dBRD9

dBRD9 is a PROTAC (proteolysis targeting chimera) that can selective degrade BRD9 (Bromodomain containing 9). dBRD9 improves the bromine domain binding profile and reduces the binding activity of the whole BET (bromodomain and extra-terminal) family. CRBN (cereblon) is the substrate-binding component of the E3 protein ligase complex DDB1-CUL4A-RBX1 involved in the ubiquitination and proteasomal degradation of target proteins. Cereblon binds to DDB1 (Damaged DNA binding protein 1), to the scaffolding protein CUL4A (Cullin 4A), and its regulator RBX1 (RING-Box protein 1). Binding of CRBN to a substrate protein engages the E3 ligase activity of the complex and results in the ubiquitination and ultimate degradation of the protein substrate. Many proteins are known targets of CRBN, including several transcription factors, growth factors, kinases and more. CRBN has become a target of choice for the development of many therapeutic PROTACs(R) (proteolysis targeting chimera). BRD9 (Bromodomain-containing protein 9) functions as a transcriptional regulator and is a component of a chromatin remodeling complex. It also regulates the formation of the RAD51-RAD54 complex, involved in homologous recombination. BRD9 plays a role in cancer and is a potential therapeutic target for cancer drugs. dBRD9 is a BRD9 targeting PROTAC.