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
-
Mevalonate Cascade and Neurodevelopmental and Neurodegenerative Diseases: Future Targets for Therapeutic Application
Current Molecular Pharmacology Serotonergic Drugs: Agonists/Antagonists at Specific Serotonergic Subreceptors for the Treatment of Cognitive, Depressant and Psychotic Symptoms in Alzheimer’s Disease
Current Pharmaceutical Design Induced Pluripotent Stem Cells (iPSCs) Derived from Different Cell Sources and their Potential for Regenerative and Personalized Medicine
Current Molecular Medicine Translocator Protein (TSPO) Role in Aging and Alzheimer’s Disease
Current Aging Science Advanced Neoplastic Disease as Immunologic, Endocrine and Metabolic Disorder
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry MRI of Pancreas in Patients with Chronic Pancreatitis and Healthy Volunteers: Can Pancreatic Signal Intensity and Contrast Enhancement Patterns be Valuable Predictors of Early Chronic Pancreatitis?
Current Medical Imaging New Strategies in the Development of Antidepressants: Towards the Modulation of Neuroplasticity Pathways
Current Pharmaceutical Design Cubilin, the Intrinsic Factor-Vitamin B12 Receptor in Development and Disease
Current Medicinal Chemistry Inflammatory Caspases: Targets for Novel Therapies
Current Pharmaceutical Design Aceruloplasminemia
Current Drug Targets Preclinical Studies and Clinical Trials with Mesenchymal Stem Cell for Demyelinating Diseases: A Systematic Review
Current Stem Cell Research & Therapy The PTEN/PI3K/AKT Signalling Pathway in Cancer, Therapeutic Implications
Current Cancer Drug Targets The Role of Neurogenesis in Neurodegenerative Diseases and its Implications for Therapeutic Development
CNS & Neurological Disorders - Drug Targets Molecular Insights and Therapeutic Targets in Amyotrophic Lateral Sclerosis
CNS & Neurological Disorders - Drug Targets Nicotine and Gastrointestinal Disorders: Its Role in Ulceration and Cancer Development
Current Pharmaceutical Design Implication of Rho GTPases in Neurodegenerative Diseases
Current Drug Targets Sleep Related Disorders in the Elderly: An Overview
Current Respiratory Medicine Reviews Hydroximic Acid Derivatives: Pleiotropic Hsp Co-Inducers Restoring Homeostasis and Robustness
Current Pharmaceutical Design Homocysteine in Neurology: From Endothelium to Neurodegeneration
Current Nutrition & Food Science Will Plants Grow on Moon or Mars?
Current Biotechnology