Aricept Complexed with Acetylcholinesterase: Difference between revisions

Revision as of 16:06, 30 October 2007

THREE DIMENSIONAL STRUCTURE OF THE ANTI-ALZHEIMER DRUG, E2020 (ARICEPT), COMPLEXED WITH ITS TARGET ACETYLCHOLINESTERASE

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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Proteopedia Page Contributors and Editors (what is this?)Proteopedia Page Contributors and Editors (what is this?)

OCA, Joel L. Sussman, Eran Hodis, Wayne Decatur, Jaime Prilusky, Alexander Berchansky, David Canner, Lucie Kolarova, Pham Ngoc Phuong, Angel Herraez, Michal Harel

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	[[Category: serine hydrolase]]		[[Category: serine hydrolase]]

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