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Literature summary extracted from

  • Broemme, D.; Lecaille, F.
    Cathepsin K inhibitors for osteoporosis and potential off-target effects (2009), Expert Opin. Investig. Drugs, 18, 585-600.
    View publication on PubMedView publication on EuropePMC

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.22.38 balicatib potent human cathepsin K inhibitor with a high selectivity against human cathepsins B, L and S (> 4800fold, > 500fold and > 65000fold, respectively) Homo sapiens
3.4.22.38 E-64
-
 Homo sapiens
3.4.22.38 MIV-701/710
-
 Homo sapiens
3.4.22.38 MSX-081
-
 Homo sapiens
3.4.22.38 MV061194 selective, potent reversible cathepsin K inhibitor Homo sapiens
3.4.22.38 MV061645
-
 Homo sapiens
3.4.22.38 MV061748
-
 Homo sapiens
3.4.22.38 MV061940
-
 Homo sapiens
3.4.22.38 odanacatib formely MK-0822 Homo sapiens
3.4.22.38 relicatib also known as SB-462795, highly potent human cathepsin K inhibitor Homo sapiens

Localization

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

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
3.4.22.38 Collagen + H2O Homo sapiens cathepsin K cleaves within the telo as well as triple helical domains of collagens ?
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
3.4.22.38 Homo sapiens
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.4.22.38 chondrocyte
-
 Homo sapiens
-
3.4.22.38 epithelial cell
-
 Homo sapiens
-
3.4.22.38 fetus
-
 Homo sapiens
-
3.4.22.38 fibroblast
-
 Homo sapiens
-
3.4.22.38 lung
-
 Homo sapiens
-
3.4.22.38 macrophage
-
 Homo sapiens
-
3.4.22.38 osteoclast predominant expression in osteoclasts Homo sapiens
-
3.4.22.38 respiratory epithelium
-
 Homo sapiens
-
3.4.22.38 smooth muscle cell
-
 Homo sapiens
-
3.4.22.38 synovial fibroblast
-
 Homo sapiens
-
3.4.22.38 thyroid epithelial cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.4.22.38 Collagen + H2O cathepsin K cleaves within the telo as well as triple helical domains of collagens Homo sapiens ?
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.4.22.38 cathepsin O initial name Homo sapiens
3.4.22.38 Cathepsin O2 initial name Homo sapiens
3.4.22.38 catK
-
 Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.4.22.38 0.000000041
-
 relicatib apparent value, pH and temperature not specified in the publication Homo sapiens
3.4.22.38 0.0000025
-
 MV061194 pH and temperature not specified in the publication Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.4.22.38 0.0000002
-
 pH and temperature not specified in the publication Homo sapiens odanacatib
3.4.22.38 0.0000014
-
 pH and temperature not specified in the publication Homo sapiens balicatib

General Information

EC Number General Information Comment Organism
3.4.22.38 physiological function cathepsin K plays a role in skeletal development/bone turnover, lung homeostasis, skin homeostasis during scar formation, amyloidosis, thyroid carcinoma, artherosclerosis/cardiovascular disease, breast carcinoma, lung adenocarcinoma, osteoporosis, prostate cancer, bone metastases, obesity, rheumatoid arthritis, osteoarthritis, melanoma, memory disorders, lung inflammation/fibrosis, and pycndysostosis Homo sapiens