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Tacrine is a parasympathomimetic and a centrally acting cholinesterase inhibitor. | Tacrine is a parasympathomimetic and a centrally acting cholinesterase inhibitor. | ||
| - | + | 1ACJ shows the crystal structure of Torpedo californica acetylcholinesterase (TcAChE) complexed with tacrine. | |
| + | Tacrine is a parasympathomimetic and a centrally acting cholinesterase inhibitor. | ||
| + | It was the first centrally-acting cholinesterase inhibitor approved for the treatment of Alzheimer's disease. | ||
| + | Tacrine’s ring is stacked between the aromatic rings of tryptophan 84 and phenylalanine 330 (W84 and F330)..<scene name='Sandbox_c30/Inhibidor/3'>(w84- Y330)</scene> | ||
| - | <ref></ref>Harel M, Schalk I, Ehret-Sabatier L, Bouet F, Goeldner M, Hirth C, Axelsen PH, Silman I, Sussman JL. Quaternary ligand binding to aromatic residues in the active-site gorge of acetylcholinesterase. Proc Natl Acad Sci U S A. 1993 Oct 1;90(19):9031-5. PMID:8415649 | + | |
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| + | <ref></ref>PMID:8415649 | ||
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| + | Harel M, Schalk I, Ehret-Sabatier L, Bouet F, Goeldner M, Hirth C, Axelsen PH, Silman I, Sussman JL. Quaternary ligand binding to aromatic residues in the active-site gorge of acetylcholinesterase. Proc Natl Acad Sci U S A. 1993 Oct 1;90(19):9031-5. PMID:8415649 | ||
<references/> | <references/> | ||
Revision as of 13:25, 23 November 2010
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