抑制ATR與FANCD2激活之組成物與方法Methods and compositions for inhibition of ATR and FANCD2 activation

專利類型

發明

專利國別 (專利申請國家)

中華民國

專利申請案號

101117920

專利證號

I 486341

專利獲證名稱

抑制ATR與FANCD2激活之組成物與方法Methods and compositions for inhibition of ATR and FANCD2 activation

專利所屬機關 (申請機關)

高雄醫學大學

獲證日期

2015/06/01

技術說明

癌症治療時造成DNA損傷會活化ATM與ATR磷酸酶進而啟動Chk1和Chk2磷酸酶活化，這也就是DNA損傷反應的訊息傳遞。過去研究已經證實ATR抑制