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

專利類型

發明

專利國別 (專利申請國家)

美國

專利申請案號

15/835,420

專利證號

US 11,279,966

專利獲證名稱

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

專利所屬機關 (申請機關)

國立清華大學

獲證日期

2022/03/22

技術說明

組蛋白離胺酸去甲基酶負責調控細胞組蛋白上離胺酸的甲基化密碼，這類蛋白的突變、放大、消除以及異常的表示現已經在多種癌症中發現，故組蛋白離胺酸去甲基酶已成為新興治療癌症的標的蛋白質。此專利技術提攻一個尋找抑制組蛋白離胺酸去甲基酶之抑制劑的方法，利用電腦軟體模擬建構出組白離胺酸去甲基酶活化位的3D立體結構，包含了三個位點：(1) alpha-KG 位點 (2) 甲基化離胺酸位點 (3) NIQ 位點，利用電腦分析會與此三個位點作用的化合物，再以 in vitro或 in vivo試驗來檢視這些化合物抑制組蛋白離胺酸去甲基酶的活性，藉以找到有效抑制組蛋白離胺酸去甲基酶活性的抑制劑。 The present invention provides 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: 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.

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