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Enzyme Nomenclature
Information on EC 3.4.22.51 - cruzipain
for references in articles please use BRENDA:EC3.4.22.51
Word Map on EC 3.4.22.51
- 3.4.22.51
-
cathepsins
-
protozoan
- trypomastigotes
- epimastigotes
- brucei
-
proteinases
-
trypanocidal
- amastigote
- papain
-
trypanosomal
- trypanosomiasis
- benznidazole
-
latin
-
anti-trypanosoma
-
cystatins
-
antiparasitic
-
papain-like
- thiosemicarbazone
- rhodesiense
-
kininogens
- trypanothione
- nifurtimox
- congolense
-
antichagasic
-
cruzi-infected
-
chagasin
-
metacyclic
-
metacyclogenesis
-
reservosomes
- falcipain-2
- trans-sialidase
-
warhead
- pharmacology
- medicine
- molecular biology
- drug development
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The enzyme appears in viruses and cellular organisms
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EC NUMBER 
COMMENTARY 
3.4.22.51
-
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RECOMMENDED NAME
GeneOntology No.
cruzipain
-
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REACTION
REACTION DIAGRAM
COMMENTARY
ORGANISM
UNIPROT
LITERATURE
broad endopeptidase specificity similar to that of cathepsin L
-
-
-
-
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REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
hydrolysis of peptide bond
hydrolysis of peptide bond
-
-
-
-
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CAS REGISTRY NUMBER
COMMENTARY
102227-51-0
-
141588-22-9
-
84399-99-5
-
90371-53-2
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ORGANISM
COMMENTARY
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
-
638875, 638876, 638877, 638878, 638879, 638880, 638881, 638882, 638883, 638885, 638886, 638887, 638888, 638890, 638891, 638892
SwissProt
-
667144, 667653, 667936, 667951, 668522, 668551, 670178, 670179, 677418, 679761, 679892, 696523, 696645, 696710, 696760, 697814, 697939, 698164, 698293, 699388, 700567, 701365, 717475, 717894, 717917, 718066, 718182, 718307, 732453, 732673
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recombinantly expressed in Escherichia coli as a C-terminally truncated protein
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-
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GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY
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
physiological function
-
infection with wild-type parasites appears to induce cruzain-mediated proteolysis of NF-kappaB P65 leading to unresponsiveness of the host macrophage during early 60 min of infection. This immune evasion mechanism may be critical for Trypaosoma cruzi survival during early natural infection with a low number of trypmastigotes. The signaling factor NF-kappaB P65 colocalizes with cruzain on the cell surface of intracellular wild-type parasites, and is proteolytically cleaved. Transcription factor NF-kappaB P65 is translocated to the nucleus and activated only in macrophages infected with cruzain-deficient parasites
physiological function
-
cruzipain promotes Trypanosoma cruzi adhesion to Rhodnius prolixus midgut
physiological function
-
cruzipain promotes Trypanosoma cruzi adhesion to Rhodnius prolixus midgut
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SUBSTRATE
PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
(Substrate)
LITERATURE
(Substrate)
(Substrate)
COMMENTARY
(Product)
(Product)
LITERATURE
(Product)
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
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
-
-
-
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
-
-
-
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
-
-
-
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
-
-
-
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
-
-
-
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
-
-
-
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
-
-
-
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
-
-
-
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
-
-
-
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
-
-
-
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
-
-
-
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
-
-
-
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
-
-
-
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
-
-
-
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
-
-
-
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
-
-
-
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
-
-
-
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
-
-
-
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
-
-
-
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
-
-
-
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
-
-
-
ir
2-aminobenzoic acid-ALRFSKQ-N-(2,4-dinitrophenyl)ethylenediamine + H2O
?
-
-
-
-
?
2-aminobenzoic acid-KLGFSKQ-N-(2,4-dinitrophenyl)ethylenediamine + H2O
?
-
-
-
-
?
2-aminobenzoic acid-KLRFSKQ-N-(2,4-dinitrophenyl)ethylenediamine + H2O
?
