alpha-benzyloxy-carbonyl-L-phenylalanyl-L-alanine-(7-amido-4-methylcoumarin)
-
37°C, pH 6.5
0.0025
N-alpha-benzyloxycarbonyl-L-arginyl-L-alanine-(7-amido-4-methylcoumarin)
-
37°C, pH 6.5
0.0021
N-alpha-benzyloxycarbonyl-L-tyrosyl-L-alanine-(7-amido-4-methylcoumarin)
-
37°C, pH 6.5
0.011
N-carbobenzoxy-Arg-Arg-2-(4-methoxy)-naphthylamide
-
-
0.033
N-carbobenzoxy-VVR-4-nitroanilide
-
pH 9
0.0044
o-aminobenzoyl-ALRFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
0.0021
o-aminobenzoyl-HLRFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
0.006
o-aminobenzoyl-KARFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
0.0051
o-aminobenzoyl-KFRFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
0.0028
o-aminobenzoyl-KLFFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
0.0114
o-aminobenzoyl-KLGFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
0.0079
o-aminobenzoyl-KLKFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
0.004 - 0.0051
o-aminobenzoyl-KLRFAKQ-N-(2,4-dinitrophenyl)-ethylenediamine
0.0046
o-aminobenzoyl-KLRFFKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
0.0079
o-aminobenzoyl-KLRFPKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
0.0022 - 0.0073
o-aminobenzoyl-KLRFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
0.0078
o-aminobenzoyl-KLRFSPQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
0.0046
o-aminobenzoyl-KLRFSRQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
0.0038
o-aminobenzoyl-KLRLSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
0.0132
o-aminobenzoyl-KLRRSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
0.0117
o-aminobenzoyl-KPRFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
0.0032
o-aminobenzoyl-KRRFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
0.0036
o-aminobenzoyl-LLRFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0683 - 0.08
2-aminobenzoic acid-KLRFSKQ-N-(2,4-dinitrophenyl)ethylenediamine
0.1
2-aminobenzoyl-ARF-(2,4-dinitrophenyl)-epsilon-NH2-lysine-OH
Trypanosoma cruzi
-
37°C, pH 5.5
4.2
2-aminobenzoyl-FRA-(2,4-dinitrophenyl)-epsilon-NH2-lysine-NH2
Trypanosoma cruzi
-
37°C, pH 5.5
5.5
2-aminobenzoyl-FRA-(2,4-dinitrophenyl)-epsilon-NH2-lysine-OH
Trypanosoma cruzi
-
37°C, pH 5.5
2.9
2-aminobenzoyl-FRF-(2,4-dinitrophenyl)-epsilon-NH2-lysine-OH
Trypanosoma cruzi
-
37°C, pH 5.5
0.025 - 0.0583
2-aminobenzoyl-LGMISLMKRPQ-N-(2,4-dinitrophenyl)ethylenediamine
1.4
2-aminobenzoyl-Phe-Arg-(2,4-dinitrophenyl)-epsilon-NH2-lysine-Pro-OH
Trypanosoma cruzi
-
37°C, pH 5.5
3.4
