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Information on EC 3.4.22.38 - cathepsin K and Organism(s) Mus musculus and UniProt Accession P55097

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EC Tree
     3 Hydrolases
         3.4 Acting on peptide bonds (peptidases)
             3.4.22 Cysteine endopeptidases
                3.4.22.38 cathepsin K
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This record set is specific for:
Mus musculus
UNIPROT: P55097 not found.
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Word Map
The taxonomic range for the selected organisms is: Mus musculus
The enzyme appears in selected viruses and cellular organisms
Synonyms
cathepsin k, cathepsin-k, cat k, cath k, cat-k, cathepsin o2, oc-2 protein, more
SYNONYM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
cath K
-
-
cathepsin K
-
-
Cathepsin O2
-
-
-
-
OC-2 protein
-
-
-
-
rhCK
-
-
-
-
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
hydrolysis of peptide bond
-
-
-
-
CAS REGISTRY NUMBER
COMMENTARY hide
94716-09-3
-
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
2-aminobenzoyl-RPPGFSPFR-(3-nitrotyrosine) + H2O
?
show the reaction diagram
-
-
-
-
?
Benzyloxycarbonyl-Leu-Arg 4-methoxy-2-naphthylamide + H2O
Benzyloxycarbonyl-Leu-Arg + 4-methoxy-2-naphthylamine
show the reaction diagram
-
-
-
-
?
Benzyloxycarbonyl-Leu-Arg 4-methylcoumarin 7-amide + H2O
Benzyloxycarbonyl-Leu-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
bradykinin + H2O
bradykinin(1-4) + bradykinin(5-9)
show the reaction diagram
-
-
-
-
?
carbobenzyloxy-Leu-Arg-4-methoxy-2-naphthylamide + H2O
carbobenzyloxy-Leu-Arg + 4-methoxy-2-naphthylamine
show the reaction diagram
-
-
-
-
?
collagen I + H2O
?
show the reaction diagram
Collagen IV + H2O
?
show the reaction diagram
-
-
-
-
?
Collagen type I + H2O
?
show the reaction diagram
-
-
-
-
?
Elastin + H2O
?
show the reaction diagram
-
-
-
-
?
Gelatin + H2O
?
show the reaction diagram
-
substrate for CTSK zymography
-
-
?
kinin + H2O
?
show the reaction diagram
Type I collagen + H2O
?
show the reaction diagram
-
-
-
-
?
additional information
?
-
NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
collagen I + H2O
?
show the reaction diagram
Collagen IV + H2O
?
show the reaction diagram
-
-
-
-
?
Collagen type I + H2O
?
show the reaction diagram
-
-
-
-
?
Elastin + H2O
?
show the reaction diagram
-
-
-
-
?
kinin + H2O
?
show the reaction diagram
-
the potency of cathepsin K to modulate bradikinin-dependent contraction of smooth muscles, cathepsin K may act as a kininase
-
-
?
Type I collagen + H2O
?
show the reaction diagram
-
-
-
-
?
additional information
?
