Target intelligence / Profile preview

Cholinesterase enzyme family

Molecular classification
Enzyme, Hydrolase, Alpha/beta hydrolase family, Carboxylesterase family
01

Overview

The cholinesterase enzyme family consists primarily of two related enzymes: acetylcholinesterase and butyrylcholinesterase. Both catalyze the hydrolysis of the neurotransmitter acetylcholine into choline and acetic acid—a reaction essential for terminating neurotransmission at cholinergic synapses. Acetylcholinesterases are found mainly at neuromuscular junctions and neural synapses where they rapidly degrade acetylcholine after its release. Butyrylcholinesterases are present mainly in plasma and liver with broader substrate specificity. These enzymes play critical roles in nervous system function as well as detoxification processes. They are major therapeutic targets for drugs treating neurodegenerative diseases such as Alzheimer’s disease—and also key targets/inhibitors involved in pesticide/nerve agent toxicity.

Other names
CholinesterasesAcetylcholine esterase familyAChE and BChE enzymesTrue cholinesterase (for acetylcholinesterase)Pseudocholinesterase (for butyrylcholinesterase)RBC cholinesterase (acetylcholinesterase)Plasma cholinesterase (butyrylcholinesterase)
02

Mechanism of action

Drugs targeting this enzyme act primarily as enzyme inhibitors—either reversible or irreversible—leading to increased levels of acetylcholine at synapses. This can enhance cholinergic transmission in diseases like Alzheimer’s or cause toxicity in the case of poisoning.

03

Biological functions

Hydrolysis of acetylcholine and other choline estersTermination of neurotransmission at cholinergic synapsesRegulation of synaptic transmission and neuronal signaling
04

Disease associations

Neurodegenerative disease (e.g., Alzheimer’s disease)Poisoning by organophosphates, nerve agents, or pesticides
05

Safety considerations

Notable concerns include risk of toxicity from excessive inhibition, leading to symptoms such as muscle weakness/paralysis, respiratory failure; hypersensitivity reactions; genetic variants causing atypical responses to anesthetics; potential cognitive side effects with chronic use.
06

Interacting drugs

Organophosphate insecticides/nerve agents (irreversible inhibitors): e.g., sarin, parathion, malathion

3 more in the full profile.

07

Biomarkers

Measurement of cholinesterase activity in blood is used as a biomarker for exposure to organophosphate/carbamate poisoning and for monitoring patients on certain drugs.

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