2-aminobenzoyl-Phe-Arg-(2,4-dinitrophenyl)-epsilon-NH2-lysine-Trp-OH
Trypanosoma cruzi
-
37°C, pH 5.5
0.13
2-aminobenzoyl-RRF-(2,4-dinitrophenyl)-epsilon-NH2-lysine-OH
Trypanosoma cruzi
-
37°C, pH 5.5
0.0433 - 0.193
benzoyl-FR-aminomethyl coumarin
0.172
benzoyl-HR-aminomethyl coumarin
Trypanosoma cruzi
-
-
0.0783
benzoyl-RR-aminomethyl coumarin
Trypanosoma cruzi
-
-
0.158
benzyloxycarbonyl-FR-aminomethyl coumarin
Trypanosoma cruzi
-
-
2.16 - 4.49
benzyloxycarbonyl-Phe-Arg-aminomethyl coumarin
10.8
epsilon-NH2(capryl)-L-(SBzl)C-7-amido-4-methylcoumarin
Trypanosoma cruzi
-
-
0.14
N-alpha-benzyloxy-carbonyl-L-phenylalanyl-L-alanine-(7-amido-4-methylcoumarin)
Trypanosoma cruzi
-
37°C, pH 6.5
0.15
N-alpha-benzyloxycarbonyl-L-arginyl-L-alanine-(7-amido-4-methylcoumarin)
Trypanosoma cruzi
-
37°C, pH 6.5
0.13
N-alpha-benzyloxycarbonyl-L-tyrosyl-L-alanine-(7-amido-4-methylcoumarin)
Trypanosoma cruzi
-
37°C, pH 6.5
0.0805
N-carbobenzoxy-Arg-Arg-2-(4-methoxy)-naphthylamide
Trypanosoma cruzi
-
-
4.5
o-aminobenzoyl-ALRFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
Trypanosoma cruzi
-
-
5.6
o-aminobenzoyl-HLRFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
Trypanosoma cruzi
-
-
1.3
o-aminobenzoyl-KARFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
Trypanosoma cruzi
-
-
1.9
o-aminobenzoyl-KFRFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
Trypanosoma cruzi
-
-
2.5
o-aminobenzoyl-KLFFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
Trypanosoma cruzi
-
-
5.6
o-aminobenzoyl-KLGFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
Trypanosoma cruzi
-
-
14.2
o-aminobenzoyl-KLKFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
Trypanosoma cruzi
-
-
8.2 - 15.2
o-aminobenzoyl-KLRFAKQ-N-(2,4-dinitrophenyl)-ethylenediamine
9.7
o-aminobenzoyl-KLRFFKQ-N-(2,4-dinitrophenyl)-ethylenediamine
Trypanosoma cruzi
-
-
2.8
o-aminobenzoyl-KLRFPKQ-N-(2,4-dinitrophenyl)-ethylenediamine
Trypanosoma cruzi
-
-
4.3 - 6.9
o-aminobenzoyl-KLRFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
13.9
o-aminobenzoyl-KLRFSPQ-N-(2,4-dinitrophenyl)-ethylenediamine
Trypanosoma cruzi
-
-
12.5
o-aminobenzoyl-KLRFSRQ-N-(2,4-dinitrophenyl)-ethylenediamine
Trypanosoma cruzi
-
-
9.1
o-aminobenzoyl-KLRLSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
Trypanosoma cruzi
-
-
1.9
o-aminobenzoyl-KLRRSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
Trypanosoma cruzi
-
-
0.5
o-aminobenzoyl-KPRFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
Trypanosoma cruzi
-
-
7.7
o-aminobenzoyl-KRRFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
