Human carboxylesterases and fluorescent probes to image their activity in live cells
Autor: | Anchal Singh, Michael W. Beck, Mingze Gao |
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Rok vydání: | 2021 |
Předmět: |
Pharmacology
0303 health sciences Organic Chemistry Alternative splicing Pharmaceutical Science Computational biology Biology 030226 pharmacology & pharmacy Biochemistry Fluorescence Serine 03 medical and health sciences Human health Chemistry 0302 clinical medicine Live cell imaging Drug Discovery Molecular Medicine 030304 developmental biology |
Zdroj: | RSC Med Chem |
ISSN: | 2632-8682 |
Popis: | 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. |
Databáze: | OpenAIRE |
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