摘要: Protein factors can regulate gene expression by binding to specifically modified DNA-associated proteins. Small molecules that selectively interfere with such interaction may be of therapeutic value. See Article p.1067 & Letter p.1119 perturb chromatin proteins are an emerging focus current biomedical research. Two groups reporting in this issue have targeted bromodomain-containing BET bind acetylated lysine residues during activation, arriving at cell-permeable small molecule compounds similar structures based on fused triazole-diazepine rings. James Bradner and colleagues report the development a compound named JQ1. The protein BRD4, two bromodomains, is implicated human squamous cell carcinoma. JQ1 inhibits growth BRD4-dependent tumours mouse models. Alexander Tarakhovsky colleagues' inhibitor, I-BET, shown certain family members histones. It activation pro-inflammatory genes macrophages has immunomodulatory activity model inflammatory disease.
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