-
and analogues
-
-
?
2-aminobenzoic acid-peptidyl-N-(2,4-dinitrophenyl)ethylenediamine + H2O
?
-
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
?
-
-
-
-
?
2-aminobenzoyl-FRA-(2,4-dinitrophenyl)-epsilon-NH2-lysine-NH2 + H2O
?
-
-
-
-
?
2-aminobenzoyl-FRA-(2,4-dinitrophenyl)-epsilon-NH2-lysine-OH + H2O
?
-
-
-
-
?
2-aminobenzoyl-FRF-(2,4-dinitrophenyl)-epsilon-NH2-lysine-OH + H2O
?
-
-
-
-
?
2-aminobenzoyl-Phe-Arg-(2,4-dinitrophenyl)-epsilon-NH2-lysine-Pro-OH + H2O
?
-
-
-
-
?
2-aminobenzoyl-Phe-Arg-(2,4-dinitrophenyl)-epsilon-NH2-lysine-Trp-OH + H2O
?
-
-
-
-
?
2-aminobenzoyl-RRF-(2,4-dinitrophenyl)-epsilon-NH2-lysine-OH + H2O
?
-
-
-
-
?
Ac-Phe-Arg-7-amido-4-methylcoumarin + H2O
Ac-Phe-Arg + 7-amino-4-methylcoumarin
-
10 microM, 4 nanoM cruzain, 45 min, room temperature, pH 5.5
-
-
?
benzoyl-HR-4-methylcoumarin 7-amide + H2O
?
-
less susceptible substrate
-
-
?
benzoyl-Phe-Arg-4-methylcoumarin-7-amide + H2O
?
-
fluorogenic substrates based on the peptide benzoyl-Phe-Arg-4-methylcoumarin-7-amide
-
-
?
benzoyl-Phe-Val-Arg-p-nitroanilide + H2O
?
-
as active as with benzyloxycarbonyl-Arg-Arg-methoxy-beta-naphthylamide
-
-
?
benzoyl-Pro-Phe-Arg-p-nitroanilide + H2O
?
-
41% of the activity with benzyloxycarbonyl-Arg-Arg-methoxy-beta-naphthylamide
-
-
?
benzoyl-RR-4-methylcoumarin 7-amide + H2O
?
-
less susceptible substrate
-
-
?
benzoyl-Val-Gly-Arg-p-nitroanilide + H2O
?
-
52% of the activity with benzyloxycarbonyl-Arg-Arg-methoxy-beta-naphthylamide
-
-
?
benzyloxycarbonyl-Ala-Arg-Arg-methoxy-beta-naphthylamide + H2O
?
-
36% of the activity with benzyloxycarbonyl-Arg-Arg-methoxy-beta-naphthylamide
-
-
?
benzyloxycarbonyl-Gly-Pro-Arg-p-nitroanilide + H2O
?
-
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
relatively low rates of substrate hydrolysis
-
-
?
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Phe-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
benzyloxycarbonyl-Phe-Arg-methoxy-beta-naphthylamide + H2O
?
-
30% of the activity with benzyloxycarbonyl-Arg-Arg-methoxy-beta-naphthylamide
-
-
?
Bz-Phe-Arg-4-methylcoumaryl-7-amide + H2O
Bz-Phe-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
Bz-Pro-Phe-Arg-4-nitroanilide + H2O
Bz-Pro-Phe-Arg + 4-nitroaniline
-
-
-
-
?
human IgG + H2O
?
-
specific cleavage sites on human IgG subclasses by cruzipain
-
-
?
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
-
-
-
-
?
N-alpha-benzyloxycarbonyl-L-arginyl-L-alanine-(7-amido-4-methylcoumarin) + H2O
N-alpha-benzyloxycarbonyl-L-arginyl-L-alanine + 7-amino-4-methylcoumarin
-
-
-
-
?
