Cholinesterases: Structure, Role, and Inhibition

Bosak, Anita; Katalinić, Maja; Kovarik, Zrinka

doi:10.2478/10004-1254-62-2011-2107

Cited by 11 publications

(6 citation statements)

References 91 publications

(189 reference statements)

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“…One of their clinical manifestations is the depletion of acetylcholine (ACh), a neurotransmitter in cholinergic synapses, caused by its excessive metabolism to choline and acetic acid mediated by cholinesterases. In humans, there are two cholinesterases: acetylcholinesterase (AChE), whose physiological role is to hydrolyse ACh, and butyrylcholinesterase (BChE), whose physiological role is still unclear, except that it hydrolyses ACh and other esters and scavenges some toxins by reacting with them before they reach AChE ( 70 , 71 , 72 ). Treatment of patients with neurodegenerative diseases who have low ACh levels (Alzheimer’s disease) and disorders of the neuromuscular system (Parkinson’s disease, myasthenia gravis) is focused on alleviating symptoms.…”

Section: Carbamates As Drugsmentioning

confidence: 99%

Carbamate group as structural motif in drugs: a review of carbamate derivatives used as therapeutic agents

Matošević

Bosak

2020

Archives of Industrial Hygiene and Toxicology

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Due to their very good chemical and proteolytic stability, ability to penetrate cell membranes, and resemblance to a peptide bond, carbamate derivatives have received much attention in recent years and got an important role in modern drug discovery and medicinal chemistry. Today, carbamates make structural and/or functional part of many drugs and prodrugs approved and marketed for the treatment of various diseases such as cancer, epilepsy, hepatitis C, HIV infection, and Alzheimer’s disease. In drugs they can play a role in drug-target interaction or improve the biological activity of parent molecules. In prodrugs they are mainly used to delay first-pass metabolism and enhance the bioavailability and effectiveness of compounds. This brief review takes a look at the properties and use of carbamates in various fields of medicine and provides quick insights into the mechanisms of action for some of them.

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Section: Carbamates As Drugsmentioning

confidence: 99%

Carbamate group as structural motif in drugs: a review of carbamate derivatives used as therapeutic agents

Matošević

Bosak

2020

Archives of Industrial Hygiene and Toxicology

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“…Organophosphorus compounds all commonly contains carbon and phosphorus, although some are known for being an inhibitor of AChE and content of pesticides, many does not [10]. Specifically those ones capable of creating coordinating covalent bond between the sulfur and phosphor atoms [21]. Another use of organophosphate is being applied to materials used for furniture, textiles and building materials as organophosphate flame retardants (OPFR).…”

Section: Chemicals With Similar Propertiesmentioning

confidence: 99%

The possible methods of diagnosis and effects of exposure to organophosphate pesticides

Xiong¹

2023

TNS

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Organophosphate pesticide (OP), being one of those easy to access, has resulted in many cases of exposure specifically to those working field with it being commonly applied on a frequent basis. It is critical that those working with it have knowledge of its effects and the possible symptoms because of its exposure. And to those who may arrive without any relative detail about themselves, a possible method of diagnosis to confirm that the said person is at risk of exposure. Through investigation across multiple methods aiming to suggest possible pathways of obtaining detailed descriptions or further information of symptoms caused by OP exposure. Additionally, diagnosis methods and comparison to chemicals with similarity in property or classification of OP. In the aim to propose a viable method, comparison and suggestions for current applications

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“…Cholinesterases have different affinity for NA isomers due to the asymmetry of the ChE active sites gorge. AChE and BChE exhibit enantioselectivity, that is, preference for one enantiomer binding over another ( 11 , 25 , 44 , 45 , 46 ). For example, the P(−) isomers of sarin and VX are the most potent AChE inhibitors, and the C(+/−) P(−) isomers of soman are up to 50 times more toxic than the C(+/−) P(+) isomers ( 25 ).…”

Section: Cholinesterasesmentioning

confidence: 99%

Counteracting poisoning with chemical warfare nerve agents

Hrvat

Kovarik

2020

Archives of Industrial Hygiene and Toxicology

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Phosphylation of the pivotal enzyme acetylcholinesterase (AChE) by nerve agents (NAs) leads to irreversible inhibition of the enzyme and accumulation of neurotransmitter acetylcholine, which induces cholinergic crisis, that is, overstimulation of muscarinic and nicotinic membrane receptors in the central and peripheral nervous system. In severe cases, subsequent desensitisation of the receptors results in hypoxia, vasodepression, and respiratory arrest, followed by death. Prompt action is therefore critical to improve the chances of victim’s survival and recovery. Standard therapy of NA poisoning generally involves administration of anticholinergic atropine and an oxime reactivator of phosphylated AChE. Anticholinesterase compounds or NA bioscavengers can also be applied to preserve native AChE from inhibition. With this review of 70 years of research we aim to present current and potential approaches to counteracting NA poisoning.

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Cholinesterases: Structure, Role, and Inhibition

Cited by 11 publications

References 91 publications

Carbamate group as structural motif in drugs: a review of carbamate derivatives used as therapeutic agents

Carbamate group as structural motif in drugs: a review of carbamate derivatives used as therapeutic agents

The possible methods of diagnosis and effects of exposure to organophosphate pesticides

Counteracting poisoning with chemical warfare nerve agents

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