title: Drugging Chromatin in Cancer: Recent Advances and Novel Approaches.
abstract: Chromatin regulatory mechanisms play a major role in the control of gene expression programs during normal development and are disrupted in specific disease states, particularly in cancer. Important mediators of chromatin regulatory processes can broadly be classified into writers, erasers, and readers of covalent chromatin modifications that modulate eukaryotic gene transcription and maintain the integrity of the genome. The reversibility and disease-specific nature of these chromatin states make these regulators attractive therapeutic targets. As such, there is an ever-increasing number of candidate therapies aimed at targeting cancer-associated chromatin states that are in various stages of preclinical and clinical development. In this review, we discuss recent advances that have been made in the rational therapeutic targeting of chromatin regulatory mechanisms and highlight certain cancers where there is a specific rationale to assess these therapeutic approaches.
authors.affiliation: Cancer Biology and Genetics Program, Departments of Medicine and Pediatrics, Memorial Sloan Kettering Cancer Center, New York, NY 10065, USA.
authors.forename: Sheng F
authors.initials: SF
authors.lastname: Cai
authors.affiliation: Cancer Biology and Genetics Program, Departments of Medicine and Pediatrics, Memorial Sloan Kettering Cancer Center, New York, NY 10065, USA.
authors.forename: Chun-Wei
authors.initials: CW
authors.lastname: Chen
authors.affiliation: Cancer Biology and Genetics Program, Departments of Medicine and Pediatrics, Memorial Sloan Kettering Cancer Center, New York, NY 10065, USA. Electronic address: armstros@mskcc.org.
authors.forename: Scott A
authors.initials: SA
authors.lastname: Armstrong
mesh_terms: D000970:Antineoplastic Agents / Q000494:pharmacology* / Q000627:therapeutic use; D002843:Chromatin / Q000187:drug effects*; D002986:Clinical Trials as Topic; D044127:Epigenesis, Genetic / Q000187:drug effects; D006801:Humans; D058990:Molecular Targeted Therapy; D009369:Neoplasms / Q000188:drug therapy* / Q000235:genetics
chemical_list: D000970:Antineoplastic Agents; D002843:Chromatin