-
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
N'-cyano-N,N',4-trimethyl-2-(4'-(methylsulfonyl)-[1,1'-biphenyl]-3-yl)pentanehydrazide
racemic
N'-cyano-N,N',4-trimethyl-2-(4'-(methylsulfonyl)-[1,1'-biphenyl]-4-yl)pentanehydrazide
racemic
1,3-bis(CBZ-Leu-NH)-2-propanone
-
-
balicatib
-
-
benzyl [(2S)-1-{2-[(2-{(2S)-2-[(2-amino-3-phenylpropanoyl)amino]-4-methylpentanoyl}hydrazinyl)carbonyl]hydrazinyl}-4-methyl-1-oxopentan-2-yl]carbamate
-
-
BML-244
-
-
Boc-Phe-Leu-NHNH-CO-NHNH-Leu-Z
-
-
carboxybenzoyl-Phe-Phe-CHN2
-
-
cathepsin K inhibitor II
-
-
CatK-II
-
specific inhibitor
-
CatK-selective inhibitor II
-
commercial preparation
dibenzyl [(2-oxopropane-1,3-diyl)bis{imino[(2S)-4-methyl-1-oxopentane-1,2-diyl]}]biscarbamate
-
-
E-64d
-
-
K4b
-
potent, reversible, Cat K-selective inhibitor
L-873724
-
-
leupeptin
-
-
LHVS
-
a cell-permeable broad spectrum cathepsin inhibitor
Mu-Leu-Hph-fluoromethylketone
-
-
N-(1-([(cyanomethyl)amino]carbonyl)cyclohexyl)-4-[2-(4-methylpiperazin-1-yl)-1,3-thiazol-4-yl]benzamide
-
i.e. L-006235 or CRA-013788/L
NC-2300
-
-
odanacatib
-
-
relacatib
-
-
trans-epoxysuccinyl-L-leucylamido-(4-guanidino)butane
-
-
additional information
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
additional information
-
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.00048
balicatib
Mus musculus
-
pH and temperature not specified in the publication
0.000044
benzyl [(2S)-1-{2-[(2-{(2S)-2-[(2-amino-3-phenylpropanoyl)amino]-4-methylpentanoyl}hydrazinyl)carbonyl]hydrazinyl}-4-methyl-1-oxopentan-2-yl]carbamate
Mus musculus
-
pH and temperature not specified in the publication
0.000748
BML-244
Mus musculus
-
pH and temperature not specified in the publication
0.000296
Boc-Phe-Leu-NHNH-CO-NHNH-Leu-Z
Mus musculus
-
pH and temperature not specified in the publication
0.00426
dibenzyl [(2-oxopropane-1,3-diyl)bis{imino[(2S)-4-methyl-1-oxopentane-1,2-diyl]}]biscarbamate
Mus musculus
-
pH and temperature not specified in the publication
0.000145
K4b
Mus musculus
-
pH and temperature not specified in the publication
0.000043
L-873724
Mus musculus
-
pH and temperature not specified in the publication
0.000018
Mu-Leu-Hph-fluoromethylketone
Mus musculus
-
pH and temperature not specified in the publication
0.0000024
N-(1-([(cyanomethyl)amino]carbonyl)cyclohexyl)-4-[2-(4-methylpiperazin-1-yl)-1,3-thiazol-4-yl]benzamide
Mus musculus
-
recombinant cathepsin K
0.000102
NC-2300
Mus musculus
-
pH and temperature not specified in the publication
0.000108
odanacatib
Mus musculus
-
pH and temperature not specified in the publication
0.000066
relacatib
Mus musculus
-
pH and temperature not specified in the publication
additional information
additional information
Mus musculus
-
Ulmus diviana stem bral extracts show an IC50 of 0.0875 mg/ml
-
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
additional information
-
osteoclast resorption activity
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
5 - 6
-
-
6 - 7.4
-
kcat/Km with 2-aminobenzoyl-RPPGFSPFR-(3-nitrotyrosine) is 1.4fold higher at pH 6.0 than at pH 7.4
7.5
-
assay at
additional information
-
CatK is a lysosomal cysteine protease that degrades type I collagen at neutral and acidic pH
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
28
-
assay at
37
-
assay at
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
-
SwissProt
Manually annotated by BRENDA team
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
vascular smooth muscle cell line
Manually annotated by BRENDA team
-
CTSK is active mainly in the early stages of adipogenesis
Manually annotated by BRENDA team
-
in the macrophage-rich regions of atherosclerotic plaques
Manually annotated by BRENDA team
-
skeletal and nonskeletal tumor cell
Manually annotated by BRENDA team
-
recombinant enzyme
Manually annotated by BRENDA team
-
primary type II alveolar epithelial cells
Manually annotated by BRENDA team
additional information
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY hide
GeneOntology No.
