A Fluorometric CYP19A1 (Aromatase) Activity Assay in Live Cells

被引：6
|
作者：
Heidary, David K. [1 ]
Kriger, Sarah M. [1 ]
Hachey, Austin C. [1 ]
Glazer, Edith C. [1 ]
机构：
[1] Univ Kentucky, Dept Chem, 505 Rose St, Lexington, KY 40506 USA
来源：
CHEMMEDCHEM | 2021年 / 16卷 / 18期
基金：
美国国家卫生研究院;
关键词：
Aromatase; Cytochrome P450; Breast cancer; Assay development; INHIBITORS; EXEMESTANE; PHARMACOLOGY; DISCOVERY; CHEMICALS; SCREEN;
D O I：
10.1002/cmdc.202100326
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
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.
引用
收藏
页码：2845 / 2850
页数：6
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