Bromodomain (BRD)-containing kinases initiate acetylation-dependent assembly of transcriptional regulator complexes by binding to (or 'reading') acetyl-lysine marks on histone tails. The regulator complexes thus formed, control expression of sets of proteins which alter the cellular phenotype in specific ways. (BRD)-containing proteins are exciting targets for the development of novel small molecule therapeutics in the areas of cancer, inflammation and viral infection [1].

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2. Picaud S, Wells C, Felletar I, Brotherton D, Martin S, Savitsky P, Diez-Dacal B, Philpott M, Bountra C, Lingard H et al.. (2013) RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain. Proc Natl Acad Sci USA, 110 (49): 19754-9. [PMID:24248379]

3. Theodoulou NH, Bamborough P, Bannister AJ, Becher I, Bit RA, Che KH, Chung CW, Dittmann A, Drewes G, Drewry DH et al.. (2016) Discovery of I-BRD9, a Selective Cell Active Chemical Probe for Bromodomain Containing Protein 9 Inhibition. J Med Chem, 59 (4): 1425-39. [PMID:25856009]