Trypanosoma cruzi
-
-
6.7
o-aminobenzoyl-LLRFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
Trypanosoma cruzi
-
-
additional information
additional information
-
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.48 - 0.79
azocasein
-
0.023 - 0.1
benzyloxycarbonyl-Phe-Arg-aminomethyl coumarin
0.0000000076
chagasin
-
-
-
0.000005868
chagasin mutant deltaT31-T32
-
-
-
0.00000002
chagasin mutant P30A
-
-
-
0.000000317
chagasin mutant T31A
-
-
-
0.000001065
chagasin mutant T31A/T32A
-
-
-
0.000000011
chagasin mutant T31S
-
-
-
0.00000007
chagasin mutant T31V
-
-
-
0.000000747
chagasin mutant T31Y
-
-
-
0.000000016
chagasin mutant T32A
-
-
-
0.000000011
chagasin mutant T32E
-
-
-
0.00000002
chagasin mutant T32S
-
-
-
0.000000193
chagasin mutant T32V
-
-
-
0.000000016
chagasin mutant T32Y
-
-
-
0.000000031
chagasin mutant W93A
-
-
-
0.00000002
chagasin mutant Y89F
-
-
-
0.000000025
chagasin mutant Y89S
-
-
-
0.018 - 0.2637
propeptide of cruzipain
-
additional information
additional information
Ki for cystatins and kininogens in the picomolar range
-
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.00008
(1E)-1-(3,4-dichlorophenyl)-2-phenylethan-1-one thiosemicarbazone
Trypanosoma cruzi
-
IC50: 80 nM
0.00004
(1E)-1-(3,4-dichlorophenyl)-3-phenylpropan-1-one thiosemicarbazone
Trypanosoma cruzi
-
IC50: 40 nM
0.000019
(1E)-1-(3,4-dichlorophenyl)pentan-1-one thiosemicarbazone
Trypanosoma cruzi
-
IC50: 19 nM
0.00003
(1E)-1-(3,4-dichlorophenyl)propan-1-one thiosemicarbazone
Trypanosoma cruzi
-
IC50: 30 nM
0.00031
(1E)-1-(3-bromophenyl)propan-1-one thiosemicarbazone
Trypanosoma cruzi
-
IC50: 310 nM
0.00003
(1E,2E)-1-(3,4-dichlorophenyl)-3-phenylprop-2-en-1-one thiosemicarbazone
Trypanosoma cruzi
-
IC50: 30 nM
0.00003
(1Z)-1-(3,4-dichlorophenyl)-2-phenoxyethan-1-one thiosemicarbazone
Trypanosoma cruzi
-
IC50: 30 nM
0.000015
(2(1H)-pyridinethionato-kappaS2)[2,6-bis[(mercapto-KappaS)methyl]pyridine-kappaN1] oxorhenium(V)
Trypanosoma cruzi
-
-
0.1
(2E)-1,3-bis(2,4,5-trimethoxyphenyl)prop-2-en-1-one
Trypanosoma cruzi
-
pH 6.5, 22°C
0.025
(2E)-1,3-di(naphthalen-2-yl)prop-2-en-1-one
Trypanosoma cruzi
-
pH 6.5, 22°C
0.025
(2E)-1-(1,3-benzodioxol-5-yl)-3-(1-naphthyl)-2-propen-1-one
Trypanosoma cruzi
-
pH 6.5, 22°C
0.02
(2E)-1-(1,3-benzodioxol-5-yl)-3-(2,6-dichlorophenyl)-2-propen-1-one
Trypanosoma cruzi
-
pH 6.5, 22°C
0.025
(2E)-1-(1,3-benzodioxol-5-yl)-3-(2-chlorophenyl)-2-propen-1-one
Trypanosoma cruzi
-
pH 6.5, 22°C
0.05
(2E)-1-(1,3-benzodioxol-5-yl)-3-(3-methoxy-4-phenoxyphenyl)prop-2-en-1-one
