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Information on EC 3.4.22.51 - cruzipain and Organism(s) Trypanosoma cruzi and UniProt Accession P25779
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3.4.22.51 cruzipainSpecify your search results
Word Map
- 3.4.22.51
- cathepsins
- brucei
-
protozoan
- epimastigotes
- trypomastigotes
-
trypanocidal
- trypanosomiasis
-
trypanosomal
- papain
- proteinases
- amastigote
-
papain-like
- benznidazole
-
anti-trypanosoma
-
antiparasitic
-
latin
- thiosemicarbazone
-
vinyl
- rhodesiense
- cystatins
-
nitril
- trypanothione
- nifurtimox
-
antichagasic
- chagasin
- bauhinia
- kininogens
-
warhead
-
metacyclic
- medicine
-
metacyclogenesis
- falcipain-2
- congolense
-
cruzi-infected
- trans-sialidase
-
tulahuen
-
reservosomes
-
n-acylhydrazones
- pharmacology
- molecular biology
- z-phe-arg-amc
- semicarbazone
- drug development
The taxonomic range for the selected organisms is: Trypanosoma cruzi
The enzyme appears in selected viruses and cellular organisms
The enzyme appears in selected viruses and cellular organisms
Synonyms
cruzipain, cruzain, rhodesain, major cysteine proteinase, congopain, cathepsin l-like cysteine protease, cathepsin l-like protease, gp57/51, brucipain, trypanopain, 
more
topSYNONYM 
ORGANISM
UNIPROT
COMMENTARY 
LITERATURE
congopain
-
-
-
-
cruzain
cruzipain
evansain
-
-
-
-
GP57/51
-
-
-
-
proteinase, Trypanosoma congolese cysteine
-
-
-
-
proteinase, Trypanosoma cruzi cysteine
-
-
-
-
proteinase, Trypanosoma cysteine
-
-
-
-
trypanopain
-
-
-
-
Trypanosoma congolese cysteine protease
-
-
-
-
Trypanosoma cruzi cysteine protease
-
-
-
-
Trypanosoma cysteine protease
-
-
-
-
cruzain
-
-
-
-
cruzipain
-
-
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
hydrolysis of peptide bond
hydrolysis of peptide bond
-
-
-
-
CAS REGISTRY NUMBER
COMMENTARY
102227-51-0
-
141588-22-9
-
84399-99-5
-
90371-53-2
-
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
benzyloxycarbonyl-Arg-Ala-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Arg-Ala + 7-amino-4-methylcoumarin
-
-
-
?
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Arg-Arg + 7-amino-4-methylcoumarin
-
-
-
?
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Phe-Arg + 7-amino-4-methylcoumarin
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-His-Arg-7-amido-4-methylcoumarin + H2O
benzoyl-His-Arg + 7-amino-4-methylcoumarin
-
-
-
?
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-Tyr-Arg-7-amido-4-methylcoumarin + H2O
benzoyl-Tyr-Arg + 7-amino-4-methylcoumarin
-
-
-
?
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-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
tosyl-Gly-Pro-Arg + p-nitroaniline
-
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
-
-
-
-
?
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Phe-Arg + 7-amino-4-methylcoumarin
-
-
-
?
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Phe-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-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
-
-
?
benzoyl-Phe-Arg-7-amido-4-methylcoumarin + H2O
benzoyl-Phe-Arg + 7-amino-4-methylcoumarin
-
-
-
?
benzoyl-Phe-Arg-7-amido-4-methylcoumarin + H2O
benzoyl-Phe-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
benzoyl-Phe-Arg-7-amido-4-methylcoumarin + H2O
benzoyl-Phe-Arg + 7-amino-4-methylcoumarin
-
-
-
?
benzyloxycarbonyl-Phe-Arg-4-methylcoumarin 7-amide + H2O
?
-
-
-
?
benzyloxycarbonyl-Phe-Arg-4-methylcoumarin 7-amide + H2O
?
-
-
-
?
Immunoglobulin G1 + H2O
?
cleaves specifically at the hinge region
-
-
?
Immunoglobulin G3 + H2O
?
cleaves specifically at the hinge region
-
-
?
N-carbobenzoxy-Val-Val-Arg-4-nitroanilide + H2O
?
excellent substrate
-
-
?
N-carbobenzoxy-VVR-4-nitroanilide + H2O
N-carbobenzoxy-VVR + 4-nitroaniline
-
-
-
?
N-carbobenzoxy-VVR-4-nitroanilide + H2O
N-carbobenzoxy-VVR + 4-nitroaniline
-
-
-
-
?
peptidyl-beta-naphthylamide + H2O
?
derivatives of
-
-
?
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
?
-
-
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
?
-
-
antigenic character in natural human infections
-
-
?
additional information
?
-
stimulates potent humoral and cellular immune response during infection in both humans and mice
-
-
?
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
?
-
-
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
-
-
?
NATURAL SUBSTRATE
NATURAL 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
additional information
?
-
antigenic character in natural human infections
-
-
?
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
?
-
-
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
?
-
-
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
-
-
?
