Bromodomain protein inhibitors reorganize the chromatin of synovial fibroblasts

M Krošel, L Moser, M Houtman, J Friščić, M Tomšič… - Cells, 2023 - mdpi.com
Bromodomain-and extra-terminal domain (BET) proteins are epigenetic reader proteins that
regulate transcription of their target genes by binding to acetylated histone side chains …

Bromodomain and extra-terminal domain bromodomain inhibition prevents synovial inflammation via blocking IκB kinase–dependent NF-κB activation in rheumatoid …

Y Xiao, L Liang, M Huang, Q Qiu, S Zeng, M Shi… - …, 2016 - academic.oup.com
Objective. To explore the roles of the bromodomain (Brd) and extra-terminal domain (BET) of
chromatin adaptors in regulating synovial inflammation in RA. Methods. Fibroblast-like …

RVX-297, a BET bromodomain inhibitor, has therapeutic effects in preclinical models of acute inflammation and autoimmune disease

R Jahagirdar, S Attwell, S Marusic, A Bendele… - Molecular …, 2017 - ASPET
Bromodomain (BD) and extra-terminal domain containing proteins (BET) are chromatin
adapters that bind acetylated histone marks via two tandem BDs, BD1 and BD2, to regulate …

Bromodomain protein inhibition: a novel therapeutic strategy in rheumatic diseases

K Klein - RMD open, 2018 - rmdopen.bmj.com
The reading of acetylation marks on histones by bromodomain (BRD) proteins is a key event
in transcriptional activation. Small molecule inhibitors targeting bromodomain and extra …

The bromodomain protein inhibitor I-BET151 suppresses expression of inflammatory genes and matrix degrading enzymes in rheumatoid arthritis synovial fibroblasts

K Klein, PA Kabala, AM Grabiec, RE Gay… - Annals of the …, 2016 - ard.bmj.com
Objective To investigate the effects of BET bromodomain protein inhibition on inflammatory
activation and functional properties of rheumatoid arthritis synovial fibroblasts (RASF) …

Selective inhibition of CD4+ T-cell cytokine production and autoimmunity by BET protein and c-Myc inhibitors

HS Bandukwala, J Gagnon, S Togher… - Proceedings of the …, 2012 - National Acad Sciences
Bromodomain-containing proteins bind acetylated lysine residues on histone tails and are
involved in the recruitment of additional factors that mediate histone modifications and …

BRD3 Regulates the Inflammatory and Stress Response in Rheumatoid Arthritis Synovial Fibroblasts

T Seifritz, M Brunner, E Camarillo Retamosa… - Biomedicines, 2023 - mdpi.com
Background: Individual functions of members of the bromodomain (BRD) and extra-terminal
(BET) protein family underlying the anti-inflammatory effects of BET inhibitors in rheumatoid …

Evaluating the bromodomain protein BRD1 as a therapeutic target in rheumatoid arthritis

K Klein, M Kato, M Frank-Bertoncelj, C Kolling… - Scientific reports, 2018 - nature.com
Targeting epigenetic reader proteins by small molecule inhibitors represents a new
therapeutic concept in autoimmune diseases such as rheumatoid arthritis (RA). Although …

Reset of inflammatory priming of joint tissue and reduction of the severity of arthritis flares by bromodomain inhibition

J Friščić, C Reinwald, M Böttcher… - Arthritis & …, 2023 - Wiley Online Library
Objective We have recently shown that priming of synovial fibroblasts (SFs) drives arthritis
flares. Pathogenic priming of SFs is essentially mediated by epigenetic reprogramming …

Pharmacological inhibition of bromodomain-containing proteins in inflammation

U Schaefer - Cold Spring Harbor Perspectives in Biology, 2014 - cshperspectives.cshlp.org
Inflammation is associated with the activation of genes that contribute to immune defense
and tissue repair. The bromodomain-containing proteins of the BET family, which recognize …