Literature summary for 3.4.22.38 extracted from

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 (2008), Science, 319, 624-627.

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Application

Application	Comment	Organism
medicine	the results suggest that cathepsin K plays an important role in the immune system and serves as a valid therapeutic target in autoimmune diseases	Mus musculus
medicine	the results suggest that cathepsin K plays an important role in the immune system and serves as a valid therapeutic target in autoimmune diseases	Rattus norvegicus

Protein Variants

Protein Variants	Comment	Organism
additional information	targeted disruption of cathepsin K results in defective Toll-like receptor 9 signaling in dendritic cells in response to unmethylated CpG DNA, which in turn leads to an attenuated induction of T helper 17 cells, without affecting the antigen-presenting ability of dendritic cells	Mus musculus

Inhibitors

Inhibitors	Comment	Organism	Structure
(2S,3S)-3-([(1S)-3-methyl-1-[(2-methylpropoxy)methyl]butyl]carbamoyl)oxirane-2-carboxylate	through screening, a potent orally active cathepsin K inhibitor named NC-2300 is obtained, which suppresses autoimmune inflammation of the joints as well as osteoclastic bone resorption in an adjuvant-induced arthritis animal model in rats. Computer-assisted simulation of the cathepsin K/NC-2300 complex indicates that NC-2300 blocks the active-site cleft where Cys25 and His162 of cathepsin K form the catalytic site. Pharmacological inhibition of cathepsin K results in defective Toll-like receptor 9 signaling in dendritic cells in response to unmethylated CpG DNA, which in turn leads to an attenuated induction of T helper 17 cells, without affecting the antigen-presenting ability of dendritic cells	Rattus norvegicus

Organism

Organism	UniProt	Comment	Textmining
Mus musculus	-	-	-
Rattus norvegicus	-	-	-

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg]	Specific Activity Maximum [µmol/min/mg]	Comment	Organism
additional information	-	cathepsin K activity is confirmed in dendritic cells	Rattus norvegicus

Synonyms

Synonyms	Comment	Organism
cathepsin K	-	Mus musculus
cathepsin K	-	Rattus norvegicus

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Release 2023.1 (January 2023)