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.
Keywords: Acetylcholinesterase, acetylcholine, physostigmine, rivastigmine, huperzine A.
CNS & Neurological Disorders - Drug Targets
Title:Current Acetylcholinesterase-Inhibitors: A Neuroinformatics Perspective
Volume: 13 Issue: 3
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:
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.
Export Options
About this article
Cite this article as:
Shaikh Sibhghatulla, Verma Anupriya, Siddiqui Saimeen, Ahmad S. Syed, Rizvi M.D. Syed, Shakil Shazi, Biswas Deboshree, Singh Divya, Siddiqui H. Mohmmad, Shakil Shahnawaz, Tabrez Shams and Kamal A. Mohammad, Current Acetylcholinesterase-Inhibitors: A Neuroinformatics Perspective, CNS & Neurological Disorders - Drug Targets 2014; 13 (3) . https://dx.doi.org/10.2174/18715273113126660166
DOI https://dx.doi.org/10.2174/18715273113126660166 |
Print ISSN 1871-5273 |
Publisher Name Bentham Science Publisher |
Online ISSN 1996-3181 |
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Neuropsychiatric and Cognitive Symptoms in Spinocerebellar Ataxia: Relationship to Neuropathological Differences
Current Psychiatry Reviews Vitamin D Analogs as Anti-Carcinogenic Agents
Anti-Cancer Agents in Medicinal Chemistry Overlapping Molecular Signatures in Parkinson's Patient Leukocytes Before and After Treatment and in Mouse Model Brain Regions
CNS & Neurological Disorders - Drug Targets Diffusion Tensor Imaging to Determine Effects of Antidementive Treatment on Cerebral Structural Connectivity in Alzheimer’s Disease
Current Pharmaceutical Design Anti-inflammatory strategies in stroke: a potential therapeutic target
Current Vascular Pharmacology Ubiquitin and ubiquitin-like proteins in cardiac disease and protection
Current Drug Targets 1950 MHz Electromagnetic Fields Ameliorate Aβ Pathology in Alzheimer’s Disease Mice
Current Alzheimer Research Cytoprotection by Natural and Synthetic Polyphenols in the Heart: Novel Mechanisms and Perspectives
Current Pharmaceutical Design Role of Vitamins in Human Health and Nutrition: Sources and Morbidity
Current Nutrition & Food Science Nuances in Alzheimer’s Genetic Risk Reveal Differential Predictions of Non-demented Memory Aging Trajectories: Selective Patterns by APOE Genotype and Sex
Current Alzheimer Research Doppler Haemodynamics of Cerebral Venous Return
Current Neurovascular Research Good Epidemiologic Practice in Retinitis Pigmentosa: From Phenotyping to Biobanking
Current Genomics A Short Review of Diffusion Models and their Possibilities to Enhance Imaging Biomarkers for Neurodegenerative Diseases
Current Medical Imaging T-Lymphocytes: A Target for Stimulatory and Inhibitory Effects of Zinc Ions
Endocrine, Metabolic & Immune Disorders - Drug Targets Editorial [Hot Topic: Therapeutic Approaches for Vision Loss due to Choroidal Neovascularizations in Age Related Macular Degeneration (Guest Editor: Ciro Costagliola)]
Current Drug Targets The Small Bowel: An Imaging Guide
Current Medical Imaging OMICS-Derived Targets for Inflammatory Gut Disorders: Opportunities for the Development of Nutrition Related Biomarkers
Endocrine, Metabolic & Immune Disorders - Drug Targets Understanding Abnormal c-JNK/p38MAPK Signaling in Amyotrophic Lateral Sclerosis: Potential Drug Targets and Influences on Neurological Disorders
CNS & Neurological Disorders - Drug Targets Extranuclear Effects of Thyroid Hormones in Skeletal Muscle
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) Bioinformatics Approach to BDNF and BDNF-Related Disorders
Current Neuropharmacology