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Literature summary for 3.4.23.46 extracted from
- 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 (2008), J. Biol. Chem., 283, 7745-7753.
Application
| Application | Comment | Organism |
|---|---|---|
| pharmacology | treatment of London APP transgenic mouse model of Alzheimer's disease that expresses human amyloid precursor protein containing the wild-type beta-secretase site with inhibitors CA074Me or E64d results in substantial improvement in memory deficit assessed by the Morris water maze test. Improved memory function is accompanied by reduced amyloid plaque load, decreased amyloid beta40 and amyloid beta42, and reduced C-terminal beta-secretase fragment derived from amyloid precursor protein by beta-secretase. Inhibitor hHas no effects on any of these parameters in mice expressing the Swedish mutant beta-secretase site of amyloid precursor protein | Mus musculus |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| CA074Me | treatment of London APP transgenic mouse model of Alzheimer's disease that expresses human amyloid precursor protein containing the wild-type beta-secretase site results in substantial improvement in memory deficit assessed by the Morris water maze test. Improved memory function is accompanied by reduced amyloid plaque load, decreased amyloid beta40 and amyloid beta42, and reduced C-terminal beta-secretase fragment derived from amyloid precursor protein by beta-secretase. Inhibitor has no effects on any of these parameters in mice expressing the Swedish mutant beta-secretase site of amyloid precursor protein | Mus musculus |  |
| E64d | treatment of London APP transgenic mouse model of Alzheimer's disease that expresses human amyloid precursor protein containing the wild-type beta-secretase site results in substantial improvement in memory deficit assessed by the Morris water maze test. Improved memory function is accompanied by reduced amyloid plaque load, decreased amyloid beta40 and amyloid beta42, and reduced C-terminal beta-secretase fragment derived from amyloid precursor protein by beta-secretase. Inhibitor has no effects on any of these parameters in mice expressing the Swedish mutant beta-secretase site of amyloid precursor protein | Mus musculus | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Mus musculus | - |
- |
- |
| Mus musculus | - |
London APP transgenic mouse model of Alzheimer's disease that expresses human amyloid precursor protein containing the wild-type beta-secretase site | - |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| brain | - |
Mus musculus | - |
Specific Activity [micromol/min/mg]
| Specific Activity Minimum [µmol/min/mg] | Specific Activity Maximum [µmol/min/mg] | Comment | Organism |
|---|---|---|---|
| 0.01 | - |
using Z-Val-Asn-Leu-7-amido-4-methylcoumarin as substrate | Mus musculus |
| 0.02 | - |
- |
Mus musculus |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| additional information | BACE 1 does not cleave Z-Val-Lys-Met-7-amido-4-methylcoumarin | Mus musculus | ? | - |
? | |
| Z-Val-Asn-Leu-7-amido-4-methylcoumarin + H2O | - |
Mus musculus | Z-Val-Asn-Leu + 7-amino-4-methylcoumarin | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| BACE 1 | - |
Mus musculus |
| beta-secretase | - |
Mus musculus |
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Release 2023.1 (January 2023)
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