LITERATURE
SOURCE
-
the enzyme is secereted by osteoclasts
-
Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
malfunction
UNIPROT
ENTRY NAME
ORGANISM
NO. OF AA
NO. OF TRANSM. HELICES
MOLECULAR WEIGHT[Da]
SOURCE
SEQUENCE
LOCALIZATION PREDICTION?
CATK_MOUSE
329
0
36889
Swiss-Prot
Secretory Pathway (Reliability: 1)
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
32000
-
x * 32000, about, proenzyme
SUBUNIT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
?
-
x * 32000, about, proenzyme
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
proteolytic modification
PROTEIN VARIANTS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
Y67L/L205A
-
2-aminobenzoyl-RP-PGFSPFR-(3-nitrotyrosine) is not cleaved by the the mutant enzyme
additional information
pH STABILITY
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
7.2
-
2 min, soluble bone fraction, inactivation at pH 7.2 and 50°C
698935
TEMPERATURE STABILITY
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
50
-
2 min, soluble bone fraction, inactivation at pH 7.2 and 50°C
PURIFICATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
expression in Escherichia coli
-
genotyping of C57BL/6 mice either wild-type for cathepsin K, CK+/+, heterozygous for cathepsin K, CK+/-, or deficient in cathepsin K, CK-/-, overview
-
quantitative expression analysis by RT-PCR
-
EXPRESSION
ORGANISM
UNIPROT
LITERATURE
free cholesterol accumulation in macrophage membranes induces cathepsin K
-
receptor activator of nuclear factor-kappaB or small GTPase Rab do not mediate cathepsin K induction
-
APPLICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
drug development
-
lysosomal cysteine protease is an interesting target molecule with therapeutic potential to attenuate bleomycin-induced pulmonary fibrosis in mice
medicine
pharmacology
REF.
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
Kamiya, T.; Kobayashi, Y.; Kanaoka, K.; Nakashima, T.; Kato, Y.; Mizuno, A.; Sakai, H.
Fluorescence microscopic demonstration of cathepsin K activity a the major lysosomal cystein proteinase in osteoclasts
J. Biochem.
123
752-759
1998
Oryctolagus cuniculus, Mus musculus
Manually annotated by BRENDA team
Rantakokko, J.; Aro, H.T.; Savontaus, M.; Vuorio, E.
Mouse cathepsin K: cDNA cloning and predominant expression of the gene in osteoclasts, and in some hypertrophing chondrocytes during mouse development
FEBS Lett.
393
307-313
1996
Mus musculus
Manually annotated by BRENDA team
Buehling, F.; Roecken, C.; Brasch, F.; Hartig, R.; Yasuda, Y.; Saftig, P.; Broemme, D.; Welte, T.
Pivotal role of cathepsin K in lung fibrosis
Am. J. Pathol.
164
2203-2216
2004
Homo sapiens, Mus musculus
Manually annotated by BRENDA team
Godat, E.; Lecaille, F.; Desmazes, C.; Duchene, S.; Weidauer, E.; Saftig, P.; Broemme, D.; Vandier, C.; Lalmanach, G.
Cathepsin K: a cysteine protease with unique kinin-degrading properties
Biochem. J.
383
501-506
2004
Mus musculus
Manually annotated by BRENDA team
van den Brule, S.; Misson, P.; Buehling, F.; Lison, D.; Huaux, F.
Overexpression of cathepsin K during silica-induced lung fibrosis and control by TGF-beta
Respir. Res.
6
84
2005
Homo sapiens, Mus musculus
Manually annotated by BRENDA team
Samokhin, A.O.; Wong, A.; Saftig, P.; Broemme, D.
Role of cathepsin K in structural changes in brachiocephalic artery during progression of atherosclerosis in apoE-deficient mice
Atherosclerosis
200
58-68
2008
Mus musculus
Manually annotated by BRENDA team
Asagiri, M.; Hirai, T.; Kunigami, T.; Kamano, S.; Gober, H.J.; Okamoto, K.; Nishikawa, K.; Latz, E.; Golenbock, D.T.; Aoki, K.; Ohya, K.; Imai, Y.; Morishita, Y.; Miyazono, K.; Kato, S.; Saftig, P.; Takayanagi, H.
