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Literature summary for 3.4.22.27 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
Search for more literature for 3.4.22.27

Activating Compound

Activating Compound Comment Organism Structure
Ozone cathepsin S levels peak 3 h after ozone exposure in bronchoalveolar lavage cells Mus musculus
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

Application Comment Organism
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

Inhibitors Comment Organism Structure
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
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

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

Source Tissue

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

Substrates and Products (Substrate)

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

Synonyms

Synonyms Comment Organism
cathepsin S
-
 Mus musculus

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
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