Application | Comment | Organism |
---|---|---|
medicine | cathepsin B inhibitors are effective therapeutic agents in treatment of Alzheimer's disease reducing the amyloid beta plaque load in brain regions by up to 55%, reducing the formation of amyloid beta 40 and amyloid beta 42 by 45% and 40%, and improving the memory function, overview | Mus musculus |
Protein Variants | Comment | Organism |
---|---|---|
additional information | inhibitors of cathepsin B improve memory and reduce beta-amyloid in transgenic Alzheimer disease mice expressing the wild-type, but not the Swedish mutant, beta-secretase site of the amyloid precursor protein | Mus musculus |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
E64c | - |
Mus musculus | |
E64d | - |
Mus musculus | |
N-(L-3-trans-propylcarbonyl-oxirane-2-carbonyl)-L-isoleucyl-L-proline | i.e. CA074 | Mus musculus | |
N-(L-3-trans-propylcarbonyl-oxirane-2-carbonyl)-L-isoleucyl-L-proline methyl ester | i.e. CA074Me | Mus musculus |
Localization | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|
secretory vesicle | regulated | Mus musculus | 99503 | - |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
amyloid beta precursor protein + H2O | Mus musculus | cathepsin B selectively cleaves the wild-type beta-secretase site but not the rare Swedish mutant beta-secretase site | ? | - |
? | |
additional information | Mus musculus | inhibitors of cathepsin B improve memory and reduce beta-amyloid in transgenic Alzheimer disease mice expressing the wild-type, but not the Swedish mutant, beta-secretase site of the amyloid precursor protein | ? | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Mus musculus | - |
London APP mice and C57BL/6 mice | - |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
brain | - |
Mus musculus | - |
hippocampus | - |
Mus musculus | - |
additional information | two mouse models of Alzheimer's Disease, consisting of one expressing human amyloid precursor protein containing the wild-type beta-secretase site and mutation at the beta-secretase site, London amyloid precursor protein mice, and the other expressing the Swe mutant beta-secretase site and the London mutation, Swedish/London amyloid precursor protein | Mus musculus | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
amyloid beta precursor protein + H2O | cathepsin B selectively cleaves the wild-type beta-secretase site but not the rare Swedish mutant beta-secretase site | Mus musculus | ? | - |
? | |
additional information | inhibitors of cathepsin B improve memory and reduce beta-amyloid in transgenic Alzheimer disease mice expressing the wild-type, but not the Swedish mutant, beta-secretase site of the amyloid precursor protein | Mus musculus | ? | - |
? | |
N-benzoyl-Val-Asn-Leu-7-amido-4-methylcoumarin + H2O | the substrate represents the wild-type beta-secretase site | Mus musculus | N-benzoyl-Val-Lys-Met + 7-amino-4-methylcoumarin | - |
? | |
N-benzoyl-Val-Lys-Met-7-amido-4-methylcoumarin + H2O | the substrate represents the wild-type beta-secretase site | Mus musculus | N-benzoyl-Val-Lys-Met + 7-amino-4-methylcoumarin | - |
? |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.0000003 | - |
- |
Mus musculus | E64c | |
0.000002 | - |
- |
Mus musculus | N-(L-3-trans-propylcarbonyl-oxirane-2-carbonyl)-L-isoleucyl-L-proline |