BACE Inhibitors as Potential Drugs for the Treatment of Alzheimer's Disease: Focus on Bioactivity.

摘要

Current drug development for the treatment of Alzheimer's Disease is principally based on the amyloid cascade theory, and aims to reduce the levels of Abeta amyloid peptide in the brain. This can be achieved, either by decreasing peptide production through inhibition of beta-secretase (also known as BACE-1) or gamma-secretase, or by interfering with Abeta aggregation, or by promoting Abeta clearance. Targeting BACE-1, the proteolytic enzyme that initiates Abeta formation, has generated a lot of research interest recently and is currently thought to be one of the most promising therapeutic approaches. In this review, we summarize and discuss the latest patents and publications describing BACE-1 inhibitors, principally focussing on their drug properties and performance in preclinical trials.