Sandbox c6
From Proteopedia
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| - | <Structure load='1ACJ' size='400' frame='true' align='right' caption='mi estructura favorita' />1ACJ shows the crystal structure of Torpedo californica acetylcholinesterase (TcAChE) complexed with tacrine. | + | <Structure load='1ACJ' size='400' frame='true' align='right' caption='mi estructura favorita' />1ACJ shows the crystal structure of ''Torpedo californica'' acetylcholinesterase (TcAChE) complexed with '''tacrine'''.<ref>PMID 654</ref> |
Tacrine is a parasympathomimetic and a centrally acting cholinesterase inhibitor. | Tacrine is a parasympathomimetic and a centrally acting cholinesterase inhibitor. | ||
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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. | ||
| - | Tacrine’s ring is stacked between the aromatic rings of tryptophan 84 and phenylalanine 330 | + | Tacrine’s ring is stacked between the aromatic rings of tryptophan 84 and phenylalanine 330 |
| - | <scene name='Sandbox_c6/Tacrine1/1'> | + | <scene name='Sandbox_c6/Tacrine1/1'> (W84 and F330)</scene> |
| + | <ref>PMID:8415649</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 | 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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Current revision
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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
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
- ↑ Acar JF, Guibert J. [Relationship between serum antibiotic concentration and inhibiting potency of the serum. Application to ampicillin and amoxicillin]. Nouv Presse Med. 1975 Oct 15;4(34):2441-4. PMID:654
- ↑ 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
