Aricept Complexed with Acetylcholinesterase
From Proteopedia
(Difference between revisions)
| Line 2: | Line 2: | ||
[[Image:E2020_interactins_in_AChE_gorge.jpg|left|250px]]<br /> | [[Image:E2020_interactins_in_AChE_gorge.jpg|left|250px]]<br /> | ||
'''3D structure of anti-Alzheimer's drug, Aricept, complexed with acetylcholinesterase''' | '''3D structure of anti-Alzheimer's drug, Aricept, complexed with acetylcholinesterase''' | ||
| - | (see also [[AChE | + | (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 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 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. | 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 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. | ||
Current revision
| |||||||||||
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
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
