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Literature summary for 3.4.21.B25 extracted from

  • Malfait, A.M.; Arner, E.C.; Song, R.H.; Alston, J.T.; Markosyan, S.; Staten, N.; Yang, Z.; Griggs, D.W.; Tortorella, M.D.
    Proprotein convertase activation of aggrecanases in cartilage in situ (2008), Arch. Biochem. Biophys., 478, 43-51.
    View publication on PubMed
Search for more literature for 3.4.21.B25

Application

Application Comment Organism
medicine PACE4 represents a target for the development of osteoarthritis therapeutics Rattus norvegicus

Inhibitors

Inhibitors Comment Organism Structure
decanoyl-RVKR-chloromethyl ketone
-
 Rattus norvegicus

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.251
-
 benzyloxycarbonyl-REKR-7-amido-4-trifluoromethylcoumarin
-
 Rattus norvegicus

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
additional information Rattus norvegicus PACE4 is identified as a proprotein convertase responsible for activation of aggrecanases in osteoarthritic and cytokine-stimulated cartilage ?
-
 ?

Organism

Organism UniProt Comment Textmining
Rattus norvegicus Q78EH2
-
-

Source Tissue

Source Tissue Comment Organism Textmining
cartilage presence of PACE4 protein is restricted to chondrocytes of healthy cartilage, whereas the expression is increased in osteoarthritis cartilage Rattus norvegicus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
benzyloxycarbonyl-REKR-7-amido-4-trifluoromethylcoumarin + H2O
-
 Rattus norvegicus ?
-
 ?
additional information PACE4 is identified as a proprotein convertase responsible for activation of aggrecanases in osteoarthritic and cytokine-stimulated cartilage Rattus norvegicus ?
-
 ?
proADAMTS-4 + H2O recombinant PACE4 activates proADAMTS-4 by removal of the prodomain Rattus norvegicus ?
-
 ?
proADAMTS-5 + H2O recombinant PACE4 activates proADAMTS-5 by removal of the prodomain Rattus norvegicus ?
-
 ?