User:Eran Hodis: Difference between revisions
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The anti-Alzheimer's drug E2020 (marketed as Aricept®) 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>. | The anti-Alzheimer's drug E2020 (marketed as Aricept®) 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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Here are three of our favorite pages that we invite you to visit to get a feel for Proteopedia:[[Hemoglobin]], [[1eve | Aricept-Acetylcholinesterase]], and [[1v04 | Serum Paraoxonase-1 by directed evolution]]. | |||
===What is Proteopedia?=== | ===What is Proteopedia?=== | ||
Proteopedia is a free and collaborative, 3D encyclopedia of proteins, RNA, DNA, and their assemblies and interacting small molecules with emphasis on three-dimensional structure where relevant to function. | Proteopedia is a free and collaborative, 3D encyclopedia of proteins, RNA, DNA, and their assemblies and interacting small molecules with emphasis on three-dimensional structure where relevant to function. | ||
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