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
-
Mechanisms of Altered Cell Immunity and Cytotoxicity in COPD
Current Drug Targets Interrelationships Among Gut Microbiota and Host: Paradigms, Role in Neurodegenerative Diseases and Future Prospects
CNS & Neurological Disorders - Drug Targets Contemporary Animal Models For Human Gene Therapy Applications
Current Gene Therapy Protein Misfolding in Disease: Cause or Response?
Current Medicinal Chemistry - Immunology, Endocrine & Metabolic Agents Depression Under the Perspective of Oxytocin
Central Nervous System Agents in Medicinal Chemistry Platelets in Alzheimer’s Disease-Associated Cellular Senescence and Inflammation
Current Pharmaceutical Design Clinical Molecular Imaging with PET Agents Other than 18F-FDG
Current Pharmaceutical Biotechnology Neuroprotective Effects of Lithium in Human Brain? Food for Thought
Current Alzheimer Research Retinal Nerve Fiber Layer Thickness is Associated with Episodic Memory Deficit in Mild Cognitive Impairment Patients
Current Alzheimer Research Clinical Features and Disease Damage Risk Factors in an Egyptian SLE Cohort: A Multicenter Study
Current Rheumatology Reviews Central Nervous System Abnormalities in Fibromyalgia and Chronic Fatigue Syndrome: New Concepts in Treatment
Current Pharmaceutical Design mTOR in Growth and Protection of Hypertrophying Myocardium
Cardiovascular & Hematological Agents in Medicinal Chemistry Skeletal Muscle in Motor Neuron Diseases: Therapeutic Target and Delivery Route for Potential Treatments
Current Drug Targets Emerging Therapy for Diabetic Neuropathy: Cell Therapy Targeting Vessels and Nerves
Endocrine, Metabolic & Immune Disorders - Drug Targets Connections Between Herpes Simplex Virus Type 1 and Alzheimer's Disease Pathogenesis
Current Alzheimer Research Genetic and Modifying Factors that Determine the Risk of Brain Tumors
Central Nervous System Agents in Medicinal Chemistry Angiogenesis and Blood-Brain Barrier Permeability in Vascular Remodeling after Stroke
Current Neuropharmacology MicroRNAs: Newcomers into the ALS Picture
CNS & Neurological Disorders - Drug Targets Varicella-Zoster Virus Infections During Pregnancy: Epidemiology, Clinical Symptoms, Diagnosis, Prevention and Therapy
Current Pediatric Reviews Selective Glucocorticoid Receptor Ligands
Medicinal Chemistry