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Slow-binding inhibition of cholinesterases, pharmacological and toxicological relevance

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dc.contributor.author Masson P.
dc.contributor.author Lushchekina S.
dc.date.accessioned 2018-09-19T20:04:26Z
dc.date.available 2018-09-19T20:04:26Z
dc.date.issued 2016
dc.identifier.issn 0003-9861
dc.identifier.uri https://dspace.kpfu.ru/xmlui/handle/net/142515
dc.description.abstract © 2016 Elsevier Inc. All rights reserved. Slow-binding inhibition (SBI) of enzymes is characterized by slow establishment of enzyme-inhibitor equilibrium. Cholinesterases (ChEs) display slow onset of inhibition with certain inhibitors. After a survey of SBI mechanisms, SBI of ChEs is examined. SBI results either from simple slow interaction, induced-fit, or slow conformational selection. In some cases, the slow equilibrium is followed by an irreversible chemical step. This later was observed for the interaction of ChEs with certain irreversible inhibitors. Because slow-binding inhibitors present pharmacological advantages over classical reversible inhibitors (e.g. long target-residence times, resulting in prolonged efficacy with minimal unwanted side effects), slow-binding inhibitors of ChEs are promising new drugs for treatment of Alzheimer disease, myasthenia, and neuroprotection. SBI is also of toxicological importance; it may play a role in mechanisms of resistance and protection against poisoning by irreversible agents.
dc.relation.ispartofseries Archives of Biochemistry and Biophysics
dc.subject Acetylcholinesterase
dc.subject Butyrylcholinesterase
dc.subject Residence time
dc.subject Slow-binding inhibition
dc.subject Tight-binding inhibition
dc.title Slow-binding inhibition of cholinesterases, pharmacological and toxicological relevance
dc.type Review
dc.relation.ispartofseries-volume 593
dc.collection Публикации сотрудников КФУ
dc.relation.startpage 60
dc.source.id SCOPUS00039861-2016-593-SID84958157466


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  • Публикации сотрудников КФУ Scopus [24551]
    Коллекция содержит публикации сотрудников Казанского федерального (до 2010 года Казанского государственного) университета, проиндексированные в БД Scopus, начиная с 1970г.

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