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Literature summary for 3.4.23.46 extracted from

  • Stockley, J.H.; Ravid, R.; ONeill, C.
    Altered beta-secretase enzyme kinetics and levels of both BACE1 and BACE2 in the Alzheimers disease brain (2006), FEBS Lett., 580, 6550-6560.
    View publication on PubMed
Search for more literature for 3.4.23.46

Inhibitors

Inhibitors Comment Organism Structure
KTEETSEVN(statine)VAEF i.e. P10-P40 StatVal, activity completely abolished using saturating dose of 2.1 microM of the inhibitor, cleavage products of beta-secretase measured by fluoresence assay Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
additional information
-
 additional information significant individual variations of Vmax and Km values determined, Vmax values found to be significantly increased in Alzheimer disease cases Homo sapiens

Molecular Weight [Da]

Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
additional information
-
 Western blot, closely spaced doublet of about 73-75 kDa identified, detection of lower molecular weight forms including a very light band detected at about 45 kDa, no cross-reactivity to BACE2 identified, major BACE1 immunoreactive band of about 75 kDa considered for comparative analysis Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
amyloid beta-precursor protein + H2O Homo sapiens
-
 ?
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens P56817
-
-

Source Tissue

Source Tissue Comment Organism Textmining
brain Alzheimer disease brain and control Homo sapiens
-

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
additional information
-
 dysregulation of BACE1 expression and activity measured in normal and Alzheimer brains, differences between BACE1 and BACE2 analyzed, kinetics of beta-secretase enzymatic activity in individual normal and Alzheimer brains shown, activity found to be saturable following Michaelis-Menten kinetics, increased Vmax of BACE1 in Alzheimer disease cases not found to be correlated with levels of BACE1, decreased BACE1 and BACE2 levels found to be correlated with severity of neurofibrillary pathology and synaptic loss in Alzheimer disease Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
((7-methoxycoumarin-4-yl)acetyl)-Ser-Glu-Val-Asn-Leu-Asp-Ala-Glu-Phe-Lys(2,4-dinitrophenyl) + H2O MCA, cleavage product measured by fluorescence assay, significant increases in beta-secretase activity to varying degrees in Alzheimer disease cases identified, increase not immediately correlated with levels of BACE1, differences between BACE1 and BACE2 analyzed Homo sapiens ((7-methoxycoumarin-4-yl)acetyl)-Ser-Glu-Val-Asn-Leu + Asp-Ala-Glu-Phe-Lys(2,4-dinitrophenyl)
-
 ?
amyloid beta-precursor protein + H2O
-
 Homo sapiens ?
-
 ?

Synonyms

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

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
 activity assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
4.5
-
 activity assay at Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.041
-
 i.e. P10-P40 StatVal, dose-dependent inhibition shown, cleavage determined by fluoresence assay Homo sapiens KTEETSEVN(statine)VAEF