Abstract:
A method for identifying a compound that inhibits an activity of a histone lysine demethylase, in which the compound interacts with three sites of a pocket of the histone lysine demethylase generated by using a computer program, an alpha-ketoglutarate (AKG), a methylated lysine, and a NIQ.
Abstract:
The present invention relates to a method for inhibiting activity of a protein selected from the group consisting of KDM4A, KDM4B, and KDM4C, comprising the step of exposing the protein to an effective inhibiting amount of a compound having the formula wherein R1 is H or C7O5H8; R2 is H, OH, or OCH3; and R3 is H or OH. The present invention also relates to a method for treating or lessening the severity of a disease, condition, or disorder in which modulation of KDM4A, KDM4B, or KDM4C is beneficial, which method comprises administering to a subject suffering from said disease, condition, or disorder a therapeutically-effective amount of: a) a compound having the formula wherein R1 is H or C7O5H8; R2 is H, OH, or OCH3; and R3 is H or OH; or b) a composition comprising the compound and a pharmaceutically acceptable adjuvant, vehicle, or carrier.
Abstract:
A method for identifying a compound that inhibits an activity of a histone lysine demethylase, in which the compound interacts with three sites of a pocket of the histone lysine demethylase generated by using a computer program, an alpha-ketoglutarate (AKG), a methylated lysine, and a NIQ.