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
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
(2E)-2-[2-(4-bromophenoxy)-1-(4-bromophenyl)ethylidene]hydrazine-1-carbothioamide
0.05 mM, 67.5% inhibition, 23°C, pH 5.5
(2E)-2-[2-(4-bromophenoxy)-1-(4-chlorophenyl)ethylidene]hydrazine-1-carbothioamide
0.05 mM, 53.1% inhibition, 23°C, pH 5.5
(2E)-2-[2-(4-bromophenoxy)-1-(4-fluorophenyl)ethylidene]-N-methylhydrazine-1-carbothioamide
0.05 mM, 30.0% inhibition, 23°C, pH 5.5
(2E)-2-[2-(4-bromophenoxy)-1-(4-fluorophenyl)ethylidene]-N-phenylhydrazine-1-carbothioamide
0.05 mM, 35.0% inhibition, 23°C, pH 5.5
(2E)-2-[2-(4-bromophenoxy)-1-(4-fluorophenyl)ethylidene]hydrazine-1-carbothioamide
0.05 mM, 38.7% inhibition, 23°C, pH 5.5
(2E)-2-[2-(4-bromophenoxy)-1-(4-methoxyphenyl)ethylidene]-N-methylhydrazine-1-carbothioamide
0.05 mM, 29.8% inhibition, 23°C, pH 5.5
(2E)-2-[2-(4-bromophenoxy)-1-(4-methoxyphenyl)ethylidene]-N-phenylhydrazine-1-carbothioamide
0.05 mM, 42.8% inhibition, 23°C, pH 5.5
(2E)-2-[2-(4-bromophenoxy)-1-(4-methoxyphenyl)ethylidene]hydrazine-1-carbothioamide
0.05 mM, 70.9% inhibition, 23°C, pH 5.5
(2E)-2-[2-(4-bromophenoxy)-1-(4-methylphenyl)ethylidene]hydrazine-1-carbothioamide
0.05 mM, 67.6% inhibition, 23°C, pH 5.5
(2E)-2-[2-(4-bromophenoxy)-1-(naphthalen-1-yl)ethylidene]hydrazine-1-carbothioamide
0.05 mM, 73.6% inhibition, 23°C, pH 5.5
(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
(2S)-N-(1-cyano-1-methylethyl)-3-phenyl-2-(phenylformamido)propanamide
i.e. Neq0410, inhibition is enthalpy driven with a clear detrimental contribution of the entropy difference to the free binding energy
(2S)-N-(1-cyanocyclopropyl)-3-phenyl-2-(phenylformamido)propanamide
i.e. Neq0570, inhibition is enthalpy driven with a clear detrimental contribution of the entropy difference to the free binding energy
(2S)-N-(cyanomethyl)-3-phenyl-2-(phenylformamido)-propanamide
i.e. Neq0409, inhibition is enthalpy driven with a clear detrimental contribution of the entropy difference to the free binding energy
(2Z)-2-(2-[([1,1'-biphenyl]-3-yl)oxy]-1-(4-bromophenyl)ethylidene)hydrazine-1-carbothioamide
0.05 mM, 65.4% inhibition, 23°C, pH 5.5
(2Z)-2-(2-[([1,1'-biphenyl]-4-yl)oxy]-1-(4-bromophenyl)ethylidene)hydrazine-1-carbothioamide
0.05 mM, 63.7% inhibition, 23°C, pH 5.5
(2Z)-2-[1-(4-bromophenyl)-2-(2,3-dichlorophenoxy)ethylidene]hydrazine-1-carbothioamide
0.05 mM, 81.8% inhibition, 23°C, pH 5.5
(2Z)-2-[1-(4-bromophenyl)-2-(2-chlorophenoxy)ethylidene]hydrazine-1-carbothioamide
0.05 mM, 58.9% inhibition, 23°C, pH 5.5
(2Z)-2-[1-(4-bromophenyl)-2-(3,4-dichlorophenoxy)ethylidene]hydrazine-1-carbothioamide
0.05 mM, 99.1% inhibition, 23°C, pH 5.5
(2Z)-2-[1-(4-bromophenyl)-2-(3-chloro-4-fluorophenoxy)ethylidene]hydrazine-1-carbothioamide
0.05 mM, 93.7% inhibition, 23°C, pH 5.5
(2Z)-2-[1-(4-bromophenyl)-2-(3-chlorophenoxy)ethylidene]hydrazine-1-carbothioamide
0.05 mM,51.8 % inhibition, 23°C, pH 5.5
(2Z)-2-[1-(4-bromophenyl)-2-(3-methoxyphenoxy)ethylidene]hydrazine-1-carbothioamide
0.05 mM, 62.8% inhibition, 23°C, pH 5.5
(2Z)-2-[1-(4-bromophenyl)-2-(4-chlorophenoxy)ethylidene]hydrazine-1-carbothioamide
0.05 mM, 76.3% inhibition, 23°C, pH 5.5
(2Z)-2-[1-(4-bromophenyl)-2-(4-ethylphenoxy)ethylidene]hydrazine-1-carbothioamide
0.05 mM, 75.1% inhibition, 23°C, pH 5.5
(2Z)-2-[1-(4-bromophenyl)-2-(4-fluorophenoxy)ethylidene]hydrazine-1-carbothioamide
0.05 mM, 84.0% inhibition, 23°C, pH 5.5
(2Z)-2-[1-(4-bromophenyl)-2-(4-iodophenoxy)ethylidene]hydrazine-1-carbothioamide
0.05 mM, 63.3% inhibition, 23°C, pH 5.5
(2Z)-2-[1-(4-bromophenyl)-2-(4-methoxyphenoxy)ethylidene]hydrazine-1-carbothioamide
0.05 mM, 75.8% inhibition, 23°C, pH 5.5
(2Z)-2-[1-(4-bromophenyl)-2-(4-tert-butylphenoxy)ethylidene]hydrazine-1-carbothioamide
0.05 mM, 85.3% inhibition, 23°C, pH 5.5
(2Z)-2-[1-(4-bromophenyl)-2-phenoxyethylidene]hydrazine-1-carbothioamide
0.05 mM, 61.8% inhibition, 23°C, pH 5.5
(2Z)-2-[1-(4-bromophenyl)-2-[(naphthalen-1-yl)oxy]ethylidene]hydrazine-1-carbothioamide
-
(2Z)-2-[1-(4-bromophenyl)-2-[(naphthalen-2-yl)oxy]ethylidene]hydrazine-1-carbothioamide
0.05 mM, 72.1% inhibition, 23°C, pH 5.5
(2Z)-2-[1-(4-bromophenyl)-2-[4-(propan-2-yl)phenoxy]ethylidene]hydrazine-1-carbothioamide
0.05 mM, 49.7% inhibition, 23°C, pH 5.5
(2Z)-2-[2-(3-bromophenoxy)-1-(4-bromophenyl)ethylidene]hydrazine-1-carbothioamide
0.05 mM, 81.3% inhibition, 23°C, pH 5.5
(5R)-5-(3,4-difluorophenyl)-3-[2-[(5S)-5-(furan-2-yl)-3-(4-methylphenyl)-4,5-dihydro-1H-pyrazol-1-yl]-2-oxoethyl]-5-methylimidazolidine-2,4-dione
in the epimastigote form, the inhibitor does not show trypanocidal effects, against bloodstream trypomastigotes the LC50 value is greater than 0.250 mM
1-[(5R)-3,5-di(furan-2-yl)-4,5-dihydro-1H-pyrazol-1-yl]-2-([5-[(5S)-5-methyl-4,5,6,7-tetrahydro-1-benzothiophen-2-yl]-1,3,4-oxadiazol-2-yl]sulfanyl)ethanone
in the epimastigote form, the inhibitor does not show trypanocidal effects, against bloodstream trypomastigotes the LC50 value is greater than 0.250 mM
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-amino-6-methyl-3-([2-[(5R)-3-(naphthalen-2-yl)-5-phenyl-4,5-dihydro-1H-pyrazol-1-yl]-2-oxoethyl]sulfanyl)-1,2,4-triazin-5(4H)-one
shows trypanocidal activity, promising structure in the search for new agents to treat Chagas disease
benzoyl-Tyr-Ala-chloromethyl ketone
first quantum mechanics/molecular mechanics studies show that benzoyl-Tyr-Ala-chloromethyl ketone is a good candidate for the development of a proper inhibitor of cruzain, which in turn can be used in the treatment of Chagas desease
chagasin
