gsk1210151a and Periodontitis

BET bromodomain proteins are important epigenetic regulators of gene expression that bind acetylated histone tails and regulate the formation of acetylation-dependent chromatin complexes. BET inhibitors suppress inflammatory responses in multiple cell types and animal models, and protect against bone loss in experimental periodontitis in mice. Here, we analyzed the role of BET proteins in inflammatory activation of gingival fibroblasts (GFs) and gingival epithelial cells (GECs). We show that the BET inhibitors I-BET151 and JQ1 significantly reduced expression and/or production of distinct, but overlapping, profiles of cytokine-inducible mediators of inflammation and bone resorption in GFs from healthy donors (

Topics: Animals; Azepines; Cytokines; Epithelial Cells; Extracellular Signal-Regulated MAP Kinases; Fibroblasts; Gingiva; Heterocyclic Compounds, 4 or More Rings; Humans; Inflammation; Mice; Periodontitis; Porphyromonas gingivalis; Triazoles