Cathepsin K-dependent toll-like receptor 9 signaling revealed in experimental arthritis
Science
319
624-627
2008
Mus musculus, Rattus norvegicus
Manually annotated by BRENDA team
Yang, M.; Sun, J.; Zhang, T.; Liu, J.; Zhang, J.; Shi, M.A.; Darakhshan, F.; Guerre-Millo, M.; Clement, K.; Gelb, B.D.; Dolgnov, G.; Shi, G.P.
Deficiency and inhibition of cathepsin K reduce body weight gain and increase glucose metabolism in mice
Arterioscler. Thromb. Vasc. Biol.
28
2202-2208
2008
Homo sapiens, Mus musculus
Manually annotated by BRENDA team
Schurigt, U.; Hummel, K.M.; Petrow, P.K.; Gajda, M.; Stoeckigt, R.; Middel, P.; Zwerina, J.; Janik, T.; Bernhardt, R.; Schueler, S.; Scharnweber, D.; Beckmann, F.; Saftig, P.; Kollias, G.; Schett, G.; Wiederanders, B.; Braeuer, R.
Cathepsin K deficiency partially inhibits, but does not prevent, bone destruction in human tumor necrosis factor-transgenic mice
Arthritis Rheum.
58
422-434
2008
Mus musculus
Manually annotated by BRENDA team
Yamane, H.; Sakai, A.; Mori, T.; Tanaka, S.; Moridera, K.; Nakamura, T.
The anabolic action of intermittent PTH in combination with cathepsin K Inhibitor or alendronate differs depending on the remodeling status in bone in ovariectomized mice
Bone
44
1055-1062
2008
Mus musculus
Manually annotated by BRENDA team
Kozloff, K.M.; Quinti, L.; Patntirapong, S.; Hauschka, P.V.; Tung, C.H.; Weissleder, R.; Mahmood, U.
Non-invasive optical detection of cathepsin K-mediated fluorescence reveals osteoclast activity in vitro and in vivo
Bone
44
190-198
2009
Homo sapiens, Mus musculus
Manually annotated by BRENDA team
Pennypacker, B.; Shea, M.; Liu, Q.; Masarachia, P.; Saftig, P.; Rodan, S.; Rodan, G.; Kimmel, D.
Bone density, strength, and formation in adult cathepsin K (-/-) mice
Bone
44
199-207
2009
Mus musculus
Manually annotated by BRENDA team
Morko, J.; Kiviranta, R.; Mulari, M.T.; Ivaska, K.K.; Vaeaenaenen, H.K.; Vuorio, E.; Laitala-Leinonen, T.
Overexpression of cathepsin K accelerates the resorption cycle and osteoblast differentiation in vitro
Bone
44
717-728
2009
Mus musculus
Manually annotated by BRENDA team
Boskey, A.L.; Gelb, B.D.; Pourmand, E.; Kudrashov, V.; Doty, S.B.; Spevak, L.; Schaffler, M.B.
Ablation of cathepsin K activity in the young mouse causes hypermineralization of long bone and growth plates
Calcif. Tissue Int.
84
229-239
2009
Mus musculus, Mus musculus C57Bl6/J
Manually annotated by BRENDA team
Guo, J.; Bot, I.; de Nooijer, R.; Hoffman, S.J.; Stroup, G.B.; Biessen, E.A.; Benson, G.M.; Groot, P.H.; Van Eck, M.; Van Berkel, T.J.
Leucocyte cathepsin K affects atherosclerotic lesion composition and bone mineral density in low-density lipoprotein receptor deficient mice
Cardiovasc. Res.
81
278-285
2009
Mus musculus
Manually annotated by BRENDA team
Han, J.; Luo, T.; Gu, Y.; Li, G.; Jia, W.; Luo, M.
Cathepsin K regulates adipocyte differentiation: possible involvement of type I collagen degradation
Endocr. J.
