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Cited by 258

The DOI matches its Crossref record; 180 of the 180 references it cites were found in a registry or an index.

Assessment of Enzyme Inhibition: A Review with Examples from the Development of Monoamine Oxidase and Cholinesterase Inhibitory Drugs

Open access
Ramsay, Rona, Tipton, Keith·2017·Molecules

Abstract

The actions of many drugs involve enzyme inhibition. This is exemplified by the inhibitors of monoamine oxidases (MAO) and the cholinsterases (ChE) that have been used for several pharmacological purposes. This review describes key principles and approaches for the reliable determination of enzyme activities and inhibition as well as some of the methods that are in current use for such studies with these two enzymes. Their applicability and potential pitfalls arising from their inappropriate use are discussed. Since inhibitor potency is frequently assessed in terms of the quantity necessary to give 50% inhibition (the IC50 value), the relationships between this and the mode of inhibition is also considered, in terms of the misleading information that it may provide. Incorporation of more than one functionality into the same molecule to give a multi-target-directed ligands (MTDLs) requires careful assessment to ensure that the specific target effects are not significantly altered and that the kinetic behavior remains as favourable with the MTDL as it does with the individual components. Such factors will be considered in terms of recently developed MTDLs that combine MAO and ChE inhibitory functions.

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Crossref · 10.3390/molecules22071192

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Metadata

Authors
Ramsay, R., & Tipton, K.
Venue
Molecules
Publisher
MDPI AG
Published
2017-07-15
Volume
22
Issue
7
Pages
1192
ISSN
1420-3049 (ISSN-L)
OpenAlex
W2734510265
Cited by
258
References
180
FWCI
12.43
Type
journal article
Language
en
Open access
gold

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CoChat. (2026). Citation check: Assessment of Enzyme Inhibition: A Review with Examples from the Development of Monoamine Oxidase and Cholinesterase Inhibitory Drugs. https://app.cochat.ai/papers/10.3390/molecules22071192
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Ramsay, R., & Tipton, K. (2017). Assessment of Enzyme Inhibition: A Review with Examples from the Development of Monoamine Oxidase and Cholinesterase Inhibitory Drugs. Molecules. https://doi.org/10.3390/molecules22071192

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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).

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