Aricept Complexed with Acetylcholinesterase: Difference between revisions
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[[Image:E2020_AChE_overview.jpg|left|300px]]<br /> | [[Image:E2020_AChE_overview.jpg|left|300px]]<br /> | ||
'''3D Structure of anti-Alzheimer's drug, E2020 (ARICEPT), complexed with its target acetylcholinesterase'''<br /> | '''3D Structure of anti-Alzheimer's drug, E2020 (ARICEPT), complexed with its target acetylcholinesterase'''<br /> | ||
==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). 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). 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. | ||
<applet load="1eve" size="450" color="white" frame="true" align="right" spinBox="true" script="1eve/E2020_in_ache/5" /> | <applet load="1eve" size="450" color="white" frame="true" align="right" spinBox="true" script="1eve/E2020_in_ache/5" caption="1eve, resolution 2.50Å" /> | ||
==Results== | ==Results== | ||