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Literature summary for 3.4.23.46 extracted from

  • Ahmed, R.R.; Holler, C.J.; Webb, R.L.; Li, F.; Beckett, T.L.; Murphy, M.P.
    BACE1 and BACE2 enzymatic activities in Alzheimer’s disease (2010), J. Neurochem., 112, 1045-1053.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.4.23.46

Application

Application Comment Organism
medicine samples from frontal cortex of both Alzheimer's disease-affected individuals and age-matched controls. BACE1 activity shows a significant positive correlation with the amount of extractable amyloid beta-peptide, and BACE1 protein and activity are significantly increased in cases of alzheimer's disease Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
N-((1S,2R)-1-benzyl-3-cyclopropylamino-2-hydroxy-propyl)-5-(methanesulfonyl-methyl-amino)-N'-((R)-1-phenyl-ethyl)-isophthalamide beta-secretase inhibitor IV Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
endosome
-
 Homo sapiens 5768
-
Golgi apparatus
-
 Homo sapiens 5794
-

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
amyloid precursor protein + H2O Homo sapiens BACE1 cleaves amyloid precursor protein at the beta-site fragments of amyloid precursor protein
-
 ?
amyloid precursor protein-DELTANL + H2O Homo sapiens the Swedish familial mutation in APP (DELTANL) enhances beta-secretase cleavage ?
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
brain high expression Homo sapiens
-
cerebral cortex samples from frontal cortex of both Alzheimer's disease-affected individuals and age-matched controls. BACE1 activity shows a significant positive correlation with the amount of extractable amyloid beta-peptide, and BACE1 protein and activity are significantly increased in cases of alzheimer's disease Homo sapiens
-
neuron
-
 Homo sapiens
-
pancreas high expression Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
amyloid precursor protein + H2O BACE1 cleaves amyloid precursor protein at the beta-site Homo sapiens fragments of amyloid precursor protein
-
 ?
amyloid precursor protein-DELTANL + H2O the Swedish familial mutation in APP (DELTANL) enhances beta-secretase cleavage Homo sapiens ?
-
 ?

Synonyms

Synonyms Comment Organism
BACE1
-
 Homo sapiens
beta-secretase
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000015
-
 pH and temperature not specified in the publication Homo sapiens N-((1S,2R)-1-benzyl-3-cyclopropylamino-2-hydroxy-propyl)-5-(methanesulfonyl-methyl-amino)-N'-((R)-1-phenyl-ethyl)-isophthalamide

Expression

Organism Comment Expression
Homo sapiens BACE1 activity is substantially increased in the superior frontal gyrus in AlzheimerÂ’s disease cases up

General Information

General Information Comment Organism
physiological function BACE1 is the principle beta-secretase responsible for the production of beta-amyloid in the brain Homo sapiens