Progress in Study of Bromodomain-Containing Protein 4 and Its Inhibitors / 中国药学杂志

ABSTRACT

In the last several year, the bromodomain and extra-terminal domain(BET) subfamily has been an extensively researched target. The bromodomain-containing protein 4(BRD4) belongs to this subfamily. It can regulate transcription, mark the mitosis of mammals, and regulate cell cycle so that it plays a quite significant role in the development and progression of cancer as well as the production of fibrosis and inflammation. Therefore BRD4 inhibitors have been widely studied for the treatment of solid tumors, leukemia, and fibrosis. Based on vast literature, this paper mainly described the structure and function of BRD4 as well as the latest progress in the research of the structure-activity relationship of BRD4 inhibitors.