Aricept Complexed with Acetylcholinesterase (Czech)

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(New page: <StructureSection load='1eve' size='450' side='right' scene='29/2908/1eve_e20_cartoon/1' caption=''> 250px<br /> '''3D structure of anti-...)
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<StructureSection load='1eve' size='450' side='right' scene='29/2908/1eve_e20_cartoon/1' caption=''>
<StructureSection load='1eve' size='450' side='right' scene='29/2908/1eve_e20_cartoon/1' caption=''>
[[Image:E2020_interactins_in_AChE_gorge.jpg|left|250px]]<br />
[[Image:E2020_interactins_in_AChE_gorge.jpg|left|250px]]<br />
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'''3D structure of anti-Alzheimer's drug, Aricept, complexed with acetylcholinesterase'''
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'''3D struktura léčiva Aricept (na Alzheimerovu chorobu), komplex s acetylcholinesterasou'''
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(see also [[AChE bivalent inhibitors (Part II)]])
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(viz též [[AChE bivalent inhibitors (Part II)]])
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==Background==
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==Úvod==
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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.
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Několik inhibitorů cholinesteráz se buď již využívají k léčení symptomů Alzheimerovy choroby, nebo jsou v pokročilých stádiích klinických studií. '''E2020''', označována jako '''Aricept''', je členem velké rodiny inhibitorů acetylcholinesterázy ([[acetylcholinesterase]]) (AChE) založených na N-benzylpiperidinu. Byl vyvinut, syntetizován a ověřen japonskou firmou Eisai Company. Tyto inhibitory byly vytvořeny na základě QSAR studií provedených ještě před určením 3D struktury acetylcholinesterázy ''Torpedo californica'' (''Tc'' AChE) ([[lea5]]). Má výrazné účinky na modelových zvířatech s cholinergickou hypofunkcí a má vysokou afinitu k AChE - váže se jak k AChE elektrického úhoře, tak myši v nanomolární koncentraci.
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Revision as of 11:58, 25 April 2017

PDB ID 1eve

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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

See 1eve (Chinese), 1eve (French), 1eve (Arabic), 1eve (Russian), 1eve (Spanish), & 1eve (Turkish).

Proteopedia Page Contributors and Editors (what is this?)

Hana Pařízková, Jaime Prilusky, Lucie Kolarova

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