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dc.contributor.authorRamsay, Rona R.
dc.contributor.authorTipton, Keith F.
dc.identifier.citationRamsay , R R & Tipton , K F 2017 , ' Assessment of enzyme inhibition : a review with examples from the development of monoamine oxidase and cholinesterase inhibitory drugs ' , Molecules , vol. 22 , no. 7 , 1192 .
dc.identifier.otherPURE: 250484001
dc.identifier.otherPURE UUID: 06b7ab06-ab80-491b-9b1f-fc1c834f70f3
dc.identifier.otherScopus: 85042431862
dc.identifier.otherWOS: 000406621300166
dc.descriptionBoth authors are grateful for the collaborations on multi-target drugs facilitated by COST Action CM1103 (2011-2015).en
dc.description.abstractThe 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.
dc.rights© 2017 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (
dc.subjectAlzheimer’s diseaseen
dc.subjectl-deprenyl (selegiline)en
dc.subjectInhibitor constanten
dc.subjectEnzyme inhibitionen
dc.subjectMultitarget-directed ligand (MTDL)en
dc.subjectQH301 Biologyen
dc.subjectQH426 Geneticsen
dc.subjectRM Therapeutics. Pharmacologyen
dc.subjectChemistry (miscellaneous)en
dc.titleAssessment of enzyme inhibition : a review with examples from the development of monoamine oxidase and cholinesterase inhibitory drugsen
dc.typeJournal itemen
dc.contributor.sponsorEuropean Commissionen
dc.description.versionPublisher PDFen
dc.contributor.institutionUniversity of St Andrews. School of Biologyen
dc.contributor.institutionUniversity of St Andrews. Biomedical Sciences Research Complexen
dc.description.statusPeer revieweden

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