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

6 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

Publisher Copyright:
© 2021 Wiley-VCH GmbH

Keywords

Aromatase
Assay development
Breast cancer
CYP19A1
Cytochrome P450

ASJC Scopus subject areas

Drug Discovery
General Pharmacology, Toxicology and Pharmaceutics
Molecular Medicine
Biochemistry
Pharmacology
Organic Chemistry

UN SDGs

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

Access to Document

10.1002/cmdc.202100326

Cite this

@article{9e11af18e5b94f0eadc123ea6f19c8ff,

title = "A Fluorometric CYP19A1 (Aromatase) Activity Assay in Live Cells",

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.",

keywords = "Aromatase, Assay development, Breast cancer, CYP19A1, Cytochrome P450",

author = "Heidary, {David K.} and Kriger, {Sarah M.} and Hachey, {Austin C.} and Glazer, {Edith C.}",

note = "Publisher Copyright: {\textcopyright} 2021 Wiley-VCH GmbH",

year = "2021",

month = sep,

day = "16",

doi = "10.1002/cmdc.202100326",

language = "English",

volume = "16",

pages = "2845--2850",

number = "18",

}

TY - JOUR

T1 - A Fluorometric CYP19A1 (Aromatase) Activity Assay in Live Cells

AU - Heidary, David K.

AU - Kriger, Sarah M.

AU - Hachey, Austin C.

AU - Glazer, Edith C.

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

UR - http://www.scopus.com/inward/record.url?scp=85109080975&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=85109080975&partnerID=8YFLogxK

U2 - 10.1002/cmdc.202100326

DO - 10.1002/cmdc.202100326

M3 - Article

C2 - 34224206

AN - SCOPUS:85109080975

SN - 1860-7179

VL - 16

SP - 2845

EP - 2850

JO - ChemMedChem

JF - ChemMedChem

IS - 18

ER -

A Fluorometric CYP19A1 (Aromatase) Activity Assay in Live Cells

Abstract

Bibliographical note

Keywords

ASJC Scopus subject areas

UN SDGs

Access to Document

Other files and links

Fingerprint

Cite this