Trypanosoma cruzi
-
pH 6.5, 22°C
0.046
(2E)-1-(1,3-benzodioxol-5-yl)-3-(4-buthoxyphenyl)-2-propen-1-one
Trypanosoma cruzi
-
pH 6.5, 22°C
0.023
(2E)-1-(1,3-benzodioxol-5-yl)-3-(5-methylfuran-2-yl)-2-propen-1-one
Trypanosoma cruzi
-
pH 6.5, 22°C
0.022
(2E)-1-(1,3-benzodioxol-5-yl)-3-(thiophen-2-yl)-2-propen-1-one
Trypanosoma cruzi
-
pH 6.5, 22°C
0.048
(2E)-1-(2',4',5'-trimethoxyphenyl)-3-(1-naphthyl)-2-propen-1-one
Trypanosoma cruzi
-
pH 6.5, 22°C
0.1
(2E)-1-(2',4',5'-trimethoxyphenyl)-3-(thiophen-2-yl)-2-propen-1-one
Trypanosoma cruzi
-
pH 6.5, 22°C
0.037
(2E)-1-(2'-hydroxy,3'-bromo,4',6'-dimethoxyphenyl)-3-(1-naphthyl)-2-propen-1-one
Trypanosoma cruzi
-
pH 6.5, 22°C
0.082
(2E)-1-(2'-hydroxy-3'-bromo-4',6'-dimethoxyphenyl)-3-(4-buthoxyphenyl)-2-propen-1- one
Trypanosoma cruzi
-
pH 6.5, 22°C
0.1
(2E)-1-(2,4-dimethoxyphenyl)-3-(2,4,5-trimethoxyphenyl)prop-2-en-1-one
Trypanosoma cruzi
-
pH 6.5, 22°C
0.025
(2E)-1-(2-naphthyl)-3-(2,6-dimethoxyphenyl)-2-propen-1-one
Trypanosoma cruzi
-
pH 6.5, 22°C
0.025
(2E)-1-(2-naphthyl)-3-(5-methylfuran-2-yl)-2-propen-1-one
Trypanosoma cruzi
-
pH 6.5, 22°C
0.045
(2E)-1-(3-bromo-2-hydroxy-4,6-dimethoxyphenyl)-3-(3-nitrophenyl)prop-2-en-1-one
Trypanosoma cruzi
-
pH 6.5, 22°C
0.02
(2E)-1-(3-bromo-2-hydroxy-4,6-dimethoxyphenyl)-3-(4-methoxyphenyl)prop-2-en-1-one
Trypanosoma cruzi
-
pH 6.5, 22°C
0.05
(2E)-1-(3a,7a-dihydro-1,3-benzodioxol-5-yl)-3-(3,4,5-trimethoxyphenyl)prop-2-en-1-one
Trypanosoma cruzi
-
pH 6.5, 22°C
0.05
(2E)-1-(3a,7a-dihydro-1,3-benzodioxol-5-yl)-3-(3-methoxyphenyl)prop-2-en-1-one
Trypanosoma cruzi
-
pH 6.5, 22°C
0.035
(2E)-1-(3a,7a-dihydro-1,3-benzodioxol-5-yl)-3-(4-methoxyphenyl)prop-2-en-1-one
Trypanosoma cruzi
-
pH 6.5, 22°C
0.03
(2E)-1-(3a,7a-dihydro-1,3-benzodioxol-5-yl)-3-(4-methylphenyl)prop-2-en-1-one
Trypanosoma cruzi
-
pH 6.5, 22°C
0.05
(2E)-1-(3a,7a-dihydro-1,3-benzodioxol-5-yl)-3-phenylprop-2-en-1-one
Trypanosoma cruzi
-
pH 6.5, 22°C
0.025
(2E)-1-(4-hydroxy-1,3-benzodioxol-5-yl)-3-(2,4,5-trimethoxyphenyl)prop-2-en-1-one
Trypanosoma cruzi
-
pH 6.5, 22°C
0.1
(2E)-3-(1,3-benzodioxol-5-yl)-1-(2-hydroxyphenyl)prop-2-en-1-one
Trypanosoma cruzi
-
pH 6.5, 22°C
0.02
(2E)-3-(1,3-benzodioxol-5-yl)-1-(4-bromophenyl)prop-2-en-1-one
Trypanosoma cruzi
-
pH 6.5, 22°C
0.05
(2E)-3-(1,3-benzodioxol-5-yl)-1-(naphthalen-2-yl)prop-2-en-1-one
Trypanosoma cruzi
-
pH 6.5, 22°C
0.1
(2E)-3-(3-methoxyphenyl)-1-(2,4,5-trimethoxyphenyl)prop-2-en-1-one
Trypanosoma cruzi
-
pH 6.5, 22°C
0.03
(2E)-3-(4-bromophenyl)-1-(3a,7a-dihydro-1,3-benzodioxol-5-yl)prop-2-en-1-one
