A Fluorometric CYP19A1 (Aromatase) Activity Assay in Live Cells.

David K Heidary, Sarah M Kriger, Austin C Hachey, Edith C Glazer

ChemMedChem 2021 Sep 16

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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. © 2021 Wiley-VCH GmbH.

Citation

David K Heidary, Sarah M Kriger, Austin C Hachey, Edith C Glazer. A Fluorometric CYP19A1 (Aromatase) Activity Assay in Live Cells. ChemMedChem. 2021 Sep 16;16(18):2845-2850