title: [BACE1 inhibitors for the treatment of Alzheimer disease].
abstract: β-Site amyloid precursor protein cleaving enzyme 1 (BACEl) is the enzyme required for the production of the amyloid-β peptide(Aβ), which is associated with Alzheimer disease (AD). BACEl has emerged as a prime molecular target for reducing the brain Aβ levels. Recently, several BACEl inhibitors have been developed in clinical trials to test the efficacy in AD patients and individuals with prodromal AD. However, identification of BACE1 substrates and phenotypes of Bace1 knockout mice have raised concerns regarding potential mechanism-based adverse effects. This review summarizes the current status of the development of BACE1 inhibitors and the evaluation of their therapeutic potential against AD.
authors.forename: Taisuke
authors.initials: T
authors.lastname: Tomita
mesh_terms: D000544:Alzheimer Disease / Q000188:drug therapy* / Q000201:enzymology; D053829:Amyloid Precursor Protein Secretases / Q000037:antagonists & inhibitors*; D016229:Amyloid beta-Peptides / Q000378:metabolism; D000818:Animals; D016282:Aspartic Acid Endopeptidases / Q000037:antagonists & inhibitors*; D002986:Clinical Trials as Topic; D015195:Drug Design; D005182:Flavin-Adenine Dinucleotide / Q000378:metabolism; D006801:Humans; D011480:Protease Inhibitors / Q000627:therapeutic use
chemical_list: D016229:Amyloid beta-Peptides; D011480:Protease Inhibitors; D005182:Flavin-Adenine Dinucleotide; D053829:Amyloid Precursor Protein Secretases; D016282:Aspartic Acid Endopeptidases; C509280:BACE1 protein, human