A Fluorometric CYP19A1 (Aromatase) Activity Assay in Live Cells

David K. Heidary; Sarah M. Kriger; Austin C. Hachey; Edith C. Glazer

doi:10.1002/cmdc.202100326

A Fluorometric CYP19A1 (Aromatase) Activity Assay in Live Cells

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

Research output: Contribution to journal › Article › peer-review

2 Scopus citations

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.

Original language	English
Pages (from-to)	2845-2850
Number of pages	6
Journal	ChemMedChem
Volume	16
Issue number	18
DOIs	https://doi.org/10.1002/cmdc.202100326
State	Published - Sep 16 2021

Bibliographical note

Funding Information:
This work was supported by the National Institute of General Medical Sciences of the US National Institutes of Health under Award Number R01GM138882. We also acknowledge the University of Kentucky Light Microscopy Core, which is supported in part by the Office of the Vice President for Research.

Publisher Copyright:
© 2021 Wiley-VCH GmbH

Keywords

Aromatase
Assay development
Breast cancer
CYP19A1
Cytochrome P450

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Pharmacology
Drug Discovery
Pharmacology, Toxicology and Pharmaceutics (all)
Organic Chemistry

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1002/cmdc.202100326

Cite this

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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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AU - Heidary, David K.

AU - Kriger, Sarah M.

AU - Hachey, Austin C.

AU - Glazer, Edith C.

N1 - Funding Information: This work was supported by the National Institute of General Medical Sciences of the US National Institutes of Health under Award Number R01GM138882. We also acknowledge the University of Kentucky Light Microscopy Core, which is supported in part by the Office of the Vice President for Research. Publisher Copyright: © 2021 Wiley-VCH GmbH

PY - 2021/9/16

Y1 - 2021/9/16

N2 - 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.

AB - 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.

KW - Aromatase

KW - Assay development

KW - Breast cancer

KW - CYP19A1

KW - Cytochrome P450

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A Fluorometric CYP19A1 (Aromatase) Activity Assay in Live Cells

Abstract

Bibliographical note

Keywords

ASJC Scopus subject areas

UN SDGs

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