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Literature summary for 3.4.22.38 extracted from

  • Podgorski, I.
    Future of anticathepsin K drugs: dual therapy for skeletal disease and atherosclerosis? (2009), Future Med. Chem., 1, 21-34.
    View publication on PubMedView publication on EuropePMC

Application

Application Comment Organism
medicine cathepsin K is associated with skeletal and cardiovascular disorders, cathepsin K is a pharmaceutical industry target for treatment of osteoporosis Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
AFG-495
-
Homo sapiens
balicatib
-
Homo sapiens
L-873724 has a greater than 800fold selectivity over other cysteine cathepsins Homo sapiens
MIV-701
-
Homo sapiens
odabnacatib MK-0822 Homo sapiens
ONO-5334
-
Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
aggrecan + H2O Homo sapiens
-
?
-
?
Collagen type I + H2O Homo sapiens
-
?
-
?
collagen type II + H2O Homo sapiens
-
?
-
?
kinin + H2O Homo sapiens
-
?
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
cartilage osteoarthritic cartilage Homo sapiens
-
gastric mucosa inflamed gastric mucosa Homo sapiens
-
lung inflamed lung tissues Homo sapiens
-
macrophage
-
Homo sapiens
-
osteoclast expressed selectively in the osteoclast Homo sapiens
-
rheumatoid arthritis disease specific giant cell
-
Homo sapiens
-
serum
-
Homo sapiens
-
synovial fibroblast
-
Homo sapiens
-
synovial tissue inflamesynovial tissue associated with rheumatoid arthritis Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
aggrecan + H2O
-
Homo sapiens ?
-
?
Collagen type I + H2O
-
Homo sapiens ?
-
?
collagen type II + H2O
-
Homo sapiens ?
-
?
kinin + H2O
-
Homo sapiens ?
-
?

Expression

Organism Comment Expression
Homo sapiens increased expression of cathepsin K in tumors and tumor-associated cells may be a direct result of transcriptional regulation by ETS family members up

General Information

General Information Comment Organism
physiological function cathepsin K is the major enzyme involved in bone resorption, associated with obesity and inflammation, major contributor to skeletal and vascular health, Cathepsin K plays a functional role in atherogenesis Homo sapiens