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Information on EC 3.4.22.15 - cathepsin L

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EC Tree
     3 Hydrolases
         3.4 Acting on peptide bonds (peptidases)
             3.4.22 Cysteine endopeptidases
                3.4.22.15 cathepsin L
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UNIPROT: Q95PM0 not found.
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Word Map
The enzyme appears in viruses and cellular organisms
Reaction Schemes
similar to that of papain. As compared to cathepsin B, cathepsin L exhibits higher activity towards protein substrates, but has little activity on Z-Arg-Arg-NHMec, and no peptidyl-dipeptidase activity
Synonyms
cathepsin l, cathepsin l-like, cathepsin-l, human cathepsin l, cpl-1, cat l, cwp84, cathl, major excreted protein, smcl1, more
SYNONYM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
cathepsin L-like protein
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Aldrichina grahami cysteine proteinase
-
-
-
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major excreted protein
-
-
-
-
MEP
-
-
-
-
PDP
-
-
-
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progesterone-dependent protein
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-
-
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SMCL1
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-
-
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CAS REGISTRY NUMBER
COMMENTARY hide
60616-82-2
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SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
benzyloxycarbonyl-L-Phe-L-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-L-Phe-L-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
?
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(N-[4-(5-benzoyl-1H-benzimidazol-2-yl)phenyl]-2-chlorobenzamide)
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2,6-dimethoxy-4-[4-(4-phenoxyphenyl)-5-phenyl-1H-imidazol-2-yl]phenol
the compound shows significant inhibitory activity against rhodesain, but displays poor antitrypanosomal activity at 0.020 mM
2,6-dimethoxy-4-[5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazol-2-yl]phenol
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2-(1,3-benzodioxol-5-yl)-5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazole
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2-(3,4-dimethoxyphenyl)-5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazole
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2-(4-methoxyphenyl)-4-[8-[2-(4-methoxyphenyl)-4-phenyl-1H-imidazol-5-yl]dibenzo[b,d]furan-2-yl]-5-phenyl-1H-imidazole
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2-(4-methoxyphenyl)-5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazole
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2-(acetylamino)-N-[4-(6-[[2-(acetylamino)benzoyl]amino]-1H-benzimidazol-2-yl)phenyl]benzamide
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2-(furan-2-yl)-4-[8-[2-(furan-2-yl)-4-phenyl-1H-imidazol-5-yl]dibenzo[b,d]furan-2-yl]-5-phenyl-1H-imidazole
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4,4'-[methanediylbis(1H-benzimidazole-5,2-diyl)]dianiline
has H-bond and steric interactions with Cys 25 of rhodesain's catalytic triad as well as residues Leu67 and Met68 while its dianiline motifs have steric interactions with Gly64 and Leu160
4-(4-[8-[2-(4-carboxyphenyl)-4-phenyl-1H-imidazol-5-yl]dibenzo[b,d]furan-2-yl]-5-phenyl-1H-imidazol-2-yl)benzoic acid
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4-(4-[8-[2-(4-hydroxyphenyl)-4-phenyl-1H-imidazol-5-yl]dibenzo[b,d]furan-2-yl]-5-phenyl-1H-imidazol-2-yl)phenol
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4-amino-N-(4-[6-[(4-aminobenzoyl)amino]-1H-benzimidazol-2-yl]phenyl)benzamide
the compound shows significant inhibitory activity against rhodesain, but displays poor antitrypanosomal activity at 0.020 mM
4-[(E)-benzylideneamino]-N-[4-[6-([4-[(E)-benzylideneamino]benzoyl]amino)-1H-benzimidazol-2-yl]phenyl]benzamide
the compound shows significant inhibitory activity against rhodesain, but displays poor antitrypanosomal activity at 0.020 mM
4-[4-(5,5-dioxidodibenzo[b,d]thiophen-2-yl)-5-phenyl-1H-imidazol-2-yl]-2,6-dimethoxyphenol
-
4-[5-(4-[[2-(4-aminophenyl)-1H-benzimidazol-6-yl]oxy]phenoxy)-1H-benzimidazol-2-yl]aniline
-
4-[5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazol-2-yl]phenol
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4-[8-(2,4-diphenyl-1H-imidazol-5-yl)dibenzo[b,d]furan-2-yl]-2,5-diphenyl-1H-imidazole)
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5-phenyl-4-[4-(phenylsulfanyl)phenyl]-2-(2,4,5-trimethoxyphenyl)-1H-imidazole
the compound shows significant inhibitory activity against rhodesain, but displays poor antitrypanosomal activity at 0.020 mM