computational protocol allows the identification and prediction of thermodynamics binding energy parameters for cruzipain/chagasin-like heterodimers
-
N-(1-cyanocyclopropyl)-Nalpha-(phenylacetyl)-L-phenylalaninamide
pKi: 6.4 (-log(Ki/M))
N-(1-cyanocyclopropyl)-Nalpha-[(4-fluorophenyl)acetyl]-L-phenylalaninamide
pKi: 6.3 (-log(Ki/M))
N-(1-cyanocyclopropyl)-Nalpha-[(4-hydroxyphenyl)acetyl]-L-phenylalaninamide
pKi: 7.0 (-log(Ki/M))
N-(1-cyanocyclopropyl)-Nalpha-[(4-iodophenyl)acetyl]-L-phenylalaninamide
pKi: 7.2 (-log(Ki/M))
N-(1-cyanocyclopropyl)-Nalpha-[(4-methylphenyl)acetyl]-L-phenylalaninamide
pKi: 6.6 (-log(Ki/M))
N-(1-cyanocyclopropyl)-Nalpha-[(pyridin-4-yl)acetyl]-L-phenylalaninamide
pKi: 5.9 (-log(Ki/M))
N-(1-cyanocyclopropyl)-Nalpha-[[4-(trifluoromethyl)phenyl]acetyl]-L-phenylalaninamide
pKi: 6.6 (-log(Ki/M))
N-(4-([(2Z)-2-(4-bromophenyl)-2-(2-carbamothioylhydrazinylidene)ethyl]oxy)phenyl)acetamide
0.05 mM, 80.7% inhibition, 23°C, pH 5.5
N-[4-methyl-3-(piperidin-1-ylsulfonyl)phenyl]-4-oxo-4-(3-phenyl-4,5-dihydro-1H-pyrazol-1-yl)butanamide
weak inhibitor shows trypanocidal activity, against bloodstream trypomastigotes the LC50 value is greater than 0.250 mM
Nalpha-[(4-bromophenyl)acetyl]-N-(1-cyanocyclopropyl)-L-phenylalaninamide
pKi: 6.9 (-log(Ki/M))
Nalpha-[(4-chlorophenyl)acetyl]-N-(1-cyanocyclopropyl)-L-phenylalaninamide
pKi: 7.2 (-log(Ki/M))
(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
-
-
(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
-
-
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 inhibition 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
L-trans-epoxysuccinylleucylamido(4-guanidino)butane
strong inhibitor
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
(2E)-2-[1-([1,1'-biphenyl]-4-yl)-2-(4-bromophenoxy)ethylidene]hydrazine-1-carbothioamide
0.05 mM, 11.8% inhibition, 23°C, pH 5.5
(2E)-2-[1-([1,1'-biphenyl]-4-yl)-2-(4-bromophenoxy)ethylidene]hydrazine-1-carbothioamide
0.05 mM, 88.9% inhibition, 23°C, pH 5.5
Nalpha-[(3-chlorophenyl)acetyl]-N-(1-cyanocyclopropyl)-L-phenylalaninamide
pKi: 6,4 (-log(Ki/M))
Nalpha-[(3-chlorophenyl)acetyl]-N-(1-cyanocyclopropyl)-L-phenylalaninamide
pKi: 6.6 (-log(Ki/M))
L-kininogen
high molecular weight kininogen, inhibition decreases 10fold in presence of 0.1 mM heparan sulfate
-
trans-epoxysuccinyl-L-leucylamido-(4-guanidino)butane
-
irreversible inhibitor
additional information
apolar substituents or halogen atom substitution at the aryl position improved cruzain inhibition and antiparasitic activity in comparison to unsubstituted thiosemicarbazone
-
additional information
-
apolar substituents or halogen atom substitution at the aryl position improved cruzain inhibition and antiparasitic activity in comparison to unsubstituted thiosemicarbazone
-
additional information
nitrile-based inhibitors are efficient inhibitors of cruzain that bind by forming a covalent bond with this enzyme
-
additional information
the AS2 site as a target for the design of cruzain inhibitors is limited
-
additional information
-
AM1 semi-empirical molecular modeling studies analysing cruzain inhibitory activity, overview
-
additional information
-
synthesis and inhibitory effects against cruzipaon of a series of thirty-three chalcone and seven hydrazide derivatives, overview
-
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
-
0.01% (v/v) of Triton X-100 does not interfere with enzyme activity
-
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
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
0.038
benzyloxycarbonyl-Arg-Ala-7-amido-4-methylcoumarin
pH 7.5, 25°C, wild-type enzyme
0.163
benzyloxycarbonyl-Arg-Ala-7-amido-4-methylcoumarin
pH 7.5, 25°C, mutant enzyme E208A
0.0029
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 8.5, 25°C, wild-type enzyme
0.0036
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 9.0, 25°C, wild-type enzyme
0.0037
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 7.5, 25°C, wild-type enzyme
0.0041
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 9.5, 25°C, wild-type enzyme
0.0043
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 8.0, 25°C, wild-type enzyme
0.0046
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 7.0, 25°C, wild-type enzyme
0.0066
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 6.5, 25°C, wild-type enzyme
0.011
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 6.0, 25°C, wild-type enzyme
0.012
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 9.9, 25°C, wild-type enzyme
0.017
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 5.5, 25°C, wild-type enzyme
0.028
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 5.0, 25°C, wild-type enzyme
0.045
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 7.5, 25°C, mutant enzyme E208A
0.056
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 4.4, 25°C, wild-type enzyme
0.068
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 4.1, 25°C, wild-type enzyme
0.078
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 3.5, 25°C, wild-type enzyme
0.00054
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 9.0, 25°C, wild-type enzyme
0.00056
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 8.5, 25°C, wild-type enzyme
0.00061
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 8.0, 25°C, wild-type enzyme
0.00062
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 7.5, 25°C, wild-type enzyme
0.00068
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 7.0, 25°C, wild-type enzyme
0.0007
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 6.5, 25°C, wild-type enzyme
0.00077
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 9.5, 25°C, wild-type enzyme
0.00087