N-alpha-benzyloxycarbonyl-L-tyrosyl-L-alanine-(7-amido-4-methylcoumarin) + H2O
N-alpha-benzyloxycarbonyl-L-tyrosyl-L-alanine + 7-amino-4-methylcoumarin
-
-
-
-
?
N-carbobenzoxy-Arg-Arg-2-(4-methoxy)-naphthylamide + H2O
N-carbobenzoxy-Arg-Arg + 2-amino-4-methoxynaphthalene
-
-
-
-
?
N-tert-butoxycarbonyl-O-benzyl-Ser-Gly-Arg-p-nitroanilide + H2O
?
-
39% of the activity with benzyloxycarbonyl-Arg-Arg-methoxy-beta-naphthylamide
-
-
?
N-tert-butoxycarbonyl-Val-Leu-Gly-Arg-p-nitroanilide + H2O
?
-
24% of the activity with benzyloxycarbonyl-Arg-Arg-methoxy-beta-naphthylamide
-
-
?
o-aminobenzoyl-ALRFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine + H2O
?
-
-
-
-
?
o-aminobenzoyl-HLRFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine + H2O
?
-
-
-
-
?
o-aminobenzoyl-KARFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine + H2O
?
-
-
-
-
?
o-aminobenzoyl-KFRFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine + H2O
?
-
-
-
-
?
o-aminobenzoyl-KLFFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine + H2O
o-aminobenzoyl-KLF + FSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
-
-
?
o-aminobenzoyl-KLGFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine + H2O
o-aminobenzoyl-KLG + FSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
-
-
?
o-aminobenzoyl-KLKFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine + H2O
o-aminobenzoyl-KLK + FSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
-
-
?
o-aminobenzoyl-KLRFAKQ-N-(2,4-dinitrophenyl)-ethylenediamine + H2O
o-aminobenzoyl-KLR + FAKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
-
-
?
o-aminobenzoyl-KLRFFKQ-N-(2,4-dinitrophenyl)-ethylenediamine + H2O
o-aminobenzoyl-KLR + FFKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
-
-
?
o-aminobenzoyl-KLRFPKQ-N-(2,4-dinitrophenyl)-ethylenediamine + H2O
o-aminobenzoyl-KLR + FPKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
-
-
?
o-aminobenzoyl-KLRFSFQ-N-(2,4-dinitrophenyl)-ethylenediamine + H2O
o-aminobenzoyl-KLR + FSFQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
no hydrolysis is detected
-
-
?
o-aminobenzoyl-KLRFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine + H2O
o-aminobenzoyl-KLR + FSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
-
-
?
o-aminobenzoyl-KLRFSPQ-N-(2,4-dinitrophenyl)-ethylenediamine + H2O
o-aminobenzoyl-KLR + FSPQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
-
-
?
o-aminobenzoyl-KLRFSRQ-N-(2,4-dinitrophenyl)-ethylenediamine + H2O
o-aminobenzoyl-KLR + FSRQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
-
-
?
o-aminobenzoyl-KLRLSKQ-N-(2,4-dinitrophenyl)-ethylenediamine + H2O
o-aminobenzoyl-KLR + LSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
-
-
?
o-aminobenzoyl-KLRRSKQ-N-(2,4-dinitrophenyl)-ethylenediamine + H2O
o-aminobenzoyl-KLR + RSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
-
-
?
o-aminobenzoyl-KPRFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine + H2O
?
-
-
-
-
?
o-aminobenzoyl-KRRFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine + H2O
?
-
-
-
-
?
o-aminobenzoyl-LLRFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine + H2O
?
-
-
-
-
?
peptidyl-methylcoumarin amide + H2O
?
-
and derivatives, enzyme shows preference for benzyl-Cys or Arg at the P1 position and a hydrophobic non-aromatic residue at position P2
-
-
?
tosyl-Gly-Pro-Arg-p-nitroanilide + H2O
?
-
25% of the activity with benzyloxycarbonyl-Arg-Arg-methoxy-beta-naphthylamide
-
-
?
