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Biochemicals> | … terminal His-tag. These constructs were cloned, expressed, and purified by nickel affinity and size exclusion chromatography by either Genscript or Xtal BioStructures, frozen at −80 °C for competition experiments. Time Resolved … | Get A Quote |
Bromodomains are key transcriptional regulators that are thought to be druggable epigenetic targets for cancer, inflammation, diabetes and cardiovascular therapeutics. Of particular importance is the first of two bromodomains in bromodomain containing 4 protein (BRD4(1)). Protein-ligand docking in BRD4(1) was used to purchase a small, focused screening set of compounds possessing a large variety of core structures. Within this set, a small number of weak hits each contained a dihydroquinoxalinone ring system. We purchased other analogs with this ring system and further validated the new hit series and obtained improvement in binding inhibition. Limited exploration by new analog synthesis showed that the binding... More