Sandbox c12
From Proteopedia
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It was the first centrally-acting cholinesterase inhibitor approved for the treatment of Alzheimer's disease. | It was the first centrally-acting cholinesterase inhibitor approved for the treatment of Alzheimer's disease. | ||
| - | <scene name='Sandbox_c12/Label/1'> | + | <scene name='Sandbox_c12/Label/1'>Tacrines ring</scene> is stacked between the aromatic rings of tryptophan 84 and phenylalanine 330 (<scene name='Sandbox_c12/Residuos_84_y_330/1'>W84 and F330</scene>). |
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 | 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 | ||
Revision as of 13:19, 23 November 2010
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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.
is stacked between the aromatic rings of tryptophan 84 and phenylalanine 330 ().
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
