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Literature summary for 3.4.22.1 extracted from

  • Hook, V.Y.; Kindy, M.; Hook, G.
    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.
    View publication on PubMed
Search for more literature for 3.4.22.1

Application

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

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

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

Localization Comment Organism GeneOntology No. Textmining
secretory vesicle regulated Mus musculus 99503
-

Natural Substrates/ Products (Substrates)

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

Organism UniProt Comment Textmining
Mus musculus
-
 London APP mice and C57BL/6 mice
-

Source Tissue

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 and Products (Substrate)

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 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