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 5.6, 25°C, wild-type enzyme
0.00088
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 6.0, 25°C, wild-type enzyme
0.0013
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 5.0, 25°C, wild-type enzyme
0.0016
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 7.5, 25°C, mutant enzyme E208A
0.0019
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 4.1, 25°C, wild-type enzyme
0.0025
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 4.4, 25°C, wild-type enzyme
0.0052
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 3.5, 25°C, wild-type enzyme
0.0003
2-aminobenzoic acid-KLRFSKQ-N-(2,4-dinitrophenyl)ethylenediamine
recombinant form without C-terminal extension
0.001
2-aminobenzoic acid-KLRFSKQ-N-(2,4-dinitrophenyl)ethylenediamine
-
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-Phe-Arg-7-amido-4-methylcoumarin
recombinant form without C-terminal extension
-
0.0008
benzyloxycarbonyl-Phe-Arg-aminomethyl coumarin
truncated enzyme
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
0.017
benzyloxycarbonyl-Arg-Ala-7-amido-4-methylcoumarin
pH 7.5, 25°C, mutant enzyme E208A
0.89
benzyloxycarbonyl-Arg-Ala-7-amido-4-methylcoumarin
pH 7.5, 25°C, wild-type enzyme
0.1
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 3.5, 25°C, wild-type enzyme
0.27
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 7.5, 25°C, mutant enzyme E208A
0.4
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 4.1, 25°C, wild-type enzyme
0.7
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 4.4, 25°C, wild-type enzyme
1.9
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 5.0, 25°C, wild-type enzyme
3.7
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 5.5, 25°C, wild-type enzyme
5.8
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 9.5, 25°C, wild-type enzyme
5.8
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 9.9, 25°C, wild-type enzyme
5.9
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 6.0, 25°C, wild-type enzyme
6.9
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 6.5, 25°C, wild-type enzyme
6.9
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 8.5, 25°C, wild-type enzyme
7.1
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 9.0, 25°C, wild-type enzyme
7.2
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 7.5, 25°C, wild-type enzyme
7.4
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 7.0, 25°C, wild-type enzyme
8
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 8.0, 25°C, wild-type enzyme
13
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 3.5, 25°C, wild-type enzyme
13
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 9.5, 25°C, wild-type enzyme
13
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 4.1, 25°C, wild-type enzyme
13.5
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 6.5, 25°C, wild-type enzyme
13.5
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 6.0, 25°C, wild-type enzyme
13.6
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 5.6, 25°C, wild-type enzyme
14
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 7.0, 25°C, wild-type enzyme
14
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 9.0, 25°C, wild-type enzyme
14
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 4.4, 25°C, wild-type enzyme
14.1
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 5.0, 25°C, wild-type enzyme
15
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 8.5, 25°C, wild-type enzyme
16
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 8.0, 25°C, wild-type enzyme
17
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 7.5, 25°C, wild-type enzyme
21
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 7.5, 25°C, mutant enzyme E208A
0.0683
2-aminobenzoic acid-KLRFSKQ-N-(2,4-dinitrophenyl)ethylenediamine
recombinant form without C-terminal extension
0.08
2-aminobenzoic acid-KLRFSKQ-N-(2,4-dinitrophenyl)ethylenediamine
-
0.025
2-aminobenzoyl-LGMISLMKRPQ-N-(2,4-dinitrophenyl)ethylenediamine
-
0.0583
2-aminobenzoyl-LGMISLMKRPQ-N-(2,4-dinitrophenyl)ethylenediamine
with 0.06 mM heparan sulfate
0.055
benzoyl-Phe-Arg-7-amido-4-methylcoumarin
recombinant form without C-terminal extension
-
2.16
benzyloxycarbonyl-Phe-Arg-aminomethyl coumarin
truncated enzyme
kcat/KM VALUE [1/mMs-1]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.2
benzyloxycarbonyl-Arg-Ala-7-amido-4-methylcoumarin
pH 7.5, 25°C, mutant enzyme E208A
23
benzyloxycarbonyl-Arg-Ala-7-amido-4-methylcoumarin
pH 7.5, 25°C, wild-type enzyme
1.2
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 3.5, 25°C, wild-type enzyme
5.9
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 4.1, 25°C, wild-type enzyme
6
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 7.5, 25°C, mutant enzyme E208A
13
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 4.4, 25°C, wild-type enzyme
54
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 6.0, 25°C, wild-type enzyme
70
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 5.0, 25°C, wild-type enzyme
100
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 6.5, 25°C, wild-type enzyme
150
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 9.5, 25°C, wild-type enzyme
160
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 7.0, 25°C, wild-type enzyme
190
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 8.0, 25°C, wild-type enzyme
190
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 7.5, 25°C, wild-type enzyme
200
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 9.0, 25°C, wild-type enzyme
220
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 5.5, 25°C, wild-type enzyme
240
