Sandbox 1eve
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==Example page for E2020-TcAChE complex (1eve)== | ==Example page for E2020-TcAChE complex (1eve)== | ||
| - | <StructureSection load='1eve' size='340' side='right' caption=' | + | <StructureSection load='1eve' size='340' side='right' caption='PDB entry [[1eve]]' scene='29/2908/1eve_e20_cartoon/3'> |
| - | [[Image:1eve.Workshop.jpg|thumb|left|250px|E2020 with active site and | + | [[Image:1eve.Workshop.jpg|thumb|left|250px|E2020 with active site and interacts]] |
== Introduction == | == Introduction == | ||
E2020, marketed as Aricept, is a member of a large family of N-benzylpiperidine- based acetylcholinesterase (AChE) inhibitors developed, synthesized and evaluated by the Elsai 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. | E2020, marketed as Aricept, is a member of a large family of N-benzylpiperidine- based acetylcholinesterase (AChE) inhibitors developed, synthesized and evaluated by the Elsai 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. | ||
| - | + | <scene name='10/1052408/E2020_and_aricept/3'>E2020 and TcAChE</scene>. | |
== Exploring the Structure == | == Exploring the Structure == | ||
| - | <scene name='10/1052408/E2020_space_fill/ | + | <scene name='10/1052408/E2020_space_fill/5'>E2020</scene> has a unique orientation along the active-site gorge, extending from the anionic subsite of the active site, at the bottom, to the peripheral anlonic site, at the top, via aromatic stacking interactions with conserved aromatic acid residues. E2020 does not, however, interact directly with either the catalytic triad or the 'oxyanion hole', but only indirectly via solvent molecules. |
<ref>PMID:10368299</ref> | <ref>PMID:10368299</ref> | ||
| + | </StructureSection> | ||
== References == | == References == | ||
<references/> | <references/> | ||
Current revision
Example page for E2020-TcAChE complex (1eve)
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