View source for Main Page 20190127

<applet load="1eve" size="400" color="white" frame="true" align="right" spinBox="true" script="1eve/E2020_in_ache/6" caption="PDB: 1eve, resolution 2.50&Aring;. DRAG TO ROTATE." />

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The anti-Alzheimer's drug E2020 (marketed as Aricept&reg;) is an inhibitor that binds acetylcholinesterase (AChE) with high affinity.  The X-ray structure of the E2020-AChE (AChE from ''Torpedo california'') complex shows that E2020 has a '''<scene name='1eve/E2020_close_up_with_84_279/7'>unique orientation</scene>''' along the active-site gorge, extending from the anionic subsite ('''<scene name='1eve/E2020_close_up_with_84lbld/3'>W84</scene>''') of the active site, at the bottom, to the peripheral anionic site ('''<scene name='1eve/E2020_close_up_with_84_279lbld/2'>near W279</scene>'''), 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 '''<scene name='1eve/E20_interactionshown/3'>indirectly via solvent molecules</scene>'''.
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