title: Therapeutic strategies to inhibit MYC.
abstract: MYC is a master regulator of stem cell state, embryogenesis, tissue homeostasis, and aging. As in health, in disease MYC figures prominently. Decades of biological research have identified a central role for MYC in the pathophysiology of cancer, inflammation, and heart disease. The centrality of MYC to such a vast breadth of disease biology has attracted significant attention to the historic challenge of developing inhibitors of MYC. This review will discuss therapeutic strategies toward the development of inhibitors of MYC-dependent transcriptional signaling, efforts to modulate MYC stability, and the elusive goal of developing potent, direct-acting inhibitors of MYC.
authors.affiliation: Department of Medical Oncology, Dana-Farber Cancer Institute, Boston, Massachusetts 02215.
authors.forename: Michael R
authors.initials: MR
authors.lastname: McKeown
authors.affiliation: Department of Medical Oncology, Dana-Farber Cancer Institute, Boston, Massachusetts 02215 Center for the Science of Therapeutics, Broad Institute, Cambridge, Massachusetts 02141 Department of Medicine, Harvard Medical School, Boston, Massachusetts 02115.
authors.forename: James E
authors.initials: JE
authors.lastname: Bradner
mesh_terms: D000818:Animals; D043171:Chromosomal Instability; D015195:Drug Design; D005786:Gene Expression Regulation; D016259:Genes, myc / Q000235:genetics*; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy* / Q000235:genetics*; D016271:Proto-Oncogene Proteins c-myc / Q000037:antagonists & inhibitors*; D015398:Signal Transduction; D014158:Transcription, Genetic
chemical_list: D016271:Proto-Oncogene Proteins c-myc