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Information on EC 3.4.22.27 - cathepsin S and Organism(s) Rattus norvegicus and UniProt Accession Q02765
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EC Tree
3.4.22.27 cathepsin SSpecify your search results
Word Map
- 3.4.22.27
- cathepsins
- lysosomal
-
point-of-care
- cystatins
- dendritic
- atherosclerosis
- proteinases
- elastin
- papain
-
antigen-presenting
-
histocompatibility
- autoimmune
- drug development
-
lacrimal
-
papain-like
- diagnostics
-
ii-associated
-
elastolytic
-
resource-limited
-
s-deficient
-
procathepsins
-
l-like
- pharmacology
- endostatin
- microglial
- fractalkine
- medicine
- par2
-
collagenolytic
- syphilis
-
ii-restricted
The taxonomic range for the selected organisms is: Rattus norvegicus
The expected taxonomic range for this enzyme is: Eukaryota, Bacteria
The expected taxonomic range for this enzyme is: Eukaryota, Bacteria
Reaction Schemes
similar to cathepsin L, but with much less activity on Z-Phe-Arg-/-NHMec, and more activity on the Z-Val-Val-Arg-/- compound
Synonyms
cathepsin s, pocts, cat s, cat-s, pfctssa, socats, cath s, rs1136774, rs7534124, rs16827671, 
more
topSYNONYM 
ORGANISM
UNIPROT
COMMENTARY 
LITERATURE
C01.034
-
-
-
-
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
hydrolysis of peptide bond
hydrolysis of peptide bond
-
-
-
-
CAS REGISTRY NUMBER
COMMENTARY
71965-46-3
-
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
Z-Leu-Leu-Arg-7-amido-4-methylcoumarin + H2O
Z-Leu-Leu-Arg + 7-amino-4-methylcoumarin
-
-
-
?
benzyloxycarbonyl-Leu-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Leu-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Phe-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
benzyloxycarbonyl-Val-Val-Arg-4-methyl-coumaryl-7-amide + H2O
benzyloxycarbonyl-Val-Val-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Val-Val-Arg + 7-amino-4-methylcoumarin
butyloxycarbonyl-Val-Leu-Lys-7-amido-4-methylcoumarin + H2O
butyloxycarbonyl-Val-Leu-Lys + 7-amino-4-methylcoumarin
-
-
-
-
?
benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Val-Val-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Val-Val-Arg + 7-amino-4-methylcoumarin
-
73% of the activity with benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
-
-
?
additional information
?
-
-
cathepsin S is implicated as a key enzyme in the processing of major histocompatability complex class II molecules
-
-
?
additional information
?
-
-
primary role of the enzyme in heterophagocytosis of proteins from the ultrafiltrate
-
-
?
additional information
?
-
-
cathepsin S is possibly involved in thyroid hormone biosynthesis
-
-
?
additional information
?
-
-
cathepsin S catalyzes a key step in antigen presentation, detailed overview
-
-
?
additional information
?
-
-
CATS is an important player in the spinal mechanisms involved in chronic pain induction and maintenance
-
-
?
additional information
?
-
-
CATS is widely expressed in the brain and is implicated in several neurological conditions such as Alzheimer's disease, amyotrophic lateral sclerosis and age-related inflammation, CATS is also implicated in neuropathic hyperalgesia and allodynia
-
-
?
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
?
-
-
cathepsin S is implicated as a key enzyme in the processing of major histocompatability complex class II molecules
-
-
?
additional information
?
-
-
primary role of the enzyme in heterophagocytosis of proteins from the ultrafiltrate
-
-
?
additional information
?
-
-
cathepsin S is possibly involved in thyroid hormone biosynthesis
-
-
?
additional information
?
-
-
cathepsin S catalyzes a key step in antigen presentation, detailed overview
-
-
?
additional information
?
-
-
CATS is an important player in the spinal mechanisms involved in chronic pain induction and maintenance
-
-
?
additional information
?
-
-
CATS is widely expressed in the brain and is implicated in several neurological conditions such as Alzheimer's disease, amyotrophic lateral sclerosis and age-related inflammation, CATS is also implicated in neuropathic hyperalgesia and allodynia
-
-
?
