The potential for BACE1 inhibitors in the treatment of Alzheimer's disease.

摘要

Alzheimer's disease (AD) is a debilitating neurodegenerative disease of the elderly characterized by the loss of memory and other cognitive functions. Currently marketed drugs for the treatment of this disease only offer symptomatic relief, and, consequently, there is a large unmet clinical need for disease-modifying therapies for the treatment of AD. Substantial research efforts are focused on inhibiting the proteases involved in the generation of the amyloidogenic beta-amyloid (A beta) peptide. One of these key proteases, beta-secretase, was identified as a novel transmembrane aspartic protease and named BACE1. Due to its pivotal role in A beta production, many pharmaceutical companies are actively pursuing the challenging task of developing BACE1 inhibitors for evaluation in the clinic.