FKBP12 in complex with bifunctional ligand a1d and the first bromodomain of BRD4

Non-catalytic heterobifunctional molecules promise to expand the range of therapeutic options by establishing complexes between key target proteins and presenter with additional functions. Here, we present the structure of a bifunctional ligand which induces a ternary complex with the immunophilin FKBP12 and the first bromodomain of the transcriptional regulator BRD4. The complex structure has been solved at a resolution of 1.8A.