METHOD FOR IDENTIFYING COMPOUND FOR INHIBITING AN ACTIVITY OF A HISTONE LYSINE DEMETHYLASE

摘要

The present invention relates to a method for identifying a compound that inhibits an activity of a histone lysine demethylase.

主权项

1. A method for identifying a compound which inhibits an activity of a histone lysine demethylase, comprising:
(a) using a computer program to generate a three-dimensional structure of a pocket of a histone lysine demethylase, wherein the pocket comprises three sites: an alpha-ketoglutarate (AKG), a methylated lysine, and a NIQ; (b) screening for a compound that interacts with the three sites of said pocket; and (c) testing the compound screened in (b) by in vitro or in vivo assay for its ability to inhibit the activity of the histone lysine demethylase, thereby identifying a compound that inhibits the activity of the histone lysine demethylase.