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 β-amyloid (Aβ) aggregation process has been disclosed. We present here, for the first time, a direct evidence of the Aβ antiaggregating action of an AChE inhibitor (AP2238) purposely designed to bind at both the catalytic and the peripheral sites of the human enzyme.
Piazzi L., Rampa A., Bisi A., Gobbi S., Belluti F., Cavalli A., et al. (2003). 3-(4-{[benzyl(methyl)amino]methyl}-phenyl)-6,7-dimethoxy-2H-2-chromenone (AP2238) inhibits both acetylcholinesterase and acetylcholinesterase-induced β-amyloid aggregation: A dual function lead for Alzheimer's disease therapy. JOURNAL OF MEDICINAL CHEMISTRY, 46(12), 2279-2282 [10.1021/jm0340602].
3-(4-{[benzyl(methyl)amino]methyl}-phenyl)-6,7-dimethoxy-2H-2-chromenone (AP2238) inhibits both acetylcholinesterase and acetylcholinesterase-induced β-amyloid aggregation: A dual function lead for Alzheimer's disease therapy
Piazzi L.;Rampa A.;Bisi A.;Gobbi S.;Belluti F.;Cavalli A.;Bartolini M.;Andrisano V.;Valenti P.;Recanatini M.
2003
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 β-amyloid (Aβ) aggregation process has been disclosed. We present here, for the first time, a direct evidence of the Aβ antiaggregating action of an AChE inhibitor (AP2238) purposely designed to bind at both the catalytic and the peripheral sites of the human enzyme.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
