BioCentury
ARTICLE | Distillery Therapeutics

Therapeutics: Histone methyltransferase DOT1L (DOT1L); bromodomain containing 4 (BRD4)

April 14, 2016 7:00 AM UTC

Cell culture studies suggest combining inhibitors of DOT1L and BRD4 could help treat mixed lineage leukemia (MLL). In mouse hematopoietic cells transformed by a chimeric version of the MLL-ENL fusion oncogene, a DOT1L inhibitor tool compound plus a BRD4 inhibitor tool compound decreased proliferation compared with the DOT1L inhibitor alone. Next steps could include testing the combination therapy in an animal model of MLL.

Resverlogix Corp and Shenzhen Hepalink Pharmaceutical Co. Ltd. have apabetalone, a BRD4 inhibitor, in Phase III testing to treat Type II diabetes and prevent major cardiac events in patients with coronary artery disease (CAD) and Type II diabetes, Phase II testing to treat atherosclerosis and Phase I testing to treat Alzheimer's disease (AD). ...