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
6-[[4-(4-acetylpiperazin-1-yl)-2-fluorophenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-[2-(4,4-difluorocyclohexyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
(2R)-N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydrofuran-2-carboxamide
-
-
(2S)-N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]tetrahydrofuran-2-carboxamide
-
-
(2S)-N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydrofuran-2-carboxamide
-
-
1,2-dichloro-4-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene
-
-
1-bromo-3-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene
-
-
1-bromo-4-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene
-
-
1-[(1S)-1-[[(1R)-2-[(1-cyanocyclopropyl)amino]-1-[[(cyclopropylmethoxy)sulfinyl]methyl]-2-oxoethyl]amino]-2,2,2-trifluoroethyl]-4-fluorobenzene
-
-
1-[([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propyl]sulfinyl]oxy)methyl]-2,3-difluorobenzene
-
-
4-methyl-N-[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-N2-(morpholin-4-ylcarbonyl)-L-leucinamide
-
-
4-methyl-N2-(morpholin-4-ylcarbonyl)-N-(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)-L-leucinamide
-
-
methyl (2R)-2-[[(1S)-1-(4-bromophenyl)-2,2,2-trifluoroethyl]amino]-3-[(1-cyanocyclopropyl)amino]-3-oxopropane-1-sulfinate
-
-
methyl (2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propane-1-sulfenate
-
-
methyl (2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propane-1-sulfinate
-
-
methyl (3S)-3-[[3-cyclohexyl-N-(morpholin-4-ylcarbonyl)-L-alanyl]amino]-4-[[4-(trifluoromethoxy)phenyl]amino]butane-1-sulfinate
-
-
morpholinurea-leucine-homophenylalanine-vinyl sulfone-phenyl
-
irreversible inhibitor
morpholinurea-leucinehomophenylalanine-vinyl phenyl sulfone
-
irreversible CatS inhibitor
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]-1-benzofuran-2-carboxamide
-
-
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]-5-(3-fluorophenyl)furan-2-carboxamide
-
-
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]-5-[3-(trifluoromethyl)phenyl]furan-2-carboxamide
-
-
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]furan-2-carboxamide
-
-
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]furan-3-carboxamide
-
-
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]morpholine-4-carboxamide
-
-
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]tetrahydrofuran-3-carboxamide
-
-
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[[(1S)-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]amino]ethyl]morpholine-4-carboxamide
-
-
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]morpholine-4-carboxamide
-
-
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydro-2H-pyran-4-carboxamide
-
-
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydrofuran-3-carboxamide
-
-
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-2-(5-fluoro-2,2-dimethyl-2,3-dihydro-1H-indol-1-yl)-1-methylethyl]amino]-2-oxoethyl]morpholine-4-carboxamide
-
-
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-2-(5-fluoro-2,3-dihydro-1H-indol-1-yl)-1-methylethyl]amino]-2-oxoethyl]morpholine-4-carboxamide
-
-
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-2-(5-fluoro-3,3-dimethyl-2,3-dihydro-1H-indol-1-yl)-1-methylethyl]amino]-2-oxoethyl]morpholine-4-carboxamide
-
-
N-[(1S)-1-(cyclopentylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]morpholine-4-carboxamide
-
-
N-[(1S)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxo-1-[(2-phenylethyl)sulfanyl]ethyl]morpholine-4-carboxamide
-
-
N-[(1S)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxo-1-[(2-phenylethyl)sulfonyl]ethyl]morpholine-4-carboxamide
-
-
Na-(morpholin-4-ylcarbonyl)-N-(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)-L-phenylalaninamide
-
-
tetrahydro-2H-pyran-4-yl [(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]carbamate
-
-
tetrahydrofuran-3-yl [(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]carbamate
-
-
additional information
-
synthesis and inhibitory effects of diverse arylaminoethyl carbamate inhibitors possessing a substrate peptidomimetic scaffold, structue-activity relationship, pharmacokinetics, overview
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.288
benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin
-
pH 7.5, 37°C
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.000012
6-[[4-(4-acetylpiperazin-1-yl)-2-fluorophenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Rattus norvegicus
rat Cat S, Z-Leu-Leu-Arg-7-amido-4-methylcumarin as substrate
0.00001
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Rattus norvegicus
rat Cat S, Z-Leu-Leu-Arg-7-amido-4-methylcumarin as substrate