Z-Phe-Arg-7-amido-4-methylcoumarin + H2O
Z-Phe-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
2-aminobenzoyl-LGMISLMKRPQ-N-(2,4-dinitrophenyl)ethylenediamine + H2O
?
-
-
-
-
?
2-aminobenzoyl-LGMISLMKRPQ-N-(2,4-dinitrophenyl)ethylenediamine + H2O
?
-
Abz-LGMISLMKRPQ-EDDnp
-
-
?
benzoyl-FR-4-methylcoumarin 7-amide + H2O
?
-
fluorigenic substrates based on this peptide, substitution of Phe results in less susceptible substrates
-
-
?
benzyloxycarbonyl-Phe-Arg-4-methylcoumarin 7-amide + H2O
?
-
-
-
?
benzyloxycarbonyl-Phe-Arg-4-methylcoumarin 7-amide + H2O
?
-
-
-
-
?
Gelatin + H2O
?
-
-
-
?
N-carbobenzoxy-Val-Val-Arg-4-nitroanilide + H2O
?
-
excellent substrate
-
-
?
additional information
?
-
-
enzyme may be involved in facilitating parasite entry into the brain
-
-
-
additional information
?
-
-
enzyme may be involved in facilitating parasite entry into the brain
-
-
-
additional information
?
-
no substrate: benzyloxycarbonyl-Arg-Arg-aminomethyl coumarin
-
-
-
additional information
?
-
-
substrates are chromogenic peptides with a carboxyl Arg or Lys, enzyme requires at least one more amino acid, preferably Arg, Phe, Val or Leu between the terminal Arg or Lys and the amino-blocking group
-
-
?
additional information
?
-
-
substrates are chromogenic peptides with a carboxyl Arg or Lys, enzyme requires at least one more amino acid, preferably Arg, Phe, Val or Leu between the terminal Arg or Lys and the amino-blocking group
-
-
?
additional information
?
-
-
antigenic character in natural human infections
-
-
-
additional information
?
-
stimulates potent humoral and cellular immune response during infection in both humans and mice
-
-
-
additional information
?
-
-
enzyme plays a role in the production of antibodies against cardiac M2 muscarinic acetylcholine receptor
-
-
-
additional information
?
-
-
cruzipain may act as a survival factor for cardiomyocytes because it rescues them from apoptosis and stimulates arginase-2
-
-
-
additional information
?
-
-
substrate specificity of cruzipain 2 isoform is analysed using internally quenched flurogenic substrates. It is found that cruzipain 2 compared to cruzipain differs substantially regarding the specificity in the S2, S1' and S2' pockets, suggesting that cruzipain 2 acts on distinct natural substrates
-
-
-
additional information
?
-
-
design of selective prodrugs of primaquine: Lys-Arg-primaquine, Phe-Ala-primaquine, and Phe-Arg-primaquine, cleaved by the enzyme in vivo and selectively inhibiting it, overview
-
-
-
additional information
?
-
-
design of selective prodrugs of primaquine: Lys-Arg-primaquine, Phe-Ala-primaquine, and Phe-Arg-primaquine, cleaved by the enzyme in vivo and selectively inhibiting it, overview. The molecular mechanism acts via nucleophilic attack of the catalytic Cys25 residue on the respective prodrug amide carbonyl carbon, releasing primaquine, docking study showing specific interactions between the prodrug and the S1 and S2 pockets of cruzipain with the dipeptides acting as distance holders
-
-
-
additional information
?
-
-
involvement of O-linked GlcNAc moiety present in the major cysteine protease both in cruzipain recognition and in the cross-reactivity between cruzipain and myosin molecules
-
-
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
NATURAL SUBSTRATES
NATURAL PRODUCTS
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
(Substrate)
LITERATURE
(Substrate)
(Substrate)
COMMENTARY
(Product)
(Product)
LITERATURE
(Product)
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
Gelatin + H2O
?
D0QZL7, D0QZL8, D0QZM0, D0QZM2, D0QZM5, D0QZM6, D0QZM9
-
-
-
?
additional information
?