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 8.5, 25°C, wild-type enzyme
480
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 9.9, 25°C, wild-type enzyme
250
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 3.5, 25°C, wild-type enzyme
560
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 4.4, 25°C, wild-type enzyme
680
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 4.1, 25°C, wild-type enzyme
1100
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 5.0, 25°C, wild-type enzyme
1500
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 6.0, 25°C, wild-type enzyme
1500
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 9.5, 25°C, wild-type enzyme
1600
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 5.6, 25°C, wild-type enzyme
1900
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 6.5, 25°C, wild-type enzyme
2100
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 7.0, 25°C, wild-type enzyme
2600
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 8.0, 25°C, wild-type enzyme
2600
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 9.0, 25°C, wild-type enzyme
2700
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 7.5, 25°C, wild-type enzyme
2700
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 8.5, 25°C, wild-type enzyme
13000
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 7.5, 25°C, mutant enzyme E208A
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.018
propeptide of cruzipain
-
at pH 6.5 the propeptide of cruzipain inactivates cruzipain competitively
-
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.0006
(2E)-2-[1-([1,1'-biphenyl]-4-yl)-2-(4-bromophenoxy)ethylidene]hydrazine-1-carbothioamide
Trypanosoma cruzi
23°C, pH 5.5
0.000008
(2Z)-2-[1-(4-bromophenyl)-2-(3,4-dichlorophenoxy)ethylidene]hydrazine-1-carbothioamide
Trypanosoma cruzi
23°C, pH 5.5
0.00007
(2Z)-2-[1-(4-bromophenyl)-2-(3-chloro-4-fluorophenoxy)ethylidene]hydrazine-1-carbothioamide
Trypanosoma cruzi
23°C, pH 5.5
0.0004
(2Z)-2-[1-(4-bromophenyl)-2-(4-fluorophenoxy)ethylidene]hydrazine-1-carbothioamide
Trypanosoma cruzi
23°C, pH 5.5
0.05035
(5R)-5-(3,4-difluorophenyl)-3-[2-[(5S)-5-(furan-2-yl)-3-(4-methylphenyl)-4,5-dihydro-1H-pyrazol-1-yl]-2-oxoethyl]-5-methylimidazolidine-2,4-dione
Trypanosoma cruzi
23°C, pH 6.8
0.08437
1-[(5R)-3,5-di(furan-2-yl)-4,5-dihydro-1H-pyrazol-1-yl]-2-([5-[(5S)-5-methyl-4,5,6,7-tetrahydro-1-benzothiophen-2-yl]-1,3,4-oxadiazol-2-yl]sulfanyl)ethanone
Trypanosoma cruzi
23°C, pH 6.6
0.05623
4-amino-6-methyl-3-([2-[(5R)-3-(naphthalen-2-yl)-5-phenyl-4,5-dihydro-1H-pyrazol-1-yl]-2-oxoethyl]sulfanyl)-1,2,4-triazin-5(4H)-one
Trypanosoma cruzi
23°C, pH 6.7
1.41
N-[4-methyl-3-(piperidin-1-ylsulfonyl)phenyl]-4-oxo-4-(3-phenyl-4,5-dihydro-1H-pyrazol-1-yl)butanamide
Trypanosoma cruzi
23°C, pH 6.5
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
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
-
-
0.016
(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
0.02 - 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
0.005
(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
0.1
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
-
-
0.073
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
Nalpha-[(2R,3E)-2-benzyl-4-(phenylsulfonyl)but-3-enoyl]-N-[(4-methylpiperazin-1-yl)carbonyl]-L-phenylalaninamide
Trypanosoma cruzi
-
-
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
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
4.5
-
hydrolysis of 2-aminobenzoyl-FRA-(2,4-dinitrophenyl)-epsilon-NH2-lysine-OH
6 - 7
-
hydrolysis of 2-aminobenzoyl-FRA-(2,4-dinitrophenyl)-epsilon-NH2-lysine-NH2
6.5
6.8
7.6
additional information
6.5
-
assay at room temperature, 5 min, 0.64 nM cruzain, 50 mM sodium phosphate, 100 mM sodium chloride, 5 mM EDTA
8
-
30 min, 50 mM Tris-acetate buffer, 0.3 mM Bz-Pro-Phe-Arg-pNA, 10 mM beta-mercaptoethanol
additional information
substrates placing hydrophobic residues in the specificity pocket are cleaved at a broader pH range than hydrophilic substrates
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
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
LITERATURE
37
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
ORGANISM
COMMENTARY
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
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
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
-
membrane bound compartments between nucleus and kinetoplast
-
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
metabolism
the enzyme is expressed by the protozoan parasite Trypanosoma cruzi during Chagas disease infection
physiological function
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
cruzain is the major cysteine protease involved in the survival of the parasite Trypanosoma cruzi
physiological function
key enzyme for the survival and propagation of this parasite lifecycle
physiological function
the enzyme is the etiological agent of Chagas disease
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
UNIPROT
ENTRY NAME
ORGANISM
NO. OF AA
NO. OF TRANSM. HELICES
MOLECULAR WEIGHT[Da]
SOURCE
SEQUENCE
LOCALIZATION PREDICTION
The reliability class of the localization prediction ranges from 1 (very reliable) to 5 (not reliable).
The reliability class of the localization prediction ranges from 1 (very reliable) to 5 (not reliable). CYSP_TRYCR
467
1
49836
Swiss-Prot
Secretory Pathway (Reliability: 1)
PDB
SCOP
CATH
UNIPROT
ORGANISM
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
12000
-
x * 12000, non-adsorbed (to concanavalin A-Sepharose) cruzipain isoform, SDS-PAGE
50000
SUBUNIT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
?
