Carbonate-Based Fluorescent Chemical Tool for Uncovering Carboxylesterase 1 (CES1) Activity Variations in Live Cells.
Chembiochem
; 23(12): e202200069, 2022 06 20.
Article
in En
| MEDLINE
| ID: mdl-35255177
ABSTRACT
Carboxylesterase 1 (CES1) plays a key role in the metabolism of endogenous biomolecules and xenobiotics including a variety of pharmaceuticals. Despite the established importance of CES1 in drug metabolism, methods to study factors that can vary CES1 activity are limited with only a few suitable for use in live cells. Herein, we report the development of FCP1, a new CES1 specific fluorescent probe with a unique carbonate substrate constructed from commercially available reagents. We show that FCP-1 can specifically report on endogenous CES1 activity with a robust fluorescence response in live HepG2 cells through studies with inhibitors and genetic knockdowns. Subsequently, we deployed FCP-1 to develop a live cell fluorescence microscopy-based approach to identify activity differences between CES1 isoforms. To the best of our knowledge, this is the first application of a fluorescent probe to measure the activity of CES1 sequence variants in live cells.
Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Carboxylic Ester Hydrolases
/
Carboxylesterase
Type of study:
Prognostic_studies
Language:
En
Journal:
Chembiochem
Journal subject:
BIOQUIMICA
Year:
2022
Document type:
Article
Affiliation country: