Acetylcholinesterase: Substrate traffic and inhibition
نویسندگان
چکیده
منابع مشابه
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...
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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...
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Itopride is a gastroprokinetic benzamide derivative. This agent inhibited both electric eel acetylcholinesterase (AChE) and horse serum butyrylcholinesterase (BuChE). The IC50 of itopride with AChE (2.04 +/- 0.27 microM) was, however, 100-fold less than that with BuChE, whereas in the case of neostigmine with AChE (11.3 +/- 3.4 nM), it was 10-fold less. The recovery of AChE activity inhibited b...
متن کاملTandem driven dynamic self-inhibition of acetylcholinesterase.
A concept of tandem driven dynamic self-inhibition is demonstrated through dynamic inhibitors of acetylcholinesterase (AChE) using reversible transthiolesterification.
متن کاملAcetylcholinesterase inhibition by flavonoids from Agrimonia pilosa.
In a bioassay-guided search for acetylcholinesterase (AChE) inhibitors from 180 medicinal plants, an ethyl acetate extract of whole plants of Agrimonia pilosa ledeb yielded tiliroside (1), 3-methoxy quercetin (2), quercitrin (3) and quercetin (4). We report herein for the first time that all four flavonol compounds showed significant inhibitory effects on AChE, particularly quercetin (4), which...
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ژورنال
عنوان ژورنال: Biochemistry and Molecular Biology Education
سال: 2012
ISSN: 1470-8175
DOI: 10.1002/bmb.20604