4.3 Article

Current Acetylcholinesterase-Inhibitors: A Neuroinformatics Perspective

Journal

CNS & NEUROLOGICAL DISORDERS-DRUG TARGETS
Volume 13, Issue 3, Pages 391-401

Publisher

BENTHAM SCIENCE PUBL
DOI: 10.2174/18715273113126660166

Keywords

Acetylcholinesterase; acetylcholine; physostigmine; rivastigmine; huperzine A

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This review presents a concise update on the inhibitors of the neuroenzyme, acetylcholinesterase (AChE; EC 3.1.1.7). AChE is a serine protease, which hydrolyses the neurotransmitter, acetylcholine into acetate and choline thereby terminating neurotransmission. Molecular interactions (mode of binding to the target enzyme), clinical applications and limitations have been summarized for each of the inhibitors discussed. Traditional inhibitors (e.g. physostigmine, tacrine, donepezil, rivastigmine etc.) as well as novel inhibitors like various physostigmine-derivatives have been covered. This is followed by a short glimpse on inhibitors derived from nature (e.g. Huperzine A and B, Galangin). Also, a discussion on 'hybrid of pre-existing drugs' has been incorporated. Furthermore, current status of therapeutic applications of AChE- inhibitors has also been summarized.

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