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. Author manuscript; available in PMC: 2017 Apr 24.
Published in final edited form as: Nat Chem Biol. 2016 Oct 24;12(12):1089–1096. doi: 10.1038/nchembio.2209

Figure 1. Rational design of bivalent BET family bromodomain inhibitors.

Figure 1

(a) Structure and activity of the prototype BET family bromodomain inhibitor JQ1 and its close analog MS417. General chemical structure and design of dimeric JQ1-like molecules are also shown. Linkage sites at the 6 position of the diazepine and the 2 position of the thiophene are indicated. (b,c) BRD4(1) biochemical and MV4;11 cellular activity of the (b) (6+6) homo-dimer and the (c) (2+2) homo-dimer. Biochemical and cellular data represent the mean of at least 2 or 4 replicates, respectively ± SD.