A Fluorometric CYP19A1 (Aromatase) Activity Assay in Live Cells.
ChemMedChem
; 16(18): 2845-2850, 2021 09 16.
Article
en En
| MEDLINE
| ID: mdl-34224206
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.
Palabras clave
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Aromatasa
/
Inhibidores de la Aromatasa
/
Colorantes Fluorescentes
/
Fluorometría
Límite:
Humans
Idioma:
En
Revista:
ChemMedChem
Asunto de la revista:
FARMACOLOGIA
/
QUIMICA
Año:
2021
Tipo del documento:
Article
País de afiliación:
Estados Unidos