title: Compounds and methods for inhibiting histone demethylases: a patent evaluation of US20160102096A1.
abstract: The Jumonji C (JmjC) domain containing histone lysine demethylases have a clear role both in the development and in some diseases including inflammation and cancer. The histone lysine demethylases represent an attractive target for the identification of therapeutic agents and the pyridine derivatives are a scaffolds largely investigated for the identification and development of inhibitors of enzymes of the Jumonji family. This commentary is a scientific evaluation of a patent application US20160102096A1 that describes novel pyridine derivatives in which the introduction of specific substituents is used to modulate the selectivity profile of the inhibitors.
authors.affiliation: a Experimental Therapeutics Unit , IFOM - The FIRC Institute of Molecular Oncology , Milan , Italy.
authors.forename: Florian
authors.initials: F
authors.lastname: Thaler
authors.affiliation: a Experimental Therapeutics Unit , IFOM - The FIRC Institute of Molecular Oncology , Milan , Italy.
authors.forename: Ciro
authors.initials: C
authors.lastname: Mercurio
mesh_terms: D015195:Drug Design; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D056466:Histone Demethylases / Q000037:antagonists & inhibitors*; D006801:Humans; D007249:Inflammation / Q000188:drug therapy / Q000473:pathology; D056484:Jumonji Domain-Containing Histone Demethylases / Q000037:antagonists & inhibitors; D009369:Neoplasms / Q000188:drug therapy / Q000473:pathology; D010330:Patents as Topic; D011725:Pyridines / Q000737:chemistry / Q000494:pharmacology
chemical_list: D004791:Enzyme Inhibitors; D011725:Pyridines; D056466:Histone Demethylases; D056484:Jumonji Domain-Containing Histone Demethylases
keywords: Histone lysine demethylases; Jumonji C (JmjC)-domain containing proteins; KDM2B; KDM4C; KDM5B; PHF8