A Fluorometric CYP19A1 (Aromatase) Activity Assay in Live Cells.

David K HeidarySarah M KrigerAustin C HacheyEdith C Glazer

Published in: ChemMedChem (2021)

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.

Keyphrases

high throughput
estrogen receptor
induced apoptosis
single cell
cell cycle arrest
endoplasmic reticulum stress
oxidative stress
cell therapy
cell death
signaling pathway
mesenchymal stem cells
mass spectrometry
bone marrow
protein protein
pi k akt
replacement therapy
amino acid
smoking cessation