Phospho-BRD4: transcription plasticity and drug targeting

CM Chiang - Drug Discovery Today: Technologies, 2016 - Elsevier
BRD4 is an epigenetic regulator and transcription cofactor whose phosphorylation by CK2
and dephosphorylation by PP2A modulates its function in chromatin targeting, factor
recruitment, and cancer progression. While the bromodomains of BET family proteins,
including BRD4, BRD2, BRD3 and BRDT, have been the primary targets of small
compounds such as JQ1, I-BET and MS417 that show promising anticancer effects against
some hematopoietic cancer and solid tumors, drug resistance upon prolonged treatment …