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.
|Number of pages||6|
|State||Published - Sep 16 2021|
Bibliographical noteFunding Information:
This work was supported by the National Institute of General Medical Sciences of the US National Institutes of Health under Award Number R01GM138882. We also acknowledge the University of Kentucky Light Microscopy Core, which is supported in part by the Office of the Vice President for Research.
© 2021 Wiley-VCH GmbH
- Assay development
- Breast cancer
- Cytochrome P450
ASJC Scopus subject areas
- Molecular Medicine
- Drug Discovery
- Pharmacology, Toxicology and Pharmaceutics (all)
- Organic Chemistry