Molecular Classification
Enzyme, Pepsin family/aspartic proteases, Type I transmembrane protein
Other Names
β-secretase, beta-site APP cleaving enzyme 1, membrane-associated aspartic protease 2, memapsin-2, aspartyl protease 2, ASP2
Disease Roles
Alzheimer’s diseaseNeurodegenerative diseaseSchizophrenia (potential link)

Beta-site Amyloid Precursor Protein Cleaving Enzyme 1 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.

Mechanism of Action

Inhibition of BACE1 enzymatic activity, preventing Aβ production

Biological Functions

Cleavage of APP
Aβ peptide generation
Myelination regulation
Synaptic function
Neural development
Neuregulin 1 cleavage

Disease Associations

Alzheimer’s disease
Neurodegenerative disease
Schizophrenia (potential link)
Cognitive deficits

Safety Considerations

  • Off-target effects due to cleavage of other substrates
  • Potential cognitive side effects
  • Myelination-related side effects

Interacting Drugs

BACE1 inhibitors (small-molecule)

Associated Biomarkers

Biomarker
Aβ40/42 levels
BACE1 activity levels