AI Article Synopsis
- - Acetylcholinesterase is an enzyme that breaks down acetylcholine, a neurotransmitter, into acetic acid and choline, playing a key role in nerve signal termination.
- - The enzyme has a complex structure with multiple binding sites that allow various inhibitors to interfere with its function, leading to increased levels of acetylcholine in synapses and disrupted neurotransmission, relevant for both therapy and toxicology.
- - This review covers the enzyme's properties, its inhibitors, their mechanisms of action, and the resistance developed by organisms due to excessive use of these inhibitors.
Article Abstract
Background: Acetylcholinesterase is a serine hydrolase that terminates the action of the neurotransmitter acetylcholine by hydrolyzing it into acetic acid and choline.
Objective: The enzyme, containing an ellipsoidal structure, possesses three binding sites such as active site (with catalytic anionic and esteratic subsites), aromatic gorge and peripheral anionic site, where the inhibiting compounds interact. The acetylcholinesterase inhibitors bind to the enzyme and interfere with the breakdown of acetylcholine, leading to the deposition of acetylcholine in the nerve synapses and causing disrupted neurotransmission. Based on this principle of action, many therapeutic drugs for the treatment of different diseases, pesticides and chemical warfare agents have been synthesized targeting the actylcholinesterase.
Conclusion: The present review summarizes the current knowledge about acetylcholinesterase, its structure, function and biosynthesis, its inhibitors, and mode of action of inhibitors on it. Besides, the review also presents an overview about the resistance mechanism that the organisms develop due to the over-application of acetylcholinesterase inhibitors.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.2174/1389557517666170120153930 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!