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

5 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

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

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