5-phenyl-4-[4-(phenylsulfanyl)phenyl]-2-(3,4,5-trimethoxyphenyl)-1H-imidazole
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bis[2-(4-aminophenyl)-1H-benzimidazol-5-yl]methanone
the compound shows significant inhibitory activity against rhodesain, but displays poor antitrypanosomal activity at 0.020 mM
N-[4-(1H-benzimidazol-2-yl)phenyl]-2,2-diphenylacetamide
the compound shows significant inhibitory activity against rhodesain, but displays poor antitrypanosomal activity at 0.020 mM
N-[4-(5-benzoyl-1H-benzimidazol-2-yl)phenyl]-2-chlorobenzamide
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additional information
screening and identification of inhibitors of Trypanosoma brucei cathepsin L with antitrypanosomal activity, overview. No inhibition by 7 and 13
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IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.00236
2,6-dimethoxy-4-[4-(4-phenoxyphenyl)-5-phenyl-1H-imidazol-2-yl]phenol
Trypanosoma brucei rhodesiense
pH 5.5, 25°C
0.02
2,6-dimethoxy-4-[5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazol-2-yl]phenol
Trypanosoma brucei rhodesiense
above, pH 5.5, 25°C
0.02
2-(1,3-benzodioxol-5-yl)-5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazole
Trypanosoma brucei rhodesiense
above, pH 5.5, 25°C
0.00241
2-(3,4-dimethoxyphenyl)-5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazole
Trypanosoma brucei rhodesiense
pH 5.5, 25°C
0.02
2-(4-methoxyphenyl)-4-[8-[2-(4-methoxyphenyl)-4-phenyl-1H-imidazol-5-yl]dibenzo[b,d]furan-2-yl]-5-phenyl-1H-imidazole
Trypanosoma brucei rhodesiense
above, pH 5.5, 25°C
0.02
2-(4-methoxyphenyl)-5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazole
Trypanosoma brucei rhodesiense
above, pH 5.5, 25°C
0.02
2-(acetylamino)-N-[4-(6-[[2-(acetylamino)benzoyl]amino]-1H-benzimidazol-2-yl)phenyl]benzamide
Trypanosoma brucei rhodesiense
above, pH 5.5, 25°C
0.02
2-(furan-2-yl)-4-[8-[2-(furan-2-yl)-4-phenyl-1H-imidazol-5-yl]dibenzo[b,d]furan-2-yl]-5-phenyl-1H-imidazole
Trypanosoma brucei rhodesiense
above, pH 5.5, 25°C
0.00089
4,4'-[methanediylbis(1H-benzimidazole-5,2-diyl)]dianiline
Trypanosoma brucei rhodesiense
pH 5.5, 25°C
0.02
4-(4-[8-[2-(4-carboxyphenyl)-4-phenyl-1H-imidazol-5-yl]dibenzo[b,d]furan-2-yl]-5-phenyl-1H-imidazol-2-yl)benzoic acid
Trypanosoma brucei rhodesiense
above, pH 5.5, 25°C
0.00056
4-(4-[8-[2-(4-hydroxyphenyl)-4-phenyl-1H-imidazol-5-yl]dibenzo[b,d]furan-2-yl]-5-phenyl-1H-imidazol-2-yl)phenol
Trypanosoma brucei rhodesiense
pH 5.5, 25°C
0.00215
4-amino-N-(4-[6-[(4-aminobenzoyl)amino]-1H-benzimidazol-2-yl]phenyl)benzamide
Trypanosoma brucei rhodesiense
pH 5.5, 25°C
0.00178
4-[(E)-benzylideneamino]-N-[4-[6-([4-[(E)-benzylideneamino]benzoyl]amino)-1H-benzimidazol-2-yl]phenyl]benzamide
Trypanosoma brucei rhodesiense
pH 5.5, 25°C
0.02
4-[4-(5,5-dioxidodibenzo[b,d]thiophen-2-yl)-5-phenyl-1H-imidazol-2-yl]-2,6-dimethoxyphenol
Trypanosoma brucei rhodesiense
above, pH 5.5, 25°C
0.00047
4-[5-(4-[[2-(4-aminophenyl)-1H-benzimidazol-6-yl]oxy]phenoxy)-1H-benzimidazol-2-yl]aniline
Trypanosoma brucei rhodesiense
pH 5.5, 25°C
0.02
4-[5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazol-2-yl]phenol
Trypanosoma brucei rhodesiense
above, pH 5.5, 25°C
0.02
4-[8-(2,4-diphenyl-1H-imidazol-5-yl)dibenzo[b,d]furan-2-yl]-2,5-diphenyl-1H-imidazole)
Trypanosoma brucei rhodesiense
above, pH 5.5, 25°C
0.00338
5-phenyl-4-[4-(phenylsulfanyl)phenyl]-2-(2,4,5-trimethoxyphenyl)-1H-imidazole
Trypanosoma brucei rhodesiense
pH 5.5, 25°C
0.02
5-phenyl-4-[4-(phenylsulfanyl)phenyl]-2-(3,4,5-trimethoxyphenyl)-1H-imidazole
Trypanosoma brucei rhodesiense
above, pH 5.5, 25°C
0.0011
bis[2-(4-aminophenyl)-1H-benzimidazol-5-yl]methanone
Trypanosoma brucei rhodesiense
pH 5.5, 25°C
0.00304
N-[4-(1H-benzimidazol-2-yl)phenyl]-2,2-diphenylacetamide
Trypanosoma brucei rhodesiense
pH 5.5, 25°C
0.02
N-[4-(5-benzoyl-1H-benzimidazol-2-yl)phenyl]-2-chlorobenzamide
Trypanosoma brucei rhodesiense
above, pH 5.5, 25°C
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
UNIPROT
ENTRY NAME
ORGANISM
NO. OF AA
NO. OF TRANSM. HELICES
MOLECULAR WEIGHT[Da]
SOURCE
SEQUENCE
LOCALIZATION PREDICTION?
Q95PM0_TRYBR
450
0
48432
TrEMBL
-
PURIFICATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
recombinant rhodesain from Pichia pastoris
CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
recombinant expression of rhodesain in Pichia pastoris
REF.
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
Jefferson, T.; McShan, D.; Warfield, J.; Ogungbe, I.V.
Screening and identification of inhibitors of Trypanosoma brucei cathepsin L with antitrypanosomal activity
Chem. Biol. Drug Des.
87
154-158
2016
Homo sapiens (P07711), Homo sapiens, Trypanosoma brucei brucei (Q95PM0), Trypanosoma brucei rhodesiense (Q95PM0), Trypanosoma brucei brucei 427 (Q95PM0)
Manually annotated by BRENDA team