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Structures of Human Acetylcholinesterase in Complex with Pharmacologically Important Ligands

2012; American Chemical Society; Volume: 55; Issue: 22 Linguagem: Inglês

10.1021/jm300871x

1520-4804

Jonah Cheung, M. Rudolph, F. Burshteyn, M. Cassidy, E. Gary, J. Love, Matthew C. Franklin, J.J. Height,

Enzyme function and inhibition

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.