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.
Original language | English |
---|---|
Pages (from-to) | 2845-2850 |
Number of pages | 6 |
Journal | ChemMedChem |
Volume | 16 |
Issue number | 18 |
DOIs | |
State | Published - Sep 16 2021 |
Bibliographical note
Publisher Copyright:© 2021 Wiley-VCH GmbH
Keywords
- Aromatase
- Assay development
- Breast cancer
- CYP19A1
- Cytochrome P450
ASJC Scopus subject areas
- Drug Discovery
- General Pharmacology, Toxicology and Pharmaceutics
- Molecular Medicine
- Biochemistry
- Pharmacology
- Organic Chemistry