-
-
enzyme may be involved in facilitating parasite entry into the brain
-
-
-
additional information
?
-
-
enzyme may be involved in facilitating parasite entry into the brain
-
-
-
additional information
?
-
-
antigenic character in natural human infections
-
-
-
additional information
?
-
Q598P5
stimulates potent humoral and cellular immune response during infection in both humans and mice
-
-
-
additional information
?
-
-
enzyme plays a role in the production of antibodies against cardiac M2 muscarinic acetylcholine receptor
-
-
-
additional information
?
-
-
cruzipain may act as a survival factor for cardiomyocytes because it rescues them from apoptosis and stimulates arginase-2
-
-
-
additional information
?
-
-
design of selective prodrugs of primaquine: Lys-Arg-primaquine, Phe-Ala-primaquine, and Phe-Arg-primaquine, cleaved by the enzyme in vivo and selectively inhibiting it, overview
-
-
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY
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
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY
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,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-(1,3-benzodioxol-5-yl)-3-(3-methoxy-4-phenoxyphenyl)prop-2-en-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-(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-(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-(4-bromophenyl)-1-(3a,7a-dihydro-1,3-benzodioxol-5-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'-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)-5-chloro-7-methyl-1H-indole-2,3-dione 3-thiosemicarbazone
-
IC50: 0.0105 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
(methanethiolato)[2,2'-(thio-kappaS)bis[ethanethiolato-kappaS]] oxorhenium (V)
-
-
(p-methoxyphenylthiolato-S)[2,6-bis[(mercapto-kappaS)methyl]pyridine-kappaN] oxorhenium(V)
-
-
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-(5-bromo-2-hydroxybenzylidene)hydrazine
-
-
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 semicarbazone
-
0.1 mM, 36% of inhibition
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
-
-
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
-
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
guanidine hydrochloride
-
activates at low concentrations but inhibits above 2 M
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
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
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,N'-diphenylpiperazine-1-carboximidamide
-
6.3% inhibition at 0.1 mM, at pH 5.3, temperature not specified in the publication
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-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
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)
-
Triton X-100
-
non-specific inhibition in the presence of 0.02% (v/v) Triton X-100
[(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
(3S,5R,10R)-N-benzyl-3-(2-methylpropyl)-2-oxo-10-[(E)-2-(phenylsulfonyl)ethenyl]-1,4-diazecane-5-carboxamide
-
-
(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
-
-
(3S,5R,11R)-N-benzyl-3-(2-methylpropyl)-2-oxo-11-[(E)-2-(phenylsulfonyl)ethenyl]-1,4-diazacycloundecane-5-carboxamide
-
-
L-kininogen
-
high molecular weight kininogen, inhibition decreases 10fold in presence of 0.1 mM heparan sulfate
-
Nalpha-[(2R,3E)-2-benzyl-4-(phenylsulfonyl)but-3-enoyl]-N-[(4-methylpiperazin-1-yl)carbonyl]-L-phenylalaninamide
-
-
Nalpha-[(2R,3E)-2-benzyl-4-(phenylsulfonyl)but-3-enoyl]-N-[(4-methylpiperazin-1-yl)carbonyl]-L-phenylalaninamide
-
-
trans-epoxysuccinyl-L-leucylamido-(4-guanidino)butane
-
irreversible inhibitor
additional information
pro-region of the trypanosomal enzyme inhibits the enzyme function, cystatins and kininogens are inhibitors, overview: inhibitors
-
