Acetylcholinesterase: Reversible Inhibitors, Substrate Inhibition

Acetylcholinesterase: reversible inhibitors, substrate inhibition.

Observations with acetylcholinesterase can be well explained by postulating that the active site contains two subsites: one, an anionic site which binds and orients substituted ammonium ions, and the other, an esteratic site where the hydrolytic process occurs and which contains a basic group which is acetylated and deacetylated during the process (4, 5). The formation of an acetyl enzyme sugge...

Structural insights into substrate traffic and inhibition in acetylcholinesterase.

Acetylcholinesterase (AChE) terminates nerve-impulse transmission at cholinergic synapses by rapid hydrolysis of the neurotransmitter, acetylcholine. Substrate traffic in AChE involves at least two binding sites, the catalytic and peripheral anionic sites, which have been suggested to be allosterically related and involved in substrate inhibition. Here, we present the crystal structures of Torp...

Acetylcholinesterase inhibitors attenuate angiogenesis

Donepezil {(RS)-2-[(1-benzyl-4-piperidyl)methyl]-5,6-dimethoxy-2,3-dihydroinden-1-one} is a reversible acetylcholinesterase inhibitor and used for treatment of patients with AD (Alzheimer's disease). Recent studies showed that treatment with donepezil reduced production of inflammatory cytokines in PBMCs (peripheral blood mononuclear cells). It was also reported that muscle-derived inflammatory...

Inhibitors of Acetylcholinesterase

Acetylcholinesterase inhibitors from plants.

Inhibition of acetylcholinesterase (AChE), the key enzyme in the breakdown of acetylcholine, is considered as a promising strategy for the treatment of neurological disorders such as Alzheimer's disease, senile dementia, ataxia and myasthenia gravis. A potential source of AChE inhibitors is certainly provided by the abundance of plants in nature. This article aims to provide a comprehensive lit...