Trypanosoma cruzi
-
pH 6.5, 22°C
0.05
(2E)-3-(4-fluorophenyl)-1-(naphthalen-2-yl)prop-2-en-1-one
Trypanosoma cruzi
-
pH 6.5, 22°C
0.05 - 0.06
(2E)-3-(4-methoxyphenyl)-1-(naphthalen-2-yl)prop-2-en-1-one
0.037
(2E)-3-[4-(benzyloxy)-3-methoxyphenyl]-1-(2,4-dimethoxyphenyl)prop-2-en-1-one
Trypanosoma cruzi
-
pH 6.5, 22°C
0.05
(2E)-N'-(3'-bromo-4'-hydroxy-5'-methoxybenzilidene)-3,4,5-trimethoxybenzohydrazide
Trypanosoma cruzi
-
pH 6.5, 22°C
0.047
(2E)-N'-(4'-buthoxybenzilidene)-3,4,5-trimethoxybenzohydrazide
Trypanosoma cruzi
-
pH 6.5, 22°C
0.05
(2E)-N'-(4'-hydroxy-5'-methoxybenzilidene)-3,4,5-trimethoxybenzohydrazide
Trypanosoma cruzi
-
pH 6.5, 22°C
0.01
(3S,5R,10R)-N-benzyl-3-(2-methylpropyl)-2-oxo-10-[(E)-2-(phenylsulfonyl)ethenyl]-1,4-diazecane-5-carboxamide
0.0002 - 0.006
(3S,5R,11R)-N-benzyl-3-(2-methylpropyl)-2-oxo-11-[(E)-2-(phenylsulfonyl)ethenyl]-1,4-diazacycloundecane-5-carboxamide
0.008
(3Z)-1H-indole-2,3-dione 3-thiosemicarbazone
Trypanosoma cruzi
-
IC50: 0.008 mM
0.016
(3Z)-5,7-dimethyl-1H-indole-2,3-dione 3-thiosemicarbazone
Trypanosoma cruzi
-
IC50: 0.016 mM
0.02
(3Z)-5-bromo-1H-indole-2,3-dione 3-thiosemicarbazone
Trypanosoma cruzi
-
IC50: 0.02 mM
0.021
(3Z)-5-chloro-1H-indole-2,3-dione 3-thiosemicarbazone
Trypanosoma cruzi
-
IC50: 0.021 mM
0.0105
(3Z)-5-chloro-7-methyl-1H-indole-2,3-dione 3-thiosemicarbazone
Trypanosoma cruzi
-
IC50: 0.0105 mM
0.009
(3Z)-5-iodo-1H-indole-2,3-dione 3-thiosemicarbazone
Trypanosoma cruzi
-
IC50: 0.009 mM
0.02 - 0.05
(3Z)-5-methyl-1H-indole-2,3-dione 3-thiosemicarbazone
Trypanosoma cruzi
-
IC50: 0.02-0.05 mM
0.03
(3Z)-5-nitro-1H-indole-2,3-dione 3-thiosemicarbazone
Trypanosoma cruzi
-
IC50: 0.03 mM
0.00003
(E)-(3,4-dichlorophenyl)(2-phenylcyclopropyl)methanone thiosemicarbazone
Trypanosoma cruzi
-
IC50: 30 nM
0.00004
(E)-(3,4-dichlorophenyl)(4-methylphenyl)methanone thiosemicarbazone
Trypanosoma cruzi
-
IC50: 40 nM
0.003
(E)-cyclohexyl(3,4-dichlorophenyl)methanone thiosemicarbazone
Trypanosoma cruzi
-
IC50: 3000 nM
0.02
(E/Z)-N'-(2-hydroxybenzylidene)-3-methylquinoxaline-2-hydrazide
Trypanosoma cruzi
-
-
0.0159
(E/Z)-N'-(2-hydroxybenzylidene)-3-phenylquinoxaline-2-hydrazide
Trypanosoma cruzi
-
-
0.005
(methanethiolato)[2,2'-(thio-kappaS)bis[ethanethiolato-kappaS]] oxorhenium (V)
Trypanosoma cruzi
-
-
0.00035
(p-methoxyphenylthiolato-S)[2,6-bis[(mercapto-kappaS)methyl]pyridine-kappaN] oxorhenium(V)
Trypanosoma cruzi
-
-
0.08
1-(2,5-dimethylbenzyl)-5-methyl-1H-indole-2,3-dione
Trypanosoma cruzi
-
IC50: 0.08 mM