additional information
-
in general immunoglobulin G fractions isolated from rabbits immunised with rabbit apha2-macroglobulin-recombinant catalytic domain of congopain-complexes are the most inhibitory towards the proteolytic activity of congopain. Antibodies produced by rabbits immunised with recombinant catalytic domain of congopain in Freund's adjuvant are generally found to weakly inhibit congopain with a maximum of 40%
-
additional information
-
synthesis of 2-hydrazolyl-4-thiazolidinones based on multicomponent reactions and biological evaluation against Trypanosoma cruzi, inhibitory potencies and cytotoxic effects, molecular modeling and QSAR studies, overview. No inhibition by (RS)-2-(2-(2-bromobenzylidene)hydrazono)-3-methyl-4-oxo-5-thiazolidine-N-methylacetamide and (Z)-((2-(4-fluorobenzylidene)hydrazono)-3-methyl-5-methoxycarbonylmethylene)thiazolidin-4-one at 0.1 mM
-
additional information
-
synthesis and inhibitory effects against cruzipaon of a series of thirty-three chalcone and seven hydrazide derivatives, overview
-
additional information
-
AM1 semi-empirical molecular modeling studies analysing cruzain inhibitory activity, overview
-
additional information
-
0.01% (v/v) of Triton X-100 does not interfere with enzyme activity
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
guanidine hydrochloride
-
activates at low concentrations but inhibits above 2 M
Urea
-
maximal at 2 M with natural substrates, no activation with synthetic substrates
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
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
0.0036
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
0.0021
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
0.0003
2-aminobenzoic acid-KLRFSKQ-N-(2,4-dinitrophenyl)ethylenediamine
-
recombinant form without C-terminal extension
0.000065
2-aminobenzoyl-LGMISLMKRPQ-N-(2,4-dinitrophenyl)ethylenediamine
-
with 0.06 mM heparan sulfate
0.00012
2-aminobenzoyl-LGMISLMKRPQ-N-(2,4-dinitrophenyl)ethylenediamine
-
-
0.0006
benzoyl-FR-aminomethyl coumarin
-
recombinant form without C-terminal extension
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.1
2-aminobenzoyl-ARF-(2,4-dinitrophenyl)-epsilon-NH2-lysine-OH
-
37°C, pH 5.5
4.2
2-aminobenzoyl-FRA-(2,4-dinitrophenyl)-epsilon-NH2-lysine-NH2
-
37°C, pH 5.5
5.5
2-aminobenzoyl-FRA-(2,4-dinitrophenyl)-epsilon-NH2-lysine-OH
-
37°C, pH 5.5
2.9
2-aminobenzoyl-FRF-(2,4-dinitrophenyl)-epsilon-NH2-lysine-OH
-
37°C, pH 5.5
1.4
2-aminobenzoyl-Phe-Arg-(2,4-dinitrophenyl)-epsilon-NH2-lysine-Pro-OH
-
37°C, pH 5.5
3.4
2-aminobenzoyl-Phe-Arg-(2,4-dinitrophenyl)-epsilon-NH2-lysine-Trp-OH
-
37°C, pH 5.5
0.13
2-aminobenzoyl-RRF-(2,4-dinitrophenyl)-epsilon-NH2-lysine-OH
-
37°C, pH 5.5
0.14
N-alpha-benzyloxy-carbonyl-L-phenylalanyl-L-alanine-(7-amido-4-methylcoumarin)
-
37°C, pH 6.5
0.15
N-alpha-benzyloxycarbonyl-L-arginyl-L-alanine-(7-amido-4-methylcoumarin)
-
37°C, pH 6.5
0.13
N-alpha-benzyloxycarbonyl-L-tyrosyl-L-alanine-(7-amido-4-methylcoumarin)
-
37°C, pH 6.5
0.0683
2-aminobenzoic acid-KLRFSKQ-N-(2,4-dinitrophenyl)ethylenediamine
-
recombinant form without C-terminal extension
0.0583
2-aminobenzoyl-LGMISLMKRPQ-N-(2,4-dinitrophenyl)ethylenediamine
-
with 0.06 mM heparan sulfate
0.055
benzoyl-FR-aminomethyl coumarin
-
recombinant form without C-terminal extension
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
additional information
additional information
Ki for cystatins and kininogens in the picomolar range
-
0.018
propeptide of cruzipain
-
at pH 6.5 the propeptide of cruzipain inactivates cruzipain competitively
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
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;
-
-
0.025
(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
0.037
