Structures of human acetylcholinesterase in complex with pharmacologically important ligands

Jonah Cheung, Michael J. Rudolph, Fiana Burshteyn, Michael S. Cassidy, Ebony N. Gary, James Love, Matthew C. Franklin, Jude J. Height

Research output: Contribution to journalArticle

364 Citations (Scopus)

Abstract

Human acetylcholinesterase (AChE) is a significant target for therapeutic drugs. Here we present high resolution crystal structures of human AChE, alone and in complexes with drug ligands; donepezil, an Alzheimer's disease drug, binds differently to human AChE than it does to Torpedo AChE. These crystals of human AChE provide a more accurate platform for further drug development than previously available.

Original languageEnglish (US)
Pages (from-to)10282-10286
Number of pages5
JournalJournal of Medicinal Chemistry
Volume55
Issue number22
DOIs
StatePublished - Nov 26 2012

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Acetylcholinesterase
Ligands
Pharmaceutical Preparations
Torpedo
Alzheimer Disease
Therapeutics

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

Cite this

Cheung, J., Rudolph, M. J., Burshteyn, F., Cassidy, M. S., Gary, E. N., Love, J., ... Height, J. J. (2012). Structures of human acetylcholinesterase in complex with pharmacologically important ligands. Journal of Medicinal Chemistry, 55(22), 10282-10286. https://doi.org/10.1021/jm300871x

Structures of human acetylcholinesterase in complex with pharmacologically important ligands. / Cheung, Jonah; Rudolph, Michael J.; Burshteyn, Fiana; Cassidy, Michael S.; Gary, Ebony N.; Love, James; Franklin, Matthew C.; Height, Jude J.

In: Journal of Medicinal Chemistry, Vol. 55, No. 22, 26.11.2012, p. 10282-10286.

Research output: Contribution to journalArticle

Cheung, J, Rudolph, MJ, Burshteyn, F, Cassidy, MS, Gary, EN, Love, J, Franklin, MC & Height, JJ 2012, 'Structures of human acetylcholinesterase in complex with pharmacologically important ligands', Journal of Medicinal Chemistry, vol. 55, no. 22, pp. 10282-10286. https://doi.org/10.1021/jm300871x
Cheung J, Rudolph MJ, Burshteyn F, Cassidy MS, Gary EN, Love J et al. Structures of human acetylcholinesterase in complex with pharmacologically important ligands. Journal of Medicinal Chemistry. 2012 Nov 26;55(22):10282-10286. https://doi.org/10.1021/jm300871x
Cheung, Jonah ; Rudolph, Michael J. ; Burshteyn, Fiana ; Cassidy, Michael S. ; Gary, Ebony N. ; Love, James ; Franklin, Matthew C. ; Height, Jude J. / Structures of human acetylcholinesterase in complex with pharmacologically important ligands. In: Journal of Medicinal Chemistry. 2012 ; Vol. 55, No. 22. pp. 10282-10286.
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