Issue 7, 2021

Human carboxylesterases and fluorescent probes to image their activity in live cells

Abstract

Human carboxylesterases (CESs) are serine hydrolases that are responsible for the phase I metabolism of an assortment of ester, amide, thioester, carbonate, and carbamate containing drugs. CES activity is known to be influenced by a variety of factors including single nucleotide polymorphisms, alternative splicing, and drug–drug interactions. These different factors contribute to interindividual variability of CES activity which has been demonstrated to influence clinical outcomes among people treated with CES-substrate therapeutics. Detailed exploration of the factors that influence CES activity is emerging as an important area of research. The use of fluorescent probes with live cell imaging techniques can selectively visualize the real-time activity of CESs and have the potential to be useful tools to help reveal the impacts of CES activity variations on human health. This review summarizes the properties of the five known human CESs including factors reported to or that could potentially influence their activity before discussing the design aspects and use considerations of CES fluorescent probes in general in addition to highlighting several well-characterized probes.

Graphical abstract: Human carboxylesterases and fluorescent probes to image their activity in live cells

Supplementary files

Article information

Article type
Review Article
Submitted
07 Mrz 2021
Accepted
26 Apr 2021
First published
18 Mai 2021

RSC Med. Chem., 2021,12, 1142-1153

Human carboxylesterases and fluorescent probes to image their activity in live cells

A. Singh, M. Gao and M. W. Beck, RSC Med. Chem., 2021, 12, 1142 DOI: 10.1039/D1MD00073J

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