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Literature summary for 3.4.22.38 extracted from

  • Kometani, M.; Nonomura, K.; Tomoo, T.; Niwa, S.
    Hurdles in the drug discovery of cathepsin K inhibitors (2010), Curr. Top. Med. Chem., 10, 733-744.
    View publication on PubMed
Search for more literature for 3.4.22.38

Inhibitors

Inhibitors Comment Organism Structure
L-873724
-
 Homo sapiens
odanacatib MK-0822 Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
lysosome
-
 Homo sapiens 5764
-

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
Elastin + H2O Homo sapiens the preferred cleavage site is at Pro-Xaa-Gly ?
-
 ?
kinin + H2O Homo sapiens
-
 ?
-
 ?
Type I collagen + H2O Homo sapiens cleavage sites in type I collagen are telopeptides and multiple sites in triple helix ?
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
macrophage
-
 Homo sapiens
-
osteoclast
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
benzyloxycarbonyl-Gly-L-Pro-L-Arg-7-amido-4-methylcoumarin + H2O
-
 Homo sapiens benzyloxycarbonyl-Gly-L-Pro-L-Arg + 7-amino-4-methylcoumarin
-
 ?
Elastin + H2O the preferred cleavage site is at Pro-Xaa-Gly Homo sapiens ?
-
 ?
kinin + H2O
-
 Homo sapiens ?
-
 ?
Type I collagen + H2O cleavage sites in type I collagen are telopeptides and multiple sites in triple helix Homo sapiens ?
-
 ?

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
6.1
-
-
 Homo sapiens

pH Range

pH Minimum pH Maximum Comment Organism
5.5 7.5
-
 Homo sapiens

pH Stability

pH Stability pH Stability Maximum Comment Organism
5.5 7.5 91% residual activity at pH 5.5, 85% residual activity at pH 6.5, and 11% residual activity at pH 7.5 (at 37°C after 30 min) Homo sapiens

General Information

General Information Comment Organism
physiological function cathepsin K has a pivotal function in bone matrix degradation Homo sapiens

kcat/KM [mM/s]

kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
118.8
-
 benzyloxycarbonyl-Gly-L-Pro-L-Arg-7-amido-4-methylcoumarin pH and temperature not specified in the publication Homo sapiens