title: BET Bromodomain Proteins as Cancer Therapeutic Targets.
abstract: Epigenetic regulators are emerging therapeutic targets in a wide variety of human cancers. BET bromodomain proteins have been identified as key regulators of oncogenic transcription factors including MYC; therefore, their inhibition might provide a way to block these "undruggable" targets. Several BET bromodomain inhibitors are in clinical development with promising preliminary findings. However, tumors acquire resistance to these agents in several different ways. In this review, we summarize the role that BET bromodomain proteins play in tumorigenesis as well as the molecular mechanisms underlying therapeutic responses and resistance to their inhibition with emphasis on BRD4 and breast cancer.
authors.affiliation: Department of Medical Oncology, Dana-Farber Cancer Institute; Department of Medicine, Brigham and Women's Hospital; and Department of Medicine, Harvard Medical School, Boston, Massachusetts 02215.
authors.forename: Shaokun
authors.initials: S
authors.lastname: Shu
authors.affiliation: Department of Medical Oncology, Dana-Farber Cancer Institute; Department of Medicine, Brigham and Women's Hospital; and Department of Medicine, Harvard Medical School, Boston, Massachusetts 02215.
authors.forename: Kornelia
authors.initials: K
authors.lastname: Polyak
mesh_terms: D000818:Animals; D018797:Cell Cycle Proteins; D049109:Cell Proliferation / Q000502:physiology; D044127:Epigenesis, Genetic / Q000502:physiology*; D006801:Humans; D009369:Neoplasms / Q000378:metabolism / Q000628:therapy*; D009687:Nuclear Proteins / Q000378:metabolism*; D014157:Transcription Factors / Q000378:metabolism*; D000092468:Bromodomain Containing Proteins
chemical_list: D018797:Cell Cycle Proteins; D009687:Nuclear Proteins; D014157:Transcription Factors; C441289:BRD4 protein, human; D000092468:Bromodomain Containing Proteins