Human carboxylesterases and fluorescent probes to image their activity in live cells
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, alter...
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| Published in | MedChemComm Vol. 12; no. 7; pp. 1142 - 1153 |
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| Main Authors | , , |
| Format | Journal Article |
| Language | English |
| Published |
England
Royal Society of Chemistry
21.07.2021
RSC |
| Subjects | |
| Online Access | Get full text |
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| Summary: | 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.
In this review, drug metabolizing human carboxylesterases and fluorescent probes capable of studying their activity in live cells are discussed. |
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| Bibliography: | Michael W. Beck earned his B.S. in Chemistry (Biochemistry Concentration) at Tennessee Technological University in 2011 where he started his research career by performing undergraduate research with Edward Lisic. He then obtained his Ph.D. in Chemistry (2015) at the University of Michigan with Mi Hee Lim. After completing his postdoctoral studies with Bryan Dickinson at the University of Chicago, he joined the Department of Chemistry and Biochemistry at Eastern Illinois University as an assistant professor in 2019. His research group focuses on designing chemical tools to study biological problems in live cells while training the next generation of scientists. Anchal Singh born in Durg, India obtained her B.S. in Biotechnology in 2015 from Sam Higginbottom University of Agricultural Technology and Sciences in Allahabad, India. Her interest in biotechnology was cemented during her undergraduate studies when completing an undergraduate research thesis on genetic alterations in wound healing of diabetes mellitus patients under the guidance of Prof. Kiran Singh and Kanhaiya Kumar. In 2019, she moved to the United States to pursue a M.S. in Biochemistry at Eastern Illinois University working with Michael W. Beck as part of an interdisciplinary research team to complete her thesis studies on human carboxylesterase enzymes. Mingze Gao, born in Xianyang, China, started his undergraduate education at North University of China before transferring to Eastern Illinois University where he is currently pursuing a B.S. in Biological Sciences. He began his research career in 2019 studying transcription factors that are involved in cell migration and outgrowth with Gary Bulla. In 2020, he joined Michael W. Beck's group to study human carboxylesterase enzymes. His research interests revolve around projects that have eventual impacts to human health. Electronic supplementary information (ESI) available. See DOI 10.1039/d1md00073j |
| ISSN: | 2632-8682 2040-2503 2632-8682 2040-2511 |
| DOI: | 10.1039/d1md00073j |