-
x * 12000, non-adsorbed (to concanavalin A-Sepharose) cruzipain isoform, SDS-PAGE
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
glycoprotein
glycoprotein
N-glycosylation at Asn254, no O-glycosylation or phosphorylation
glycoprotein
-
presence of sialic acid in N-linked oligosaccharide chains and O-linked N-acetylglucosamine
glycoprotein
-
sulfated high-mannose type oligosaccharides, lactosaminic glycans and fucosylated oligosaccharides
glycoprotein
-
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
CRYSTALLIZATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
cruzain crystals diffract to 1.2 A resolution, yielding two novel cruzain structures: apocruzain and cruzain bound to the reversible covalent inhibitor S-methyl thiomethanesulfonate. Mass-spectrometric experiments confirm the presence of a methylthiol group attached to the catalytic cysteine
bound to benzoyl-Arg-Ala-fluoromethyl ketone and benzoyl-Tyr-Ala-fluoromethyl ketone, hanging drop vapor diffusion method
enzyme lacking the C-terminal domain, complexed with benzyloxycarbonyl-Phe-Ala-fluoromethylketone
PROTEIN VARIANTS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
E208A
the mutant enzyme recognizes benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin less effectively than wild-type cruzain does, turnover of the substrate is comparable, suggesting that once bound, mutant cruzain processes benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarinat rates similar to that of the wild-type enzyme. Diminutions by 300fold and 200fold in the kcat/Km values of benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin and benzyloxycarbonyl-Arg-Ala-7-amido-4-methylcoumarin, respectively, are observed for the E208A mutant cruzain compared to that of the wild type, suggesting that ion pairing between Glu208 and P2 Arg is essential for recognition of these substrates. This is also reflected in values of Km, which are increased for benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin (10fold) and benzyloxycarbonyl-Arg-Ala-7-amido-4-methylcoumarin (4fold)
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
TEMPERATURE STABILITY
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
5 - 37
inactivation at pH 2.25 and pH 10 increases with increasing temperature
GENERAL STABILITY
ORGANISM
UNIPROT
LITERATURE
STORAGE STABILITY
ORGANISM
UNIPROT
LITERATURE
PURIFICATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
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
-
APPLICATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
medicine
drug development
-
cruzipain is an attractive target for the development of novel trypanocidal drugs
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
medicine
cruzain is a primary cysteine protease expressed by the protozoan parasite Trypanosoma cruzi during Chagas disease infection, and thus, the development of inhibitors of this protein is a promising target for designing an effective therapy against the disease
medicine
cruzipain inhibition is a chemotherapeutic approach for Chagas disease because of its trypanocidal activity and due to the inhibitory effect on TGF-beta activation
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TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
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Expression in insect cells of active mature cruzipain from Trypanosoma cruzi, containing its C-terminal domain
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Trypanosoma cruzi (Q598P5), Trypanosoma cruzi
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Trypanosoma cruzi (Q598P5), Trypanosoma cruzi
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Trypanosoma cruzi (Q598P5), Trypanosoma cruzi
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Some kinetic properties of a cysteine proteinase (cruzipain) from Trypanosoma cruzi
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Trypanosoma cruzi (Q598P5)
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Cruzipain, the major cysteine proteinase from the protozoan parasite Trypanosoma cruzi
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Trypanosoma cruzi (Q598P5), Trypanosoma cruzi
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Trypanosoma cruzi (Q598P5)
-
Eakin, A.E.; McGrath, M.E.; McKerrow, J.H.; Fletterick, R.J.; Craik, C.S.
Production of crystallizable cruzain, the major cysteine protease from Trypanosoma cruzi
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Trypanosoma cruzi (Q598P5), Trypanosoma cruzi
Gillmor, S.A.; Craik, C.S.; Fletterick, R.J.
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1603-1611
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Trypanosoma cruzi (Q598P5), Trypanosoma cruzi
Judice, W.A.; Cezari, M.H.; Lima, A.P.; Scharfstein, J.; Chagas, J.R.; Tersariol, I.L.; Juliano, M.A.; Juliano, L.
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268
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Trypanosoma cruzi (Q598P5), Trypanosoma cruzi
Lima, A.P.C.A.; Almeida, P.C.; Tersariol, I.L.S.; Schmitz, V.; Schmaier, A.H.; Juliano, L.; Hirata, I.Y.; Muller-Esterl, W.; Chagas, J.R.; Scharfstein, J.
Heparan sulfate modulates kinin release by Trypanosoma cruzi through the activity of cruzipain
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277
5875-5881
2002
Trypanosoma cruzi (Q598P5), Trypanosoma cruzi
McGrath, M.E.; Eakin, A.E.; Engel, J.C.; McKerrow, J.H.; Craik, C.C.; Fletterick, R.J.
The crystal structure of cruzain: a therapeutic target for Chagas' disease
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247
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Trypanosoma cruzi (Q598P5), Trypanosoma cruzi
Ramos, A.M.; Duschak, V.G.; Gerez de Burgos, N.M.; Barboza, M.; Remedi, M.S.; Vides, M.A.; Chiabrando, G.A.
Trypanosoma cruzi: cruzipain and membrane-bound cysteine proteinase isoform(s) interacts with human alpha2-macroglobulin and pregnancy zone protein
Exp. Parasitol.
100
121-130
2002
Trypanosoma cruzi (Q598P5), Trypanosoma cruzi
Salvati, L.; Mattu, M.; Polticelli, F.; Tiberi, F.; Gradoni, L.; Venturini, G.; Bolognesi, M.; Ascenzi, P.
Modulation of the catalytic activity of cruzipain, the major cysteine proteinase from Trypanosoma cruzi, by temperature and pH
Eur. J. Biochem.
268
3253-3258
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Trypanosoma cruzi (Q598P5), Trypanosoma cruzi
Schnapp, A.R.; Eickhoff, C.S.; Sizemore, D.; Curtiss, R.3rd.; Hoft, D.F.
Cruzipain induces both mucosal and systemic protection against Trypanosoma cruzi in mice
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70
5065-5074
2002
Trypanosoma cruzi (Q598P5), Trypanosoma cruzi
Sterin-Borda, L.; Giordanengo, L.; Joensen, L.; Gea, S.
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33
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Trypanosoma cruzi (Q598P5), Trypanosoma cruzi
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The high stability of cruzipain against pH-induced inactivation is not dependent on its C-terminal domain
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469
29-32
2000
Trypanosoma cruzi (Q598P5)
Cazzulo, J.J.; Martinez, J.; Parodi, A.J.; Wernstedt, C.; Hellman, U.
On the post-translational modifications at the C-terminal domain of the major cysteine proteinase (cruzipain) from Trypanosoma cruzi
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79
411-416
1992
Trypanosoma cruzi (Q598P5), Trypanosoma cruzi
Aoki, M.P.; Guinazu, N.L.; Pellegrini, A.V.; Gotoh, T.; Masih, D.T.; Gea, S.
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286
C206-C212
2004
Trypanosoma cruzi
Polticelli, F.; Zaini, G.; Bolli, A.; Antonini, G.; Gradoni, L.; Ascenzi, P.
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44
2781-2789
2005
Trypanosoma cruzi
Chiyanzu, I.; Hansell, E.; Gut, J.; Rosenthal, P.J.; McKerrow, J.H.; Chibale, K.
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13
3527-3530
2003
Trypanosoma cruzi
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15
121-123
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Trypanosoma cruzi
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271
1046-1053
2004
Trypanosoma cruzi
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Trypanosoma cruzi: partial characterization of minor cruzipain isoforms non-adsorbed to concanavalin A-Sepharose
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104
122-130
2003
Trypanosoma cruzi
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Structural analysis of the N-glycans of the major cysteine proteinase of Trypanosoma cruzi. Identification of sulfated high-mannose type oligosaccharides
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272
3803-3815
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Trypanosoma cruzi
Barboza, M.; Duschak, V.G.; Cazzulo, J.J.; de Lederkremer, R.M.; Couto, A.S.