0.002
1-(3-methoxybenzyl)-5-methyl-1H-indole-2,3-dione
Trypanosoma cruzi
-
IC50: 0.002 mM
0.0028
1-(biphenyl-2-ylmethyl)-5-methyl-1H-indole-2,3-dione
Trypanosoma cruzi
-
IC50: 0.0028 mM
0.09
1-benzyl-5-chloro-1H-indole-2,3-dione
Trypanosoma cruzi
-
IC50: 0.09 mM
0.09
1-benzyl-5-iodo-1H-indole-2,3-dione
Trypanosoma cruzi
-
IC50: 0.09 mM
0.15
2-(N-2-methoxy-benzylidenehydrazino)-6-methyl-4-trifluoromethyl-pyrimidine
Trypanosoma cruzi
-
above 0.15 mM
0.1
2-(N-2-methyl-benzylidenehydrazino)-4-trifluoromethyl-pyrimidine
Trypanosoma cruzi
-
above 0.1 mM
0.1
2-(N-2-methyl-benzylidenehydrazino)-6-methyl-4-trifluoromethyl-pyrimidine
Trypanosoma cruzi
-
above 0.1 mM
0.085
2-(N-4-chloro-benzylidenehydrazino)-4-trifluoromethyl-pyrimidine
Trypanosoma cruzi
-
-
0.1
2-(N-4-chloro-benzylidenehydrazino)-6-methyl-4-trifluoro-methyl-pyrimidine
Trypanosoma cruzi
-
about 0.1 mM
0.1
2-(N-4-methoxy-benzylidenehydrazino)-4-trifluoromethyl-pyrimidine
Trypanosoma cruzi
-
above 0.1 mM
0.1
2-(N-4-methyl-benzylidenehydrazino)-4-trifluoromethyl-pyrimidine
Trypanosoma cruzi
-
above 0.1 mM
0.1
2-(N-4-nitro-benzylidenehydrazino)-4-trifluoromethylpyrimidine
Trypanosoma cruzi
-
about 0.1 mM
0.15
2-(N-benzylidenehydrazino)-4-trifluoromethylpyrimidine
Trypanosoma cruzi
-
above 0.15 mM
0.068
2-[(benzofuroxan-5-yl)methylene]-1-(2-hydroxybenzylidene)hydrazine
Trypanosoma cruzi
-
-
0.1
2-[(benzofuroxan-5-yl)methylene]-1-(4-hydroxybenzylidene)hydrazine
Trypanosoma cruzi
-
-
0.073
2-[(benzofuroxan-5-yl)methylene]-1-(5-bromo-2-hydroxybenzylidene)hydrazine
Trypanosoma cruzi
-
-
0.06
3,4,5-trimethoxy-N'-[(E)-(4-nitrophenyl)methylidene]benzohydrazide
Trypanosoma cruzi
-
pH 6.5, 22°C
0.04
3,4,5-trimethoxy-N'-[(E)-naphthalen-1-ylmethylidene]benzohydrazide
Trypanosoma cruzi
-
pH 6.5, 22°C
0.032
4-(benzofuroxan-5-ylmethyloxy)benzaldehyde amidinohydrazone
Trypanosoma cruzi
-
-
0.1
4-(benzofuroxan-5-ylmethyloxy)benzaldehyde semicarbazone
Trypanosoma cruzi
-
above 0.1 mM
0.043
4-(benzofuroxan-5-ylmethyloxy)benzaldehyde thiosemicarbazone
Trypanosoma cruzi
-
-
0.006
5-chloro-1-(4-chlorobenzyl)-1H-indole-2,3-dione
Trypanosoma cruzi
-
IC50: 0.006 mM
0.03
5-fluoro-1H-indole-2,3-dione
Trypanosoma cruzi
-
IC50: 0.03 mM
0.00007
aceto[2,6-bis[(butylthio-jS)methyl]phenyl-kappaC]-,(SP-4-3)-palladium(II)
Trypanosoma cruzi
-
-
0.1
benzofuroxan-5-carboxaldehyde thiosemicarbazone
Trypanosoma cruzi
-
above 0.1 mM
0.08
benzyl 5-chloro-2,3-dioxoindoline-1-carboxylate
Trypanosoma cruzi
-
IC50: 0.08 mM
0.00004
chloro[2,2'-(thio-kappaS)bis[ethanethiolato-kappaS]] oxorhenium(V)
