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Literature summary for 3.4.22.38 extracted from
- Cathepsin K inhibitors for osteoporosis and potential off-target effects (2009), Expert Opin. Investig. Drugs, 18, 585-600.
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| balicatib | potent human cathepsin K inhibitor with a high selectivity against human cathepsins B, L and S (> 4800fold, > 500fold and > 65000fold, respectively) | Homo sapiens |  |
| E-64 | - |
Homo sapiens | |
| MIV-701/710 | - |
Homo sapiens | |
| MSX-081 | - |
Homo sapiens | |
| MV061194 | selective, potent reversible cathepsin K inhibitor | Homo sapiens | |
| MV061645 | - |
Homo sapiens | |
| MV061748 | - |
Homo sapiens | |
| MV061940 | - |
Homo sapiens | |
| odanacatib | formely MK-0822 | Homo sapiens | |
| relicatib | also known as SB-462795, highly potent human cathepsin K inhibitor | 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. |
|---|---|---|---|---|---|---|
| Collagen + H2O | Homo sapiens | cathepsin K cleaves within the telo as well as triple helical domains of collagens | ? | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| chondrocyte | - |
Homo sapiens | - |
| epithelial cell | - |
Homo sapiens | - |
| fetus | - |
Homo sapiens | - |
| fibroblast | - |
Homo sapiens | - |
| lung | - |
Homo sapiens | - |
| macrophage | - |
Homo sapiens | - |
| osteoclast | predominant expression in osteoclasts | Homo sapiens | - |
| respiratory epithelium | - |
Homo sapiens | - |
| smooth muscle cell | - |
Homo sapiens | - |
| synovial fibroblast | - |
Homo sapiens | - |
| thyroid epithelial cell | - |
Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| Collagen + H2O | cathepsin K cleaves within the telo as well as triple helical domains of collagens | Homo sapiens | ? | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| cathepsin O | initial name | Homo sapiens |
| Cathepsin O2 | initial name | Homo sapiens |
| catK | - |
Homo sapiens |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.000000041 | - |
relicatib | apparent value, pH and temperature not specified in the publication | Homo sapiens | |
| 0.0000025 | - |
MV061194 | pH and temperature not specified in the publication | Homo sapiens | |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.0000002 | - |
pH and temperature not specified in the publication | Homo sapiens | odanacatib | |
| 0.0000014 | - |
pH and temperature not specified in the publication | Homo sapiens | balicatib | |
General Information
| General Information | Comment | Organism |
|---|---|---|
| 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 |
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