Target intelligence / Profile preview

Beta-site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1)

Target
BACE1
Molecular classification
Enzyme, Pepsin family/aspartic proteases, Type I transmembrane protein
01

Overview

BACE1 is a transmembrane aspartyl protease responsible for the initial cleavage of amyloid precursor protein (APP) at the β-secretase site. This cleavage initiates the production of amyloid-beta peptides (Aβ), which are central to Alzheimer's disease pathology. BACE1 also plays a role in myelination and other neuronal functions, making it a challenging drug target due to potential off-target effects.

Other names
β-secretasebeta-site APP cleaving enzyme 1membrane-associated aspartic protease 2memapsin-2aspartyl protease 2ASP2
02

Mechanism of action

Inhibition of BACE1 enzymatic activity, preventing Aβ production

03

Biological functions

Cleavage of APPAβ peptide generationMyelination regulationSynaptic functionNeural developmentNeuregulin 1 cleavage
04

Disease associations

Alzheimer’s diseaseNeurodegenerative diseaseSchizophrenia (potential link)Cognitive deficits
05

Safety considerations

Off-target effects due to cleavage of other substratesPotential cognitive side effectsMyelination-related side effects
06

Interacting drugs

BACE1 inhibitors (small-molecule)
07

Biomarkers

Aβ40/42 levelsBACE1 activity levels

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