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Literature summary for 3.4.22.38 extracted from

  • Sharma, V.; Panwar, P.; O'Donoghue, A.J.; Cui, H.; Guido, R.V.; Craik, C.S.; Broemme, D.
    Structural requirements for the collagenase and elastase activity of cathepsin K and its selective inhibition by an exosite inhibitor (2015), Biochem. J., 465, 163-173.
    View publication on PubMed
Search for more literature for 3.4.22.38

Application

Application Comment Organism
medicine human cathepsinK is a major drug target for the treatment of osteoporosis Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Pichia pastoris Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
4-dihydrotanshinone potent exosite inhibitor of cathepsin K Homo sapiens
E-64 i.e. trans-epoxysuccinyl-L-leucylamido(4-guanidino)butane Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0094
-
 carbobenzoxy-Phe-Arg-7-amido-4-methylcoumarin at pH 5.5 and 37°C Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
bradykinin + H2O Homo sapiens
-
 ?
-
 ?
Collagen type I + H2O Homo sapiens
-
 ?
-
 ?
Elastin + H2O Homo sapiens
-
 ?
-
 ?
tissue growth factor beta1 + H2O Homo sapiens
-
 ?
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens P43235
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
bradykinin + H2O
-
 Homo sapiens ?
-
 ?
carbobenzoxy-Phe-Arg-7-amido-4-methylcoumarin + H2O
-
 Homo sapiens carbobenzoxy-Phe-Arg + 7-amino-4-methylcoumarin
-
 ?
Collagen type I + H2O
-
 Homo sapiens ?
-
 ?
Elastin + H2O
-
 Homo sapiens ?
-
 ?
tissue growth factor beta1 + H2O
-
 Homo sapiens ?
-
 ?

Synonyms

Synonyms Comment Organism
catK
-
 Homo sapiens

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
17
-
 carbobenzoxy-Phe-Arg-7-amido-4-methylcoumarin at pH 5.5 and 37°C Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0113
-
 with elastin as substrate, at pH 5.5 and 37°C Homo sapiens 4-dihydrotanshinone
0.015
-
 with collagen type I as substrate, at pH 5.5 and 37°C Homo sapiens 4-dihydrotanshinone

kcat/KM [mM/s]

kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
1800
-
 carbobenzoxy-Phe-Arg-7-amido-4-methylcoumarin at pH 5.5 and 37°C Homo sapiens