Sandbox c6

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1ACJ shows the crystal structure of Torpedo californica acetylcholinesterase (TcAChE) complexed with tacrine.^[1]

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

^[2]

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

1. ↑ 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
2. ↑ 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