(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
0.016
(3Z)-5,7-dimethyl-1H-indole-2,3-dione 3-thiosemicarbazone
Trypanosoma cruzi;
-
IC50: 0.016 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
0.00003
(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
0.0159
(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;
-
-
0.0028
1-(biphenyl-2-ylmethyl)-5-methyl-1H-indole-2,3-dione
Trypanosoma cruzi;
-
IC50: 0.0028 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
0.1
4-(benzofuroxan-5-ylmethyloxy)benzaldehyde semicarbazone
Trypanosoma cruzi;
-
above 0.1 mM
0.00007
aceto[2,6-bis[(butylthio-jS)methyl]phenyl-kappaC]-,(SP-4-3)-palladium(II)
Trypanosoma cruzi;
-
-
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;
-
-
0.05
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
0.1
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
0.05
(2E)-3-(4-methoxyphenyl)-1-(naphthalen-2-yl)prop-2-en-1-one
Trypanosoma cruzi;
-
pH 6.5, 22°C
0.06
(2E)-3-(4-methoxyphenyl)-1-(naphthalen-2-yl)prop-2-en-1-one
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
Trypanosoma brucei rhodesiense;
-
-
0.01
(3S,5R,10R)-N-benzyl-3-(2-methylpropyl)-2-oxo-10-[(E)-2-(phenylsulfonyl)ethenyl]-1,4-diazecane-5-carboxamide
Trypanosoma cruzi;
-
above 0.01 mM
0.0002
(3S,5R,11R)-N-benzyl-3-(2-methylpropyl)-2-oxo-11-[(E)-2-(phenylsulfonyl)ethenyl]-1,4-diazacycloundecane-5-carboxamide
Trypanosoma cruzi;
-
-
0.006
(3S,5R,11R)-N-benzyl-3-(2-methylpropyl)-2-oxo-11-[(E)-2-(phenylsulfonyl)ethenyl]-1,4-diazacycloundecane-5-carboxamide
Trypanosoma brucei rhodesiense;
-
-
0.000004
Nalpha-[(2R,3E)-2-benzyl-4-(phenylsulfonyl)but-3-enoyl]-N-[(4-methylpiperazin-1-yl)carbonyl]-L-phenylalaninamide
Trypanosoma cruzi;
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-
0.0001
Nalpha-[(2R,3E)-2-benzyl-4-(phenylsulfonyl)but-3-enoyl]-N-[(4-methylpiperazin-1-yl)carbonyl]-L-phenylalaninamide
Trypanosoma brucei rhodesiense;
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-
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SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
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pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
4.5
-
hydrolysis of 2-aminobenzoyl-FRA-(2,4-dinitrophenyl)-epsilon-NH2-lysine-OH
6 - 7
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hydrolysis of 2-aminobenzoyl-FRA-(2,4-dinitrophenyl)-epsilon-NH2-lysine-NH2
6.5
7.6
additional information
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substrates placing hydrophobic residues in the specificity pocket are cleaved at a broader pH range than hydrophilic substrates
6.5
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assay at room temperature, 5 min, 0.64 nM cruzain, 50 mM sodium phosphate, 100 mM sodium chloride, 5 mM EDTA
8
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30 min, 50 mM Tris-acetate buffer, 0.3 mM Bz-Pro-Phe-Arg-pNA, 10 mM beta-mercaptoethanol
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pH RANGE
ORGANISM
UNIPROT
COMMENTARY
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
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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
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TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
additional information
additional information
-
assay at room temperature, pH 6.5, 5 min, 0.64 nM cruzain, 50 mM sodium phosphate, 100 mM sodium chloride, 5 mM EDTA
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SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
SOURCE
-
studies are carried out using murine macrophage cell line J774 as well as bone marrow-derived macrophages from BALB/c mice
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LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY
GeneOntology No.