56
55-63
2009
Mus musculus
Manually annotated by BRENDA team
Svelander, L.; Erlandsson-Harris, H.; Astner, L.; Grabowska, U.; Klareskog, L.; Lindstrom, E.; Hewitt, E.
Inhibition of cathepsin K reduces bone erosion, cartilage degradation and inflammation evoked by collagen-induced arthritis in mice
Eur. J. Pharmacol.
613
155-162
2009
Homo sapiens, Mus musculus, Mus musculus DBA/1J
Manually annotated by BRENDA team
Wilson, S.R.; Peters, C.; Saftig, P.; Broemme, D.
Cathepsin K activity-dependent regulation of osteoclast actin ring formation and bone resorption
J. Biol. Chem.
284
2584-2592
2009
Homo sapiens, Mus musculus, Mus musculus C57BL/6
Manually annotated by BRENDA team
Kim, K.W.; Park, J.S.; Kim, K.S.; Jin, U.H.; Kim, J.K.; Suh, S.J.; Kim, C.H.
Inhibition of Ulmus davidiana Planch (Ulmaceae) on bone resorption mediated by processing of cathepsin K in cultured mouse osteoclasts
Phytother. Res.
22
511-517
2008
Mus musculus
Manually annotated by BRENDA team
Srivastava, M.; Steinwede, K.; Kiviranta, R.; Morko, J.; Hoymann, H.G.; Laenger, F.; Buhling, F.; Welte, T.; Maus, U.A.
Overexpression of cathepsin K in mice decreases collagen deposition and lung resistance in response to bleomycin-induced pulmonary fibrosis
Respir. Res.
9
54
2008
Mus musculus, Mus musculus FVB/N
Manually annotated by BRENDA team
Bai, L.; Beckers, L.; Wijnands, E.; Lutgens, S.P.; Herias, M.V.; Saftig, P.; Daemen, M.J.; Cleutjens, K.; Lutgens, E.; Biessen, E.A.; Heeneman, S.
Cathepsin K gene disruption does not affect murine aneurysm formation
Atherosclerosis
209
96-103
2010
Mus musculus
Manually annotated by BRENDA team
Desmarais, S.; Masse, F.; Percival, M.D.
Pharmacological inhibitors to identify roles of cathepsin K in cell-based studies: a comparison of available tools
Biol. Chem.
390
941-948
2009
Oryctolagus cuniculus, Homo sapiens, Mus musculus, Rattus norvegicus
Manually annotated by BRENDA team
Sun, Y.; Ishibashi, M.; Seimon, T.; Lee, M.; Sharma, S.M.; Fitzgerald, K.A.; Samokhin, A.O.; Wang, Y.; Sayers, S.; Aikawa, M.; Jerome, W.G.; Ostrowski, M.C.; Bromme, D.; Libby, P.; Tabas, I.A.; Welch, C.L.; Tall, A.R.
Free cholesterol accumulation in macrophage membranes activates Toll-like receptors and p38 mitogen-activated protein kinase and induces cathepsin K
Circ. Res.
104
455-465
2009
Mus musculus
Manually annotated by BRENDA team
Hu, L.; Cheng, X.W.; Song, H.; Inoue, A.; Jiang, H.; Li, X.; Shi, G.P.; Kozawa, E.; Okumura, K.; Kuzuya, M.
Cathepsin K activity controls injury-related vascular repair in mice
Hypertension
63
607-615
2014
Mus musculus
Manually annotated by BRENDA team
Yuan, X.Y.; Ren, Z.; Wu, Y.; Bougault, C.; Brizuela, L.; Magne, D.; Buchet, R.; Mebarek, S.
Design, synthesis and biological evaluation of inhibitors of cathepsin K on dedifferentiated chondrocytes
Bioorg. Med. Chem.
27
1034-1042
2019
Homo sapiens (P43235), Homo sapiens, Mus musculus (P55097), Mus musculus
Manually annotated by BRENDA team