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

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. Incorporatio

SUBMITTER: Ramsay RR 

PROVIDER: S-EPMC6152246 | biostudies-literature | 2017 Jul

REPOSITORIES: biostudies-literature