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 journalArticlepeer-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 languageEnglish
Pages (from-to)2845-2850
Number of pages6
JournalChemMedChem
Volume16
Issue number18
DOIs
StatePublished - 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

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