Inhibition of the BET family of epigenetic reader proteins: A novel principle for modulating gene expression in IgE-activated mast cells.

ABSTRACT:

Introduction

The BET family of bromodomain-containing proteins constitute epigenetic readers that bind to acetylated lysine residues of core histones, thereby translating epigenetic histone marks to effects on gene expression. BET inhibitors are currently emerging as promising therapeutic agents for treatment of various pathological conditions. Here, we explored the potential of using BET inhibition to modulate IgE-mediated responses in mast cells.

Methods

We assessed the effects of BET inhibitors PFI-1, I-BET151, and I-BET762 on responses downstream of mast cell activation through IgE receptor cross-linking.

Results

BET inhibitors were neither toxic for mast cells (at doses up to 20 μM), nor did they prevent IgE-mediated mast cell degranulation. However, we found tha

SUBMITTER: Garcia-Faroldi G 

PROVIDER: S-EPMC5418135 | biostudies-literature | 2017 Jun

REPOSITORIES: biostudies-literature