CNS & Neurological Disorders - Drug Targets

(Formerly Current Drug Targets - CNS & Neurological Disorders)

Stephen D. Skaper  
Department of Pharmaceutical and Pharmacological Sciences
University of Padova
Padova
Italy

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Current Acetylcholinesterase-Inhibitors: A Neuroinformatics Perspective

Author(s): Sibhghatulla Shaikh, Anupriya Verma, Saimeen Siddiqui, Syed S. Ahmad, Syed M.D. Rizvi, Shazi Shakil, Deboshree Biswas, Divya Singh, Mohmmad H. Siddiqui, Shahnawaz Shakil, Shams Tabrez and Mohammad A. Kamal

Affiliation: Department of Bio-engineering, Integral University, Lucknow, 226026, India.

Keywords: Acetylcholinesterase, acetylcholine, physostigmine, rivastigmine, huperzine A.

Abstract:

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 AChEinhibitors has also been summarized.

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Article Details

VOLUME: 13
ISSUE: 3
Page: [391 - 401]
Pages: 11
DOI: 10.2174/18715273113126660166