targeting acetylcholinesterase identification of chemical leads by high throughput screening, structure determination and molecular modeling针对乙酰胆碱酯酶识别化学带来的高通量筛选、结构测定和分子建模.pdfVIP
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targeting acetylcholinesterase identification of chemical leads by high throughput screening, structure determination and molecular modeling针对乙酰胆碱酯酶识别化学带来的高通量筛选、结构测定和分子建模
Targeting Acetylcholinesterase: Identification of
Chemical Leads by High Throughput Screening,
Structure Determination and Molecular Modeling
1 1 2 ¨ 2 2
Lotta Berg , C. David Andersson , Elisabet Artursson , Andreas Hornberg , Anna-Karin Tunemalm ,
1 ¨ 2
Anna Linusson *, Fredrik Ekstrom *
˚ ˚ ˚
1 Department of Chemistry, Umea University, Umea, Sweden, 2 Swedish Defence Research Agency, CBRN Defence and Security, Umea, Sweden
Abstract
Acetylcholinesterase (AChE) is an essential enzyme that terminates cholinergic transmission by rapid hydrolysis of the
neurotransmitter acetylcholine. Compounds inhibiting this enzyme can be used (inter alia) to treat cholinergic deficiencies
(e.g. in Alzheimer’s disease), but may also act as dangerous toxins (e.g. nerve agents such as sarin). Treatment of nerve agent
poisoning involves use of antidotes, small molecules capable of reactivating AChE. We have screened a collection of organic
molecules to assess their ability to inhibit the enzymatic activity of AChE, aiming to find lead compounds for further
optimization leading to drugs with increased efficacy and/or decreased side effects. 124 inhibitors were discovered, with
considerable chemical diversity regarding size, polarity, flexibility and charge distribution. An extensive structure
determination campaign resulted in a set of crystal structures of protein-ligand complexes. Overall, the ligands have
substantial interac
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