Aricept Complexed with Acetylcholinesterase: Difference between revisions
New page: left|200px<br /> <applet load="1eve" size="450" color="white" frame="true" align="right" spinBox="true" caption="1eve, resolution 2.50Å" /> '''THREE DIMENSIONAL S... |
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==About this Structure== | ==About this Structure== | ||
1EVE is a [[http://en.wikipedia.org/wiki/Single_protein Single protein]] structure of sequence from [[http://en.wikipedia.org/wiki/Torpedo_californica Torpedo californica]] with NAG and E20 as [[http://en.wikipedia.org/wiki/ligands ligands]]. The following page contains interesting information on the relation of 1EVE with [[http://pdb.rcsb.org/pdb/static.do?p=education_discussion/molecule_of_the_month/pdb54_1.html Acetylcholinesterase]]. Active as [[http://en.wikipedia.org/wiki/ ]], with EC number [[http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.1.1.7 3.1.1.7]]. Full crystallographic information is available from [[http://ispc.weizmann.ac.il/oca-bin/ocashort?id=1EVE OCA]]. | 1EVE is a [[http://en.wikipedia.org/wiki/Single_protein Single protein]] structure of sequence from [[http://en.wikipedia.org/wiki/Torpedo_californica Torpedo californica]] with NAG and E20 as [[http://en.wikipedia.org/wiki/ligands ligands]]. The following page contains interesting information on the relation of 1EVE with [[http://pdb.rcsb.org/pdb/static.do?p=education_discussion/molecule_of_the_month/pdb54_1.html Acetylcholinesterase]]. Active as [[http://en.wikipedia.org/wiki/Acetylcholinesterase Acetylcholinesterase]], with EC number [[http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.1.1.7 3.1.1.7]]. Structure known Active Sites: CAT and IHB. Full crystallographic information is available from [[http://ispc.weizmann.ac.il/oca-bin/ocashort?id=1EVE OCA]]. | ||
==Reference== | ==Reference== | ||
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[[Category: serine hydrolase]] | [[Category: serine hydrolase]] | ||
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Revision as of 12:38, 30 October 2007
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THREE DIMENSIONAL STRUCTURE OF THE ANTI-ALZHEIMER DRUG, E2020 (ARICEPT), COMPLEXED WITH ITS TARGET ACETYLCHOLINESTERASE
OverviewOverview
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 StructureAbout 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].
ReferenceReference
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
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