0.000028
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-[2-(4,4-difluorocyclohexyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Rattus norvegicus
rat Cat S, Z-Leu-Leu-Arg-7-amido-4-methylcumarin as substrate
0.000053
(2R)-N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydrofuran-2-carboxamide
Rattus norvegicus
-
-
0.000658
(2S)-N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]tetrahydrofuran-2-carboxamide
Rattus norvegicus
-
-
0.000018
(2S)-N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydrofuran-2-carboxamide
Rattus norvegicus
-
-
0.000015
1,2-dichloro-4-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene
Rattus norvegicus
-
IC50 less than 0.2 mM
0.000044
1-bromo-3-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene
Rattus norvegicus
-
IC50 less than 0.2 mM
0.000066
1-bromo-4-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene
Rattus norvegicus
-
-
0.000759
1-[(1S)-1-[[(1R)-2-[(1-cyanocyclopropyl)amino]-1-[[(cyclopropylmethoxy)sulfinyl]methyl]-2-oxoethyl]amino]-2,2,2-trifluoroethyl]-4-fluorobenzene
Rattus norvegicus
-
-
0.000021
1-[([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propyl]sulfinyl]oxy)methyl]-2,3-difluorobenzene
Rattus norvegicus
-
-
0.000093
4-methyl-N-[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-N2-(morpholin-4-ylcarbonyl)-L-leucinamide
Rattus norvegicus
-
-
0.00022
4-methyl-N2-(morpholin-4-ylcarbonyl)-N-(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)-L-leucinamide
Rattus norvegicus
-
-
0.001051
methyl (2R)-2-[[(1S)-1-(4-bromophenyl)-2,2,2-trifluoroethyl]amino]-3-[(1-cyanocyclopropyl)amino]-3-oxopropane-1-sulfinate
Rattus norvegicus
-
-
0.01
methyl (2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propane-1-sulfenate
Rattus norvegicus
-
IC50 above 0.01 mM
0.000426
methyl (2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propane-1-sulfinate
Rattus norvegicus
-
-
0.000005
methyl (3S)-3-[[3-cyclohexyl-N-(morpholin-4-ylcarbonyl)-L-alanyl]amino]-4-[[4-(trifluoromethoxy)phenyl]amino]butane-1-sulfinate
Rattus norvegicus
-
-
0.000017
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]-1-benzofuran-2-carboxamide
Rattus norvegicus
-
-
0.000034
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]-5-(3-fluorophenyl)furan-2-carboxamide
Rattus norvegicus
-
-
0.000011
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]-5-[3-(trifluoromethyl)phenyl]furan-2-carboxamide
Rattus norvegicus
-
-
0.000047
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]furan-2-carboxamide
Rattus norvegicus
-
-
0.000006
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]furan-3-carboxamide
Rattus norvegicus
-
-
0.000099
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]morpholine-4-carboxamide
Rattus norvegicus
-
-
0.000213
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]tetrahydrofuran-3-carboxamide
Rattus norvegicus
-
-
0.000011
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[[(1S)-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]amino]ethyl]morpholine-4-carboxamide
Rattus norvegicus
-
-
0.000011
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]morpholine-4-carboxamide
Rattus norvegicus
-
-
0.000012
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydro-2H-pyran-4-carboxamide
Rattus norvegicus
-
-
0.000021
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydrofuran-3-carboxamide
Rattus norvegicus
-
-
0.000111
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-2-(5-fluoro-2,2-dimethyl-2,3-dihydro-1H-indol-1-yl)-1-methylethyl]amino]-2-oxoethyl]morpholine-4-carboxamide
Rattus norvegicus
-
-
0.000087
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-2-(5-fluoro-2,3-dihydro-1H-indol-1-yl)-1-methylethyl]amino]-2-oxoethyl]morpholine-4-carboxamide
Rattus norvegicus
-
-
0.000011
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-2-(5-fluoro-3,3-dimethyl-2,3-dihydro-1H-indol-1-yl)-1-methylethyl]amino]-2-oxoethyl]morpholine-4-carboxamide
Rattus norvegicus
-
-
0.000049
N-[(1S)-1-(cyclopentylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]morpholine-4-carboxamide
Rattus norvegicus
-
-
0.000012
N-[(1S)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxo-1-[(2-phenylethyl)sulfanyl]ethyl]morpholine-4-carboxamide
Rattus norvegicus
-
-
0.000032
N-[(1S)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxo-1-[(2-phenylethyl)sulfonyl]ethyl]morpholine-4-carboxamide
Rattus norvegicus
-
-
0.0114
Na-(morpholin-4-ylcarbonyl)-N-(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)-L-phenylalaninamide
Rattus norvegicus
-
-
0.000012
tetrahydro-2H-pyran-4-yl [(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]carbamate
Rattus norvegicus
-
-
0.000042 - 0.000049
