Aricept Complexed with Acetylcholinesterase
From Proteopedia
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THREE DIMENSIONAL STRUCTURE OF THE ANTI-ALZHEIMER DRUG, E2020 (ARICEPT), COMPLEXED WITH ITS TARGET ACETYLCHOLINESTERASE
Overview
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 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].
Reference
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
Page seeded by OCA on Tue Oct 30 15:11:28 2007
Proteopedia Page Contributors and Editors (what is this?)
Eran Hodis, Joel L. Sussman, Jaime Prilusky, Alexander Berchansky, OCA, Michal Harel, David Canner, Wayne Decatur, Pham Ngoc Phuong, Angel Herraez, Lucie Kolarova
