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A Fluorometric CYP19A1 (Aromatase) Activity Assay in Live Cells
- 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.
- Subjects :
- Cell
Estrogen receptor
Biochemistry
Article
Structure-Activity Relationship
Aromatase
Drug Discovery
medicine
Humans
Fluorometry
Pharmacologic therapy
Viability assay
General Pharmacology, Toxicology and Pharmaceutics
Estrogen synthesis
Fluorescent Dyes
Pharmacology
Dose-Response Relationship, Drug
Molecular Structure
biology
Aromatase Inhibitors
Chemistry
Organic Chemistry
Cytochrome P450
Enzyme assay
HEK293 Cells
medicine.anatomical_structure
Cancer research
biology.protein
Molecular Medicine
Subjects
Details
- ISSN :
- 18607187 and 18607179
- Volume :
- 16
- Database :
- OpenAIRE
- Journal :
- ChemMedChem
- Accession number :
- edsair.doi.dedup.....c3c994635e5d4170258d9efd321edcf5