Title : Carbonate-Based Fluorescent Chemical Tool for Uncovering Carboxylesterase 1 (CES1) Activity Variations in Live Cells - Singh_2022_Chembiochem__ |
Author(s) : Singh A , Gao M , Karns CJ , Spidle TP , Beck MW |
Ref : Chembiochem , : , 2022 |
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. |
PubMedSearch : Singh_2022_Chembiochem__ |
PubMedID: 35255177 |
Singh A, Gao M, Karns CJ, Spidle TP, Beck MW (2022)
Carbonate-Based Fluorescent Chemical Tool for Uncovering Carboxylesterase 1 (CES1) Activity Variations in Live Cells
Chembiochem
:
Singh A, Gao M, Karns CJ, Spidle TP, Beck MW (2022)
Chembiochem
: