Application

Human β-secretase or BACE1 has been used to study the binding reaction between amyloid precursor protein and β-secretase. It has also been used in BACE1 assay.

Biochem/physiol Actions

BACE1 (β-site APP-cleaving enzyme 1) is a transmembrane aspartyl protease responsible for cleaving the amyloid precursor protein (APP). BACE1-mediated cleavage of amyloid precursor protein (APP) is the first step during the generation of pathogenic amyloid-β peptides, hence making it the major drug target for Alzheimer′s disease (AD). Increased levels of enzymatic activity of BACE1 was found in cerebrospinal fluid from patients having both mild cognitive impairment (MCI) and AD, thereby suggesting the importance of BACE1 enzymatic activity in conversion of MCI to AD.

BACE1 (β−Secretase or β−Site APP-Cleaving Enzyme) is a transmembrane protease responsible for the β site cleavage of the amyloid precursor protein (APP) to produce amyloid β peptide (Aβ). The accumulation of Aβ in the brain is a primary cause for the progression of Alzheimer′s, therefore BACE1 is a target for inhibitor drug discovery.

Physical form

Solution in 20 mM Hepes, pH 7.4, 125 mM NaCl.

Unit Definition

One unit will hydrolyze 1.0 picomole of 7-methoxycoumarin-4-acetyl-[Asn⁶⁷⁰, Leu⁶⁷¹]-Amyloid β/A4 Precursor Protein 770 Fragment 667-676-(2,4-dinitrophenyl)-Lys-Arg-Arg amide substrate per 1 minute at pH 4.5 at 37 °C.