The two major human carboxylesterases (CESs), CES1 and CES2 play a key role in the hydrolysis of xenobiotic esters including oseltamivir (Tamiflu), methylphenidate (Ritalin), and the illicit narcotics cocaine and heroin. CES-mediated metabolism is a major regulator of the pharmacokinetics of these ester-containing drugs. Despite the established role of CESs in drug metabolism, few techniques exist to study their activity in live cells. Fluorogenic chemical tools have been developed to expand the methods used to study CES activity, however, many of these tools are not sufficiently characterized to confidently study CES activity in live cells and are not widely used potentially due to their difficulty to obtain. To address these issues, we are exploring fluorescein as the fluorescent scaffold for CES-specific fluorogenic chemical tools. Fluorescein is a commercially available, affordable, and non-toxic fluorophore with excellent fluorescent properties making it suitable for use in live cells. Overall, our development of  fluorescein-based fluorogenic chemical tools for studying human CESs will result in improved and more accessible methods for studying the role of CESs in human drug metabolism.

Fluorescein-based fluorogenic chemical tools to study human carboxylesterases in live cells

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