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A Fluorometric CYP19A1 (Aromatase) Activity Assay in Live Cells

Authors :
Edith C. Glazer
Sarah M. Kriger
David K. Heidary
Austin C. Hachey
Source :
ChemMedChem
Publication Year :
2021
Publisher :
Wiley, 2021.

Abstract

Inhibition of estrogen synthesis is an integral component of the frontline pharmacologic therapy for the treatment of estrogen receptor positive cancers. However, there is currently no direct, high-throughput-ready assay for aromatase (also known as CYP19A1) that can be performed in live cells. Herein we present a cell-based assay that allows for multiplexed assessment of enzyme activity, protein half-life, cell viability, and identification of inhibitors with slow off-rates.

Details

ISSN :
18607187 and 18607179
Volume :
16
Database :
OpenAIRE
Journal :
ChemMedChem
Accession number :
edsair.doi.dedup.....c3c994635e5d4170258d9efd321edcf5