title: Epigenetic mechanisms and drug discovery in rheumatology.
abstract: There is a growing understanding of the epigenetic mechanisms that regulate gene expression in healthy conditions and a realisation that dysregulation of these mechanisms is an underlying factor in many human diseases. We discuss studies demonstrating that small molecule inhibitors of epigenetic regulatory proteins can block pathogenic mechanisms associated with rheumatoid arthritis, focusing on the effects of these inhibitors on synovial fibroblasts-fibroblast-like synoviocytes.
authors.affiliation: Epigenetics DPU, Immuno-inflammation Therapy Area, GlaxoSmithKline, Medicines Research Centre, Stevenage, UK;
authors.forename: David F
authors.initials: DF
authors.lastname: Tough
authors.affiliation: Epigenetics DPU, Immuno-inflammation Therapy Area Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage, UK;
authors.forename: Rab K
authors.initials: RK
authors.lastname: Prinjha
authors.affiliation: Immuno-inflammation Therapy Area Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage, UK paul-peter.x.tak@gsk.com.
authors.forename: Paul P
authors.initials: PP
authors.lastname: Tak
mesh_terms: D055808:Drug Discovery; D044127:Epigenesis, Genetic; D006801:Humans; D012219:Rheumatology
keywords: BRD4; Epigenetic; bromodomain; fibroblast-like synoviocyte; histone acetyltransferase; rheumatoid arthritis; rheumatology; synovial fibroblast