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
-
Stress, Depression and Antidepressant Treatment Options in Patients Suffering from Multiple Sclerosis
Current Pharmaceutical Design Low Activity of Plasminogen Activator: A Common Feature of Non- Iatrogenic Comorbidities of Schizophrenia
CNS & Neurological Disorders - Drug Targets Overcoming Drug Resistance by Enhancing Apoptosis of Tumor Cells
Current Cancer Drug Targets Genetics of Alzheimer's Disease and Frontotemporal Dementia
Current Molecular Medicine Current Understanding of In-stent Restenosis and the Potential Benefit of Drug Eluting Stents
Current Drug Targets - Cardiovascular & Hematological Disorders Investigating Drug-induced Mitochondrial Toxicity: A Biosensor to Increase Drug Safety?
Current Drug Safety Cardiovascular Complications of Obesity
Current Respiratory Medicine Reviews The Role of Functional Neuroimaging in Mild Cognitive Impairment
Current Medical Imaging The TLR9 Antagonist iCpG-ODN at Different Dosages Inhibits Cerebral Ischemia/Reperfusion Injury in Mice
CNS & Neurological Disorders - Drug Targets Multiple Mechanisms of Cytokine Action in Neurodegenerative and Psychiatric States: Neurochemical and Molecular Substrates
Current Pharmaceutical Design Editorial (Hot Topic: TRP Channels as Therapeutic Targets)
Current Topics in Medicinal Chemistry Role of Leptin in the Immune System
Current Immunology Reviews (Discontinued) Regulatory Approaches to Nonclinical Reproductive Toxicity Testing of Anti-Cancer Drugs
Anti-Cancer Agents in Medicinal Chemistry Alteration of Structure and Aggregation of α-Synuclein by Familial Parkinson’s Disease Associated Mutations
Current Protein & Peptide Science Drug Delivery to the Back of the Eye Following Topical Administration: An Update on Research and Patenting Activity
Recent Patents on Drug Delivery & Formulation The Role of the PACAP Signaling System in Depression
Current Pharmaceutical Design Beyond Monoamines-Novel Targets for Treatment-Resistant Depression: A Comprehensive Review
Current Neuropharmacology Proteomics Analysis of CA1 Region of the Hippocampus in Pre-, Progression and Pathological Stages in a Mouse Model of the Alzheimer’s Disease
Current Alzheimer Research Interrelation Between Protein Synthesis, Proteostasis and Life Span
Current Genomics Heat Shock Proteins And Neuroprotection
Recent Patents on DNA & Gene Sequences