title: BACE inhibitors as potential drugs for the treatment of Alzheimer's disease: focus on bioactivity.
abstract: 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 Aβ amyloid peptide in the brain. This can be achieved, either by decreasing peptide production through inhibition of β-secretase (also known as BACE-1) or γ-secretase, or by interfering with Aβ aggregation, or by promoting Aβ clearance. Targeting BACE-1, the proteolytic enzyme that initiates Aβ 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.
authors.affiliation: Department of Pathology, and Mental Health Research institute, The University of Melbourne, Parkville VIC, Australia. gmevin@unimelb.edu.au
authors.forename: Genevieve
authors.initials: G
authors.lastname: Evin
authors.forename: Guillaume
authors.initials: G
authors.lastname: Lessene
authors.forename: Simon
authors.initials: S
authors.lastname: Wilkins
mesh_terms: D000544:Alzheimer Disease / Q000188:drug therapy* / Q000209:etiology / Q000473:pathology; D053829:Amyloid Precursor Protein Secretases / Q000037:antagonists & inhibitors*; D016282:Aspartic Acid Endopeptidases / Q000037:antagonists & inhibitors*; D006801:Humans; D010330:Patents as Topic; D011480:Protease Inhibitors / Q000627:therapeutic use*
chemical_list: D011480:Protease Inhibitors; D053829:Amyloid Precursor Protein Secretases; D016282:Aspartic Acid Endopeptidases; C509280:BACE1 protein, human