tetrahydrofuran-3-yl [(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]carbamate
additional information
6-[[4-(4-acetylpiperazin-1-yl)-2-fluorophenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
0.000042
tetrahydrofuran-3-yl [(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]carbamate
Rattus norvegicus
-
-
0.000049
tetrahydrofuran-3-yl [(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]carbamate
Rattus norvegicus
-
-
additional information
6-[[4-(4-acetylpiperazin-1-yl)-2-fluorophenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Rattus norvegicus
rat mutant G137C Cat S, IC50 is above 0.01 mM, Z-Leu-Leu-Arg-7-amido-4-methylcumarin as substrate
additional information
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Rattus norvegicus
rat mutant G137C Cat S, IC50 is above 0.01 mM, Z-Leu-Leu-Arg-7-amido-4-methylcumarin as substrate
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
additional information
-
expression and activity of CATS is upregulated in the spinal cord during the development and progression of neuropathic pain in the CNS of the rat 5th lumbar spinal nerve transection model after the lesion, the strongest increase in protein content is found in the thoracic segment (63.6%)
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
6.5
-
reaction with benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin or benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin
pH RANGE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
5 - 7.5
-
pH 5.0: about 20% of maximal activity, pH 7.5: about 40% of maximal activity, reaction with benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin or benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin
5.5 - 8.5
-
pH 5.5: about 45% of maximal activity, pH 8.5: about 50% of maximal activity, reaction with benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
ORGANISM
COMMENTARY
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
SOURCE
additional information
-
the enzyme is expressed in antigen presenting cells
-
in nephron segments microdissected from lyophilized renal sections, highest cathepsin S activity is found in the proximal convoluted tubules followed by proximal straight tubules of the superficial cortex. In the remaining segments cathepsin S activity is hardly detectable
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY
GeneOntology No.
LITERATURE
SOURCE
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). CATS_RAT
330
0
36833
Swiss-Prot
other Location (Reliability: 2)
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
proteolytic modification
-
the cDNA encodes a 330-residue protein with a 17-amino acid putative signal sequence, 95-residue ürpregion, and 216-residue mature protein
PROTEIN VARIANTS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
G137C
recombinant rat Cat S mutant shows no inhibition by 6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile or 6-[[4-(4-acetylpiperazin-1-yl)-2-fluorophenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile or 6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-[2-(4,4-difluorocyclohexyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
additional information
-
addition of a carboxy-terminal hexahistidine purification tag has no effect on the kinetic characterization of any of the enzyme forms against butyloxycarbonyl-Val-Leu-Lys-7-amido-4-methylcoumarin substrate
pH STABILITY
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
TEMPERATURE STABILITY
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
37
37
-
15 min, retention of more than 80% enzyme activity at pH 7.0, about 40% retention at pH 4.7 and about 50% retention at pH 8.5
CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
expression in baculovirally infected Sf9 insect cells along with humanized forms truncated by eight residues at the amino-terminus
-
APPLICATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
drug development
discovery of orally bioavailable cathepsin S inhibitors for the reversal of neuropathic pain, cathepsin S inhibitors are attractive targets as immunological therapeutic agents
medicine
-
cathepsin S is a potential therapeutic target for regulation of major histocompatibility complex class II immune responses, possibly resulting in treatments for autoimmune diseases and allergic asthma
REF.
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
Mason, C.S.; Lamers, M.B.; Henderson, I.M.; Monk, T.; Williams, D.H.
Baculoviral expression and characterization of rodent cathepsin S
Protein Expr. Purif.
23
45-54
2001
Homo sapiens, Mus musculus, Rattus norvegicus
Schmid, H.; Koop, M.; Utermann, S.; Lambacher, L.; Mayer, P.; Schaefer, L.
