Sandbox E20
From Proteopedia
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(see also [[AChE inhibitors and substrates]]) | (see also [[AChE inhibitors and substrates]]) | ||
==Background== | ==Background== | ||
| - | Several cholinesterase inhibitors are either being utilized for symptomatic treatment of Alzheimer's disease or are in | + | Several cholinesterase inhibitors are either being utilized for symptomatic treatment of Alzheimer's disease or are in advance 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 3D structure of ''Torpedo californica'' AChE (''Tc''AChE) ([[1ea5]]). 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. |
{{Clear}} | {{Clear}} | ||
Revision as of 19:59, 20 January 2022
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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