Presence of sialic acid in N-linked oligosaccharide chains and O-linked N-acetylglucosamine in cruzipain, the major cysteine proteinase of Trypanosoma cruzi
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127
69-72
2003
Trypanosoma cruzi
Berasain, P.; Carmona, C.; Frangione, B.; Cazzulo, J.J.; Goni, F.
Specific cleavage sites on human IgG subclasses by cruzipain, the major cysteine proteinase from Trypanosoma cruzi
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130
23-29
2003
Trypanosoma cruzi
Stempin, C.C.; Garrido, V.V.; Dulgerian, L.R.; Cerban, F.M.
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106
119-127
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Trypanosoma cruzi
Reis, F.C.; Costa, T.F.; Sulea, T.; Mezzetti, A.; Scharfstein, J.; Broemme, D.; Menard, R.; Lima, A.P.
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274
1224-1234
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Trypanosoma cruzi
dos Reis, F.C.; Judice, W.A.; Juliano, M.A.; Juliano, L.; Scharfstein, J.; Lima, A.P.
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259
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Trypanosoma cruzi
Scharfstein, J.; Monteiro, A.C.; Schmitz, V.; Svensjoe, E.
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389
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Trypanosoma cruzi
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Synthesis of macrocyclic trypanosomal cysteine protease inhibitors
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18
5860-5863
2008
Trypanosoma brucei rhodesiense, Trypanosoma cruzi
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16
10236-10243
2008
Trypanosoma cruzi
Porcal, W.; Hernandez, P.; Boiani, L.; Boiani, M.; Ferreira, A.; Chidichimo, A.; Cazzulo, J.J.; Olea-Azar, C.; Gonzalez, M.; Cerecetto, H.
New trypanocidal hybrid compounds from the association of hydrazone moieties and benzofuroxan heterocycle
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16
6995-7004
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Trypanosoma cruzi, Trypanosoma cruzi Tulahuen 2
Romeiro, N.C.; Aguirre, G.; Hernandez, P.; Gonzalez, M.; Cerecetto, H.; Aldana, I.; Perez-Silanes, S.; Monge, A.; Barreiro, E.J.; Lima, L.M.
Synthesis, trypanocidal activity and docking studies of novel quinoxaline-N-acylhydrazones, designed as cruzain inhibitors candidates
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17
641-652
2009
Trypanosoma cruzi, Trypanosoma cruzi Tulahuen 2
Elias, C.G.; Pereira, F.M.; Dias, F.A.; Silva, T.L.; Lopes, A.H.; dAvila-Levy, C.M.; Branquinha, M.H.; Santos, A.L.
Cysteine peptidases in the tomato trypanosomatid Phytomonas serpens: influence of growth conditions, similarities with cruzipain and secretion to the extracellular environment
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120
343-352
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Trypanosoma cruzi, Trypanosoma cruzi Dm28c
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The role of conserved residues of chagasin in the inhibition of cysteine peptidases
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Trypanosoma cruzi
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All Trypanosoma cruzi developmental forms present lysosome-related organelles
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Trypanosoma cruzi, Trypanosoma cruzi Y
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Sulfates are main targets of immune responses to cruzipain and are involved in heart damage in BALB/c immunized mice
Int. Immunol.
20
461-470
2008
Trypanosoma cruzi, Trypanosoma cruzi Tulahuen 2
Brak, K.; Doyle, P.S.; McKerrow, J.H.; Ellman, J.A.
Identification of a new class of nonpeptidic inhibitors of cruzain
J. Am. Chem. Soc.
130
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Trypanosoma cruzi (P25779), Trypanosoma cruzi
Fricker, S.P.; Mosi, R.M.; Cameron, B.R.; Baird, I.; Zhu, Y.; Anastassov, V.; Cox, J.; Doyle, P.S.; Hansell, E.; Lau, G.; Langille, J.; Olsen, M.; Qin, L.; Skerlj, R.; Wong, R.S.; Santucci, Z.; McKerrow, J.H.
Metal compounds for the treatment of parasitic diseases
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102
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Trypanosoma cruzi
Fampa, P.; Lisboa, C.V.; Jansen, A.M.; Santos, A.L.; Ramirez, M.I.
Protease expression analysis in recently field-isolated strains of Trypanosoma cruzi: a heterogeneous profile of cysteine protease activities between TC I and TC II major phylogenetic groups
Parasitology
135
1093-1100
2008
Trypanosoma cruzi
Pereira, F.M.; Elias, C.G.; dAvila-Levy, C.M.; Branquinha, M.H.; Santos, A.L.
Cysteine peptidases in Herpetomonas samuelpessoai are modulated by temperature and dimethylsulfoxide-triggered differentiation
Parasitology
136
45-54
2009
Trypanosoma cruzi, Trypanosoma cruzi Dm28c
Cazorla, S.I.; Frank, F.M.; Becker, P.D.; Corral, R.S.; Guzman, C.A.; Malchiodi, E.L.
Prime-boost immunization with cruzipain co-administered with MALP-2 triggers a protective immune response able to decrease parasite burden and tissue injury in an experimental Trypanosoma cruzi infection model
Vaccine
26
1999-2009
2008
Trypanosoma cruzi, Trypanosoma cruzi RA
Pizzo, C.; Saiz, C.; Talevi, A.; Gavernet, L.; Palestro, P.; Bellera, C.; Blanch, L.B.; Benitez, D.; Cazzulo, J.J.; Chidichimo, A.; Wipf, P.; Mahler, S.G.
Synthesis of 2-hydrazolyl-4-thiazolidinones based on multicomponent reactions and biological evaluation against Trypanosoma cruzi
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77
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2011
Trypanosoma cruzi
Borchhardt, D.; Mascarello, A.; Chiaradia, L.; Nunes, R.; Oliva, G.; Yunes, R.; Andricopulo, A.
