AChE bivalent inhibitors

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PART I. Tacrine- and hupyridone-containing compounds

This page is a continuation of the pages AChE inhibitors and substrates, AChE inhibitors and substrates (Part II), and AChE inhibitors and substrates (Part III).

  • 1zgb Complex with (R)-tacrine-(10)-hupyridone (cmp R-3)
  • 1zgc Complex with (S)-tacrine-(10)-hupyridone (cmp S-3)
  • 1acj Complex with tacrine alone
  • 1h22 Complex with (S,S)-(-)-Bis(12)-hupyridone (cmp (S,S)-(-)-4b)
  • 1h23 Complex with (S,S)-(-)-Bis(10)-hupyridone (cmp (S,S)-(-)-4a)
  • 2cmf Complex with Bis(5)-tacrine derivative (cmp 2d)
  • 2ckm Complex with Bis(7)-tacrine derivative (cmp 2f)
  • 1ut6 Complex with N-9-(1',2',3',4'-TETRAHYDROACRIDINYL)-1,8-DIAMINOOCTANE (cmp 6)
  • 1odc Complex with cmp 7

Additional Resources

For additional information, see: Alzheimer's Disease
For information about additional AChE inhibitors see page AChE bivalent inhibitors (Part II).


  1. 1.0 1.1 Haviv H, Wong DM, Greenblatt HM, Carlier PR, Pang YP, Silman I, Sussman JL. Crystal packing mediates enantioselective ligand recognition at the peripheral site of acetylcholinesterase. J Am Chem Soc. 2005 Aug 10;127(31):11029-36. PMID:16076210 doi:
  2. Wong DM, Greenblatt HM, Dvir H, Carlier PR, Han YF, Pang YP, Silman I, Sussman JL. Acetylcholinesterase complexed with bivalent ligands related to huperzine a: experimental evidence for species-dependent protein-ligand complementarity. J Am Chem Soc. 2003 Jan 15;125(2):363-73. PMID:12517147 doi:
  3. 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
  4. Raves ML, Harel M, Pang YP, Silman I, Kozikowski AP, Sussman JL. Structure of acetylcholinesterase complexed with the nootropic alkaloid, (-)-huperzine A. Nat Struct Biol. 1997 Jan;4(1):57-63. PMID:8989325
  5. Rydberg EH, Brumshtein B, Greenblatt HM, Wong DM, Shaya D, Williams LD, Carlier PR, Pang YP, Silman I, Sussman JL. Complexes of alkylene-linked tacrine dimers with Torpedo californica acetylcholinesterase: Binding of Bis5-tacrine produces a dramatic rearrangement in the active-site gorge. J Med Chem. 2006 Sep 7;49(18):5491-500. PMID:16942022 doi:

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Alexander Berchansky, David Canner, Michal Harel, Jaime Prilusky

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