Trypanosoma cruzi
-
-
0.0007
diaceto[2-[(2-pyridinyl-kappaN)methyl]-phenyl-kappaC]Au(III)-,(SP-4-3)
Trypanosoma cruzi
-
-
0.0106
hydroxymethylnitrofurazone
Trypanosoma cruzi
-
pH 6.5, 37°C
0.05
N'-[(E)-(2,6-dichlorophenyl)methylidene]-3,4,5-trimethoxybenzohydrazide
Trypanosoma cruzi
-
pH 6.5, 22°C
0.055
N'-[(E)-(4-bromophenyl)methylidene]-3,4,5-trimethoxybenzohydrazide
Trypanosoma cruzi
-
pH 6.5, 22°C
0.078
N-phenyl benzofuroxan-5-carboxaldehyde thiosemicarbazone
Trypanosoma cruzi
-
-
0.1
N4-allyl benzofuroxan-5-carboxaldehyde thiosemicarbazone
Trypanosoma cruzi
-
above 0.1 mM
0.000004 - 0.0001
Nalpha-[(2R,3E)-2-benzyl-4-(phenylsulfonyl)but-3-enoyl]-N-[(4-methylpiperazin-1-yl)carbonyl]-L-phenylalaninamide
0.0077
nifurtimox
Trypanosoma cruzi
-
-
0.0228
nitrofurazone
Trypanosoma cruzi
-
pH 6.5, 37°C
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
0.008 - 1.68
-
4-nitroanilide derivatives
0.1 - 3.77
-
beta-naphthylamide derivatives
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
4.5
-
hydrolysis of 2-aminobenzoyl-FRA-(2,4-dinitrophenyl)-epsilon-NH2-lysine-OH
5
-
assay with azocasein
5.5
-
room temperature, 45 min
6 - 7
-
hydrolysis of 2-aminobenzoyl-FRA-(2,4-dinitrophenyl)-epsilon-NH2-lysine-NH2
6.8
-
KEEASSAVVGGPG as substrate; KEEASSAVVRGPG as substrate
7
-
beta-naphthylamide derivatives as substrate
9
-
4-nitroanilide derivatives as substrate
additional information
-
substrates placing hydrophobic residues in the specificity pocket are cleaved at a broader pH range than hydrophilic substrates
pH RANGE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
3.5 - 9
-
pH 3.5: about 65% of maximal activity, pH 6.5-9.0: about 55% of maximal activity, hydrolysis of 2-aminobenzoyl-FRA-(2,4-dinitrophenyl)-epsilon-NH2-lysine-OH
4.5 - 7.4
-
hydrophobic substrates reach 50% activity at pH 4.5 and maintain full activity above pH 7.5, more hydrophilic side chains only reach 50% activity at pH 5.5-6
4.5 - 9
-
pH 4.5: about 45% of maximal activity, pH 9.0: about 45% of maximal activity, hydrolysis of 2-aminobenzoyl-FRA-(2,4-dinitrophenyl)-epsilon-NH2-lysine-NH2
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
22
-
assay at room temperature
28
-
assay at pH 6.5
additional information
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
-
studies are carried out using murine macrophage cell line J774 as well as bone marrow-derived macrophages from BALB/c mice
Manually annotated by BRENDA team
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY hide
GeneOntology No.
