Special Issue "Advances in Acetylcholinesterase and Butyrylcholinesterase Inhibitors"
Deadline for manuscript submissions: closed (15 June 2023) | Viewed by 12935
The most commonly known function of acetylcholinesterase, the rapid termination of cholinergic neurotransmission via the hydrolysis of acetylcholine, whose inactivation leads to acetylcholine accumulation and the hyperstimulation of nicotinic and muscarinic receptors, means that acetylcholinesterase has been the focus of intense research of many medicinal chemists, biologists and pharmacists for decades. The gradual loss of acetylcholinesterase activity is associated with the progressive deterioration of cognitive, autonomic and neuromuscular functions, such as in Alzheimer’s disease, the most common cause of adult-onset dementia. The main class of drugs currently used for the treatment of Alzheimer’s disease are acetylcholinesterase or non-selective cholinesterase inhibitors that exert their activity and temporally improve cognitive symptoms, but they are concomitant and cause distinct side effects, and their effectiveness varies from person to person. In spite of known limitations, these drugs still represent a pharmacotherapeutic resource for the treatment of Alzheimer's disease and the type of dementia that Alzheimer's represents, often using different approaches. Generally, studies directed toward improving the pharmacological activity of cholinesterase compounds represent the mainstream in Alzheimer’s disease treatment management. In recent years, an appropriate strategy to achieve satisfactory therapeutic effect with regard to Alzheimer’s disease and related dementias has been proposed in the form of the development of multitarget-directed ligands (MTDLs) that can interact with multiple disease-related targets such as N-methyl-D-aspartate receptor antagonists or antioxidant agents, where one of the pharmacophores are directed toward the inhibition of acetylcholinesterase. Cholinesterase inhibitors are also used for the reversal of postoperative neuromuscular blockade or for the treatment of myasthenia gravis and Parkinson's disease dementia, the use of cholinesterase inhibitors was determined to have beneficial effects in cases of multiple sclerosis, traumatic brain injury and vascular dementia. On the other hand, the abrupt blockade of acetylcholinesterase action is lethal and as such has stimulated the development of organophosphate and carbamate compounds that are potent acetylcholinesterase inhibitors used as insecticides and/or chemical warfare agents. A lot of effort has been invested in the development of an effective way of returning the activity of phosphorylated acetylcholinesterase, mostly using oxime-based reactivators that are acetylcholinesterase inhibitors per se.
In the last few years, research on acetylcholinesterase’s sister enzyme, butyrylcholinesterase, has intensified due to its engagement in acetylcholine hydrolysis in the middle and late stages of Alzheimer’s disease. Additionally, many studies on the inhibition and/or reactivation of butyrylcholinesterase are devoted to finding an effective bioscavenger for treating organophosphate poisoning.
Dr. Anita Bosak
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- Alzheimer’s disease
- multitarget-directed ligands (MTDLs)
- reversible inhibitors
- irreversible inhibition
- organophosphate poisoning