LITERATURE
SOURCE
-
the signaling factor NF-kB P65 colocalizes with cruzain on the cell surface of intracellular wild-type parasites
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membrane bound compartments between nucleus and kinetoplast
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membrane bound compartments between nucleus and kinetoplast
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-
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PDB
SCOP
CATH
UNIPROT
ORGANISM
Trypanosoma cruzi;
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MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
12000
-
x * 12000, non-adsorbed (to concanavalin A-Sepharose) cruzipain isoform, SDS-PAGE
33000
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
50000
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SUBUNITS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
?
-
x * 12000, non-adsorbed (to concanavalin A-Sepharose) cruzipain isoform, SDS-PAGE
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POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
glycoprotein
additional information
glycoprotein
-
N-glycosylation at Asn254, no O-glycosylation or phosphorylation
glycoprotein
-
sulfated high-mannose type oligosaccharides, lactosaminic glycans and fucosylated oligosaccharides
glycoprotein
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presence of sialic acid in N-linked oligosaccharide chains and O-linked N-acetylglucosamine
glycoprotein
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single units of O-linked N-acetylglucosamine, usually components of nuclear and cytoplasmatic proteins, are present at the C-terminal domain of cruzipain. They show participation of in the molecular antigenicity of cruzipain. The immune cross-reactivity between cruzipain and myosin, in murine heart tissue, is mainly focused in the C-T domain. The O-GlcNAc moieties constitute a common epitope between cruzipain and either myosin or other cardiac O-GlcNAc-containing proteins
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Crystallization/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
bound to benzoyl-Arg-Ala-fluoromethyl ketone and benzoyl-Tyr-Ala-fluoromethyl ketone, hanging drop vapor diffusion method
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enzyme lacking the C-terminal domain, complexed with benzyloxycarbonyl-Phe-Ala-fluoromethylketone
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pH STABILITY
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
additional information
additional information
-
stable at neutral pH, inactivation studies over a pH range from pH 2.15 to pH 10
638891
additional information
-
enzymatically active and stable in neutral/acidic pH
696523
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TEMPERATURE STABILITY
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
5 - 37
-
inactivation at pH 2.25 and pH 10 increases with increasing temperature
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GENERAL STABILITY
ORGANISM
UNIPROT
LITERATURE
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STORAGE STABILITY
ORGANISM
UNIPROT
LITERATURE
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Purification/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
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Cloned/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
expression of cruzipain truncated in the C-terminal extension in Escherichia coli strains M15 and DH5alpha
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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
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EXPRESSION
ORGANISM
UNIPROT
LITERATURE
the levels of cruzipain expression by wild-type parasites are enhanced after in vivo passage in Rhodnius prolixus
the levels of cruzipain expression by wild-type parasites are enhanced after in vivo passage in Rhodnius prolixus
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the levels of cruzipain expression by wild-type parasites are enhanced after in vivo passage in Rhodnius prolixus
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-
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ENGINEERING
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
additional information
additional information
-
induction of RNAi against brucipain of Trypanosoma brucei does not cure mice from infection, however, 50% of these mice survive 60 days longer than uninduced controls. The ability of Trypanosoma brucei to cross an in vitro model of the human blood-brain barrier is also reduced by brucipain RNAi induction
additional information
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induction of RNAi against brucipain of Trypanosoma brucei does not cure mice from infection, however, 50% of these mice survive 60 days longer than uninduced controls. The ability of Trypanosoma brucei to cross an in vitro model of the human blood-brain barrier is also reduced by brucipain RNAi induction
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APPLICATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
drug development
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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
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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
pharmacology
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induction of RNAi against brucipain of Trypanosoma brucei does not cure mice from infection, however, 50% of these mice survive 60 days longer than uninduced controls. The ability of Trypanosoma brucei to cross an in vitro model of the human blood-brain barrier is also reduced by brucipain RNAi induction
pharmacology
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induction of RNAi against brucipain of Trypanosoma brucei does not cure mice from infection, however, 50% of these mice survive 60 days longer than uninduced controls. The ability of Trypanosoma brucei to cross an in vitro model of the human blood-brain barrier is also reduced by brucipain RNAi induction
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LINKS TO OTHER DATABASES (specific for EC-Number 3.4.22.51)
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