Biochemical evaluation of a series of synthetic chalcone and hydrazide derivatives as novel inhibitors of cruzain from Trypanosoma cruzi
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21
142-150
2010
Trypanosoma cruzi
-
Trossini, G.; Malvezzi, A.; Amaral, A.; Rangel-Yagui, C.; Izidoro, M.; Cezari, M.; Juliano, L.; Chin, C.; Menezes, C.; Ferreira, E.
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25
62-67
2010
Trypanosoma cruzi
Trossini, G.; Chin, C.; de Souza Menezes, C.; Ferreira, E.
Molecular modeling suggests cruzain specificity for peptide primaquine prodrugs
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7
528-533
2010
Trypanosoma cruzi
-
Acosta, D.M.; Soprano, L.L.; Ferrero, M.; Landoni, M.; Esteva, M.I.; Couto, A.S.; Duschak, V.G.
A striking common O-linked N-acetylglucosaminyl moiety between cruzipain and myosin
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33
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2011
Trypanosoma cruzi
Doyle, P.S.; Zhou, Y.M.; Hsieh, I.; Greenbaum, D.C.; McKerrow, J.H.; Engel, J.C.
The Trypanosoma cruzi protease cruzain mediates immune evasion
PLoS Pathog.
7
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2011
Trypanosoma cruzi
Merlino, A.; Benitez, D.; Campillo, N.; Pez, J.; Tinoco, L.; Gonzlez, M.; Cerecetto, H.
Amidines bearing benzofuroxan or benzimidazole 1,3-dioxide core scaffolds as Trypanosoma cruzi-inhibitors: Structural basis for their interactions with cruzipain
MedChemComm
3
90-101
2012
Trypanosoma cruzi
-
Uehara, L.A.; Moreira, O.C.; Oliveira, A.C.; Azambuja, P.; Lima, A.P.; Britto, C.; dos Santos, A.L.; Branquinha, M.H.; dAvila-Levy, C.M.
Cruzipain promotes Trypanosoma cruzi adhesion to Rhodnius prolixus midgut
PLoS Negl. Trop. Dis.
6
e1958
2012
Trypanosoma cruzi, Trypanosoma cruzi Dm28c
Barbosa da Silva, E.; Dall, E.; Briza, P.; Brandstetter, H.; Ferreira, R.S.
Cruzain structures apocruzain and cruzain bound to S-methyl thiomethanesulfonate and implications for drug design
Acta Crystallogr. Sect. F
75
419-427
2019
Trypanosoma cruzi (P25779), Trypanosoma cruzi
Arafet, K.; Ferrer, S.; Moliner, V.
First quantum mechanics/molecular mechanics studies of the inhibition mechanism of cruzain by peptidyl halomethyl ketones
Biochemistry
54
3381-3391
2015
Trypanosoma cruzi (P25779), Trypanosoma cruzi
Zhai, X.; Meek, T.D.
Catalytic mechanism of cruzain from Trypanosoma cruzi as determined from solvent kinetic isotope effects of steady-state and pre-steady-state kinetics
Biochemistry
57
3176-3190
2018
Trypanosoma cruzi (P25779), Trypanosoma cruzi
Cianni, L.; Sartori, G.; Rosini, F.; De Vita, D.; Pires, G.; Lopes, B.R.; Leitao, A.; Burtoloso, A.C.B.; Montanari, C.A.
Leveraging the cruzain S3 subsite to increase affinity for reversible covalent inhibitors
Bioorg. Chem.
79
285-292
2018
Trypanosoma cruzi (P25779), Trypanosoma cruzi
Fabian, L.; Martini, M.F.; Sarduy, E.S.; Estrin, D.A.; Moglioni, A.G.
Evaluation of quinoxaline compounds as ligands of a site adjacent to S2 (AS2) of cruzain
Bioorg. Med. Chem. Lett.
29
2197-2202
2019
Trypanosoma cruzi (P25779)
Espindola, J.W.; Cardoso, M.V.; Filho, G.B.; Oliveira E Silva, D.A.; Moreira, D.R.; Bastos, T.M.; Simone, C.A.; Soares, M.B.; Villela, F.S.; Ferreira, R.S.; Castro, M.C.; Pereira, V.R.; Murta, S.M.; Sales Junior, P.A.; Romanha, A.J.; Leite, A.C.
Synthesis and structure-activity relationship study of a new series of antiparasitic aryloxyl thiosemicarbazones inhibiting Trypanosoma cruzi cruzain
Eur. J. Med. Chem.
101
818-835
2015
Trypanosoma cruzi (P25779), Trypanosoma cruzi
Reyes-Espinosa, F.; Juarez-Saldivar, A.; Palos, I.; Herrera-Mayorga, V.; Garcia-Perez, C.; Rivera, G.
In silico analysis of homologous heterodimers of cruzipain-chagasin from structural models built by homology
Int. J. Mol. Sci.
20
E1320
2019
Trypanosoma cruzi (P25779)
Herrera-Mayorga, V.; Lara-Ramirez, E.E.; Chacon-Vargas, K.F.; Aguirre-Alvarado, C.; Rodriguez-Paez, L.; Alcantara-Farfan, V.; Cordero-Martinez, J.; Nogueda-Torres, B.; Reyes-Espinosa, F.; Bocanegra-Garcia, V.; Rivera, G.
Structure-based virtual screening and in vitro evaluation of new Trypanosoma cruzi cruzain inhibitors
Int. J. Mol. Sci.
20
E1742
2019
Trypanosoma cruzi (P25779), Trypanosoma cruzi, Trypanosoma cruzi INC-5 (P25779)
Dos Santos, A.M.; Cianni, L.; De Vita, D.; Rosini, F.; Leitao, A.; Laughton, C.A.; Lameira, J.; Montanari, C.A.
Experimental study and computational modelling of cruzain cysteine protease inhibition by dipeptidyl nitriles
Phys. Chem. Chem. Phys.
20
24317-24328
2018
Trypanosoma cruzi (P25779)
Ferrao, P.M.; dAvila-Levy, C.M.; Araujo-Jorge, T.C.; Degrave, W.M.; Goncalves, A.d.a. .S.; Garzoni, L.R.; Lima, A.P.; Feige, J.J.; Bailly, S.; Mendonca-Lima, L.; Waghabi, M.C.
Cruzipain activates latent TGF-beta from host cells during T. cruzi invasion
PLoS ONE
10
e0124832
2015
Trypanosoma cruzi (P25779), Trypanosoma cruzi
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