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A Fluorometric CYP19A1 (Aromatase) Activity Assay in Live Cells.
Heidary, David K; Kriger, Sarah M; Hachey, Austin C; Glazer, Edith C.
Afiliación
  • Heidary DK; Department of Chemistry, University of Kentucky, 505 Rose St., Lexington, KY 40506, USA.
  • Kriger SM; Department of Chemistry, University of Kentucky, 505 Rose St., Lexington, KY 40506, USA.
  • Hachey AC; Department of Chemistry, University of Kentucky, 505 Rose St., Lexington, KY 40506, USA.
  • Glazer EC; Department of Chemistry, University of Kentucky, 505 Rose St., Lexington, KY 40506, USA.
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.
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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

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
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