title: Inhibitors of emerging epigenetic targets for cancer therapy: a patent review (2010-2014).
abstract: Gene regulatory pathways comprise an emerging and active area of chemical probe discovery and investigational drug development. Emerging insights from cancer genome sequencing and chromatin biology have identified leveraged opportunities for development of chromatin-directed small molecules as cancer therapies. At present, only six agents in two epigenetic target classes have been approved by the US FDA, limited to treatment of hematological malignancies. Recently, new classes of epigenetic inhibitors have appeared in literatures. First-in-class compounds have successfully transitioned to clinical investigation, importantly also in solid tumors and pediatric malignancies. This review considers patent applications for small-molecule inhibitors of selected epigenetic targets from 2010 to 2014. Included are exemplary classes of chromatin-associated epigenomic writers (DOT1L and EZH2), erasers (LSD1) and readers (BRD4).
authors.affiliation: Department of Medical Oncology, Dana-Farber Cancer Institute, 360 Longwood Avenue, Boston, MA 02215, USA.|Department of Medicine, Harvard Medical School, 25 Shattuck Street, Boston, MA 02115, USA.
authors.forename: Minoru
authors.initials: M
authors.lastname: Tanaka
authors.affiliation: Department of Medical Oncology, Dana-Farber Cancer Institute, 360 Longwood Avenue, Boston, MA 02215, USA.
authors.forename: Justin M
authors.initials: JM
authors.lastname: Roberts
authors.forename: Jun
authors.initials: J
authors.lastname: Qi
authors.affiliation: Department of Medical Oncology, Dana-Farber Cancer Institute, 360 Longwood Avenue, Boston, MA 02215, USA.|Department of Medicine, Harvard Medical School, 25 Shattuck Street, Boston, MA 02115, USA.
authors.forename: James E
authors.initials: JE
authors.lastname: Bradner
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000737:chemistry; D016503:Drug Delivery Systems / Q000379:methods* / Q000639:trends; D057890:Epigenomics / Q000379:methods* / Q000639:trends; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy* / Q000235:genetics; D010330:Patents as Topic
chemical_list: D000970:Antineoplastic Agents