title: 3-(4-[[Benzyl(methyl)amino]methyl]phenyl)-6,7-dimethoxy-2H-2-chromenone (AP2238) inhibits both acetylcholinesterase and acetylcholinesterase-induced beta-amyloid aggregation: a dual function lead for Alzheimer's disease therapy.
abstract: In recent years, the investigation of acetylcholinesterase (AChE) inhibitors has gained further interest, because the involvement of the peripheral site of the enzyme in the beta-amyloid (Abeta) aggregation process has been disclosed. We present here, for the first time, a direct evidence of the Abeta antiaggregating action of an AChE inhibitor (AP2238) purposely designed to bind at both the catalytic and the peripheral sites of the human enzyme.
authors.affiliation: Department of Pharmaceutical Sciences, University of Bologna, Via Belmeloro 6, Italy.
authors.forename: Lorna
authors.initials: L
authors.lastname: Piazzi
authors.forename: Angela
authors.initials: A
authors.lastname: Rampa
authors.forename: Alessandra
authors.initials: A
authors.lastname: Bisi
authors.forename: Silvia
authors.initials: S
authors.lastname: Gobbi
authors.forename: Federica
authors.initials: F
authors.lastname: Belluti
authors.forename: Andrea
authors.initials: A
authors.lastname: Cavalli
authors.forename: Manuela
authors.initials: M
authors.lastname: Bartolini
authors.forename: Vincenza
authors.initials: V
authors.lastname: Andrisano
authors.forename: Piero
authors.initials: P
authors.lastname: Valenti
authors.forename: Maurizio
authors.initials: M
authors.lastname: Recanatini
mesh_terms: D000110:Acetylcholinesterase / Q000737:chemistry*; D000122:Acetylthiocholine / Q000737:chemistry; D000544:Alzheimer Disease / Q000188:drug therapy; D016229:Amyloid beta-Peptides / Q000737:chemistry*; D001578:Benzopyrans / Q000138:chemical synthesis* / Q000737:chemistry; D001596:Benzylamines / Q000138:chemical synthesis* / Q000737:chemistry; D002091:Butyrylcholinesterase / Q000737:chemistry; D020134:Catalytic Domain; D002800:Cholinesterase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry; D003374:Coumarins / Q000138:chemical synthesis* / Q000737:chemistry; D005470:Fluorometry; D006801:Humans; D006868:Hydrolysis; D008958:Models, Molecular; D013329:Structure-Activity Relationship
chemical_list: C475423:AP 2238; D016229:Amyloid beta-Peptides; D001578:Benzopyrans; D001596:Benzylamines; D002800:Cholinesterase Inhibitors; D003374:Coumarins; D000122:Acetylthiocholine; D000110:Acetylcholinesterase; D002091:Butyrylcholinesterase