Specific catalytic activity of cathepsin S in comparison to cathepsins B and L along the rat nephron
Biol. Chem.
378
61-69
1997
Rattus norvegicus
Petanceska, S.; Devi, L.
Sequence analysis, tissue distribution, and expression of rat cathepsin S
J. Biol. Chem.
267
26038-26043
1992
Rattus norvegicus
Tully, D.C.; Liu, H.; Chatterjee, A.K.; Alper, P.B.; Williams, J.A.; Roberts, M.J.; Mutnick, D.; Woodmansee, D.H.; Hollenbeck, T.; Gordon, P.; Chang, J.; Tuntland, T.; Tumanut, C.; Li, J.; Harris, J.L.; Karanewsky, D.S.
Arylaminoethyl carbamates as a novel series of potent and selective cathepsin S inhibitors
Bioorg. Med. Chem. Lett.
16
5107-5111
2006
Rattus norvegicus
Liu, W.; Spero, D.M.
Cysteine protease cathepsin S as a key step in antigen presentation
Drug News Perspect.
17
357-363
2004
Bos taurus, Homo sapiens, Mus musculus, Rattus norvegicus
Tully, D.C.; Liu, H.; Chatterjee, A.K.; Alper, P.B.; Epple, R.; Williams, J.A.; Roberts, M.J.; Woodmansee, D.H.; Masick, B.T.; Tumanut, C.; Li, J.; Spraggon, G.; Hornsby, M.; Chang, J.; Tuntland, T.; Hollenbeck, T.; Gordon, P.; Harris, J.L.; Karanewsky, D.S.
Synthesis and SAR of arylaminoethyl amides as noncovalent inhibitors of cathepsin S: P3 cyclic ethers
Bioorg. Med. Chem. Lett.
16
5112-5117
2006
Rattus norvegicus
Gauthier, J.Y.; Black, W.C.; Courchesne, I.; Cromlish, W.; Desmarais, S.; Houle, R.; Lamontagne, S.; Li, C.S.; Masse, F.; McKay, D.J.; Ouellet, M.; Robichaud, J.; Truchon, J.F.; Truong, V.L.; Wang, Q.; Percival, M.D.
The identification of potent, selective, and bioavailable cathepsin S inhibitors
Bioorg. Med. Chem. Lett.
17
4929-4933
2007
Homo sapiens, Mus musculus, Rattus norvegicus
Barclay, J.; Clark, A.K.; Ganju, P.; Gentry, C.; Patel, S.; Wotherspoon, G.; Buxton, F.; Song, C.; Ullah, J.; Winter, J.; Fox, A.; Bevan, S.; Malcangio, M.
Role of the cysteine protease cathepsin S in neuropathic hyperalgesia
Pain
130
225-234
2007
Rattus norvegicus (Q02765)
Clark, A.K.; Yip, P.K.; Grist, J.; Gentry, C.; Staniland, A.A.; Marchand, F.; Dehvari, M.; Wotherspoon, G.; Winter, J.; Ullah, J.; Bevan, S.; Malcangio, M.
Inhibition of spinal microglial cathepsin S for the reversal of neuropathic pain
Proc. Natl. Acad. Sci. USA
104
10655-10660
2007
Rattus norvegicus
Leichsenring, A.; Baecker, I.; Wendt, W.; Andriske, M.; Schmitz, B.; Stichel, C.C.; Luebbert, H.
Differential expression of cathepsin S and X in the spinal cord of a rat neuropathic pain model
BMC Neurosci.
9
80
2008
Rattus norvegicus
Irie, O.; Kosaka, T.; Ehara, T.; Yokokawa, F.; Kanazawa, T.; Hirao, H.; Iwasaki, A.; Sakaki, J.; Teno, N.; Hitomi, Y.; Iwasaki, G.; Fukaya, H.; Nonomura, K.; Tanabe, K.; Koizumi, S.; Uchiyama, N.; Bevan, S.J.; Malcangio, M.; Gentry, C.; Fox, A.J.; Yaqoob, M.; Culshaw, A.J.; Allan Hallett, A.J.
Discovery of orally bioavailable cathepsin S inhibitors for the reversal of neuropathic pain
J. Med. Chem.
51
5502-5505
2008
Homo sapiens, Mus musculus, Rattus norvegicus (Q02765)
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