The bromodomain protein module, which binds to acetylated lysine, is emerging as an important epigenetic therapeutic target. We report the structure-guided optimization of 3,5-dimethylisoxazole derivatives to develop potent inhibitors of the BET (bromodomain and extra terminal domain) bromodomain family with good ligand efficiency. X-ray crystal structures of the most potent compounds reveal key interactions required for high affinity at BRD4(1). Cellular studies demonstrate that the phenol a...Expand abstract
- Publication status:
- Publisher copy:
- Copyright date:
Optimization of 3,5-dimethylisoxazole derivatives as potent bromodomain ligands.
If you are the owner of this record, you can report an update to it here: Report update to this record