LITERATURE
SOURCE
-
the signaling factor NF-kB P65 colocalizes with cruzain on the cell surface of intracellular wild-type parasites
Manually annotated by BRENDA team
PDB
SCOP
CATH
ORGANISM
UNIPROT
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
12000
-
x * 12000, non-adsorbed (to concanavalin A-Sepharose) cruzipain isoform, SDS-PAGE
14020
-
MALDI-TOF
23540
-
electrospray mass spectrometry
35000 - 60000
-
SDS-PAGE, depending on electrophoretic conditions
36300
-
calculated from nucleotide sequence
36400
-
SDS-PAGE
40000
about 40000 Da, calculated from amino acid sequence; about 40000 Da, calculated from amino acid sequence; about 40000 Da, calculated from amino acid sequence; about 40000 Da, calculated from amino acid sequence; about 40000 Da, calculated from amino acid sequence; about 40000 Da, calculated from amino acid sequence; about 40000 Da, calculated from amino acid sequence
43000
-
deglycosylated enzyme, SDS-PAGE
51000
-
glycosylated enzyme, SDS-PAGE
SUBUNITS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
?
-
x * 12000, non-adsorbed (to concanavalin A-Sepharose) cruzipain isoform, SDS-PAGE
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
glycoprotein
additional information
Crystallization/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
bound to benzoyl-Arg-Ala-fluoromethyl ketone and benzoyl-Tyr-Ala-fluoromethyl ketone, hanging drop vapor diffusion method
-
complexed with benzyloxycarbonyl-Phe-Ala-fluoromethylketone
-
enzyme lacking the C-terminal domain, complexed with benzyloxycarbonyl-Phe-Ala-fluoromethylketone
-
recombinant protein and truncated version
-
pH STABILITY
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
2.75
-
exponential decrease of activity in the presence of substrate
638891
8.7
-
unstable in the absence of substrate at 37°C
638878
additional information
TEMPERATURE STABILITY
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
5 - 37
-
inactivation at pH 2.25 and pH 10 increases with increasing temperature
37
-
unstable in the absence of substrate at pH 8.7
45
-
E219P mutant, stable for 10 h
GENERAL STABILITY
ORGANISM
UNIPROT
LITERATURE
unstable in the absence of substrate at pH 8.7 and 37°C
-
STORAGE STABILITY
ORGANISM
UNIPROT
LITERATURE
Purification/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
a subset of cruzipain molecules
-
using an Ni-nitrilotriacetic acid-agarose resin
-
Cloned/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
active complete mature enzyme
-
enzyme and truncated version
-
expression in Escherichia coli BL21-D3 strain
-
expression in Escherichia coli strain DH5alpha
-
expression of cruzipain truncated in the C-terminal extension in Escherichia coli strains M15 and DH5alpha
-
full-length propeptide of cruzipain is cloned by PCR and expressed in Escherichia coli as a fusion protein with a 6xHis tag at the N-terminus
-
EXPRESSION
ORGANISM
UNIPROT
LITERATURE
the levels of cruzipain expression by wild-type parasites are enhanced after in vivo passage in Rhodnius prolixus
ENGINEERING
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
C25A
-
enzyme is inactive
E219P
-
variant with altered cleavage recognition site
additional information
APPLICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
drug development
-
cruzipain is an attractive target for the development of novel trypanocidal drugs
medicine
CatL-like sequences are excellent targets for diagnosis and genotyping of Trypanosoma rangeli by PCR; CatL-like sequences are excellent targets for diagnosis and genotyping of Trypanosoma rangeli by PCR; CatL-like sequences are excellent targets for diagnosis and genotyping of Trypanosoma rangeli by PCR; CatL-like sequences are excellent targets for diagnosis and genotyping of Trypanosoma rangeli by PCR; CatL-like sequences are excellent targets for diagnosis and genotyping of Trypanosoma rangeli by PCR; CatL-like sequences are excellent targets for diagnosis and genotyping of Trypanosoma rangeli by PCR; CatL-like sequences are excellent targets for diagnosis and genotyping of Trypanosoma rangeli by PCR
molecular biology
-
in this study it is shown in murine macrophage cell line J774 as well as in murine bone marrow-derived macrophages, that cruzipain induces p38 phosphorylation with Trypanosoma cruzi infection triggering mainly JNK and ERK phosphorylation. Cruzipain also favors the survival in macrophages by changing the iNOS/arginase balance
pharmacology