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Literature summary extracted from

  • Williams, A.S.; Eynott, P.R.; Leung, S.Y.; Nath, P.; Jupp, R.; De Sanctis, G.T.; Resnick, R.; Adcock, I.M.; Chung, K.F.
    Role of cathepsin S in ozone-induced airway hyperresponsiveness and inflammation (2009), Pulm. Pharmacol. Ther., 22, 27-32.
    View publication on PubMed

Activating Compound

EC Number Activating Compound Comment Organism Structure
3.4.22.27 Ozone cathepsin S levels peak 3 h after ozone exposure in bronchoalveolar lavage cells Mus musculus
3.4.22.27 TNF-alpha cathepsin S can be upregulated by TNF-alpha in endothelial cells and cathepsin S induces endothelial cell motility, invasion and migration Mus musculus

Application

EC Number Application Comment Organism
3.4.22.27 drug development important role for cathepsin S in the regulation of ozone-induced airway hyperresponsiveness and neutrophil cell recruitment, cathepsin S may be a target in the treatment of oxidative stress-induced airway hyperresponsiveness and inflammation Mus musculus

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.22.27 4-morpholinecarboxamide, N-[(1R)-2-[[(1S)-1-(2-benzoxazolylcarbonyl) propyl] amino]-1-[[(cyclopropylmethyl)-sulfonyl]methyl]-2-oxoethyl] previously reported as 05141, ihbitor-dosed mice are protected against ozone-induced airway hyperresponsiveness Mus musculus
3.4.22.27 additional information effect of cathepsin S inhibition on bronchoalveolar lavage fluid cytokines: inhibition reduces ozone-induced interleukin-6 levels at 3 h and 20-24 h and TNF-alpha levels are inhibited at 20-24 h Mus musculus

Organism

EC Number Organism UniProt Comment Textmining
3.4.22.27 Mus musculus
-
 6-8 week-old male BALB/c mice
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.4.22.27 bronchoalveolar lavage
-
 Mus musculus
-
3.4.22.27 dendritic cell
-
 Mus musculus
-
3.4.22.27 heart
-
 Mus musculus
-
3.4.22.27 lung
-
 Mus musculus
-
3.4.22.27 macrophage
-
 Mus musculus
-
3.4.22.27 spleen
-
 Mus musculus
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.4.22.27 Z-Val-Val-Arg-7-amido-4-methylcoumarin + H2O
-
 Mus musculus Z-Val-Val-Arg + 7-amino-4-methylcoumarin
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.4.22.27 cathepsin S
-
 Mus musculus

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.4.22.27 0.00000064
-
 4-morpholinecarboxamide, N-[(1R)-2-[[(1S)-1-(2-benzoxazolylcarbonyl) propyl] amino]-1-[[(cyclopropylmethyl)-sulfonyl]methyl]-2-oxoethyl] excellent selectivity and activity for cathepsin S over the other cathepsin family members L, K and B Mus musculus