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

doi:10.1021/jm300871x

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

Biochemistry

Research output: Contribution to journal › Article › peer-review

924 Scopus citations

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 language	English (US)
Pages (from-to)	10282-10286
Number of pages	5
Journal	Journal of Medicinal Chemistry
Volume	55
Issue number	22
DOIs	https://doi.org/10.1021/jm300871x
State	Published - Nov 26 2012

ASJC Scopus subject areas

Molecular Medicine
Drug Discovery

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1021/jm300871x

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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.",

author = "Jonah Cheung and Rudolph, {Michael J.} and Fiana Burshteyn and Cassidy, {Michael S.} and Gary, {Ebony N.} and James Love and Franklin, {Matthew C.} and Height, {Jude J.}",

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AU - Cheung, Jonah

AU - Rudolph, Michael J.

AU - Burshteyn, Fiana

AU - Cassidy, Michael S.

AU - Gary, Ebony N.

AU - Love, James

AU - Franklin, Matthew C.

AU - Height, Jude J.

PY - 2012/11/26

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N2 - 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.

AB - 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.

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Structures of human acetylcholinesterase in complex with pharmacologically important ligands

Abstract

ASJC Scopus subject areas

UN SDGs

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