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

Author
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.

Year of Publication
:
2021
Journal
:
ChemMedChem
Volume
:
16
Issue
:
18
Number of Pages
:
2845-2850
Date Published
:
2021
ISSN Number
:
1860-7179
URL
:
https://doi.org/10.1002/cmdc.202100326
DOI
:
10.1002/cmdc.202100326
Short Title
:
ChemMedChem
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