Aricept Complexed with Acetylcholinesterase
THREE DIMENSIONAL STRUCTURE OF THE ANTI-ALZHEIMER DRUG, E2020 (ARICEPT), COMPLEXED WITH ITS TARGET ACETYLCHOLINESTERASE
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OverviewOverview
BACKGROUND: Several cholinesterase inhibitors are either being utilized, for symptomatic treatment of Alzheimer's disease or are in advanced, clinical trials. E2020, marketed as Aricept, is a member of a large family, of N-benzylpiperidine-based acetylcholinesterase (AChE) inhibitors, developed, synthesized and evaluated by the Eisai Company in Japan. These, inhibitors were designed on the basis of QSAR studies, prior to, elucidation of the three-dimensional structure of Torpedo californica AChE, (TcAChE). It significantly enhances performance in animal models of, cholinergic hypofunction and has a high affinity for AChE, binding to both, electric eel and mouse AChE in the nanomolar range. RESULTS: Our, experimental structure of the E2020-TcAChE complex pinpoints specific, interactions ... [(full description)]
About this StructureAbout this Structure
1EVE is a [Single protein] structure of sequence from [Torpedo californica] with NAG and E20 as [ligands]. The following page contains interesting information on the relation of 1EVE with [Acetylcholinesterase]. Active as [Acetylcholinesterase], with EC number [3.1.1.7]. Structure known Active Sites: CAT and IHB. Full crystallographic information is available from [OCA].
ReferenceReference
Structure of acetylcholinesterase complexed with E2020 (Aricept): implications for the design of new anti-Alzheimer drugs., Kryger G, Silman I, Sussman JL, Structure. 1999 Mar 15;7(3):297-307. PMID:10368299
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