Discovery of a Selective BET Inhibitor for Treating Osteoarthritis

Bromodomain and extra-terminal domain (BET) family proteins are key regulators of gene transcription and have been implicated in a wide range of diseases, making these proteins a potential therapeutic target.  Abnormal BET protein activity has been linked to cancer, inflammatory disorders, viral infections, and neurodegenerative conditions.

In a recent publication, researchers highlight the discovery of a selective BET inhibitor, BBC0906.  The authors demonstrate that BBC0906 attenuated cartilage degradation and alleviated osteoarthritis (OA) in an OA mouse model.  Significantly, BBC0906 was discovered from WuXi AppTec’s DNA-encoded library (DEL), demonstrating the versatility of DEL and DEL screening at WuXi AppTec.