Human carboxylesterase 1 (CES1) and 2 (CES2) are serine hydrolases that are responsible for the metabolism of many ester-containing drugs, including methylphenidate (Ritalin), which treats ADHD, and remdesivir (Veklury), which is the first drug approved by the FDA for COVID-19 treatment. Although CESs are important to human health, only a few methods exist to study their activity. CES activity is known to be variable in humans due to a variety of factors, such as single nucleotide polymorphisms (SNPs), drug-drug interactions (DDIs), and alternative RNA splicing. To expand the deficit of methods to study CESs, our group is interested in developing new fluorogenic chemical tools that can monitor CES activity in live cells. Here we report the <i>in vitro</i> characterization of potential CES chemical tools focused on ensuring their suitability for use in living systems. The chemical tools we develop should prove useful for studying CESs and will result in a better understanding of their role in drug metabolism and human health.

<i>In vitro </i>characterization of fluorogenic chemical tools to study human carboxylesterases (CESs)

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In vitro characterization of fluorogenic chemical tools to study human carboxylesterases (CESs)