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Molecular Biology Reagents> | ... 2.2. Bromodomain purification. Single bromodomains and dual domain constructs with an N-terminal His-tag were cloned, expressed, and purified by nickel affinity and size-exclusion chromatography by Genscript or Xtal BioStructures. ... | Get A Quote |
Bromodomains are epigenetic readers that specifically bind to the acetyl lysine residues of histones and transcription factors. Small molecule BET bromodomain inhibitors can disrupt this interaction which leads to potential modulation of several disease states. Here we describe the binding properties of a novel BET inhibitor RVX-297 that is structurally related to the clinical compound RVX-208, currently undergoing phase III clinical trials for the treatment of cardiovascular diseases, but is distinctly different in its biological and pharmacokinetic profiles. We report that RVX-297 preferentially binds to the BD2 domains of the BET bromodomain and Extra Terminal (BET) family of protein. We demonstrate the diff... More