(+)-Arisugacin A—Computational evidence of a dual binding site covalent inhibitor of acetylcholinesterase

A computation docking study of the highly potent, non-nitrogen containing, acetylcholinesterase inhibitor (+)-arisugacin A is presented. The model suggests that (+)-arisugacin A is a dual binding site covalent inhibitor of AChE. These findings are examined in the context of Alzheimer’s disease-modif...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2011-05, Vol.21 (9), p.2687-2691
Hauptverfasser: Al-Rashid, Ziyad F., Hsung, Richard P.
Format: Artikel
Sprache:eng
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Zusammenfassung:A computation docking study of the highly potent, non-nitrogen containing, acetylcholinesterase inhibitor (+)-arisugacin A is presented. The model suggests that (+)-arisugacin A is a dual binding site covalent inhibitor of AChE. These findings are examined in the context of Alzheimer’s disease-modifying therapeutic design. (+)-Arisugacin A’s revealed mode of action is unique, and may serve as a basis for the development of AD therapeutics capable of treating the symptomatic aspects of AD, while being neuroprotective with long term efficacy.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2010.12.041