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Literature DB >> 34224206

A Fluorometric CYP19A1 (Aromatase) Activity Assay in Live Cells.

David K Heidary¹, Sarah M Kriger¹, Austin C Hachey¹, Edith C Glazer¹.

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.

Entities: Chemical

Keywords: Aromatase; Assay development; Breast cancer; CYP19A1; Cytochrome P450

Mesh：

Substances：

Year: 2021 PMID： 34224206 PMCID： PMC9276262 DOI： 10.1002/cmdc.202100326

Source DB: PubMed Journal: ChemMedChem ISSN： 1860-7179 Impact factor: 3.540

24 in total

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Authors: Jessica Caciolla; Alessandra Bisi; Federica Belluti; Angela Rampa; Silvia Gobbi
Journal: Molecules Date: 2020-11-16 Impact factor: 4.411

1 in total

1. Ru(II) photocages enable precise control over enzyme activity with red light.

Authors: Dmytro Havrylyuk; Austin C Hachey; Alexander Fenton; David K Heidary; Edith C Glazer
Journal: Nat Commun Date: 2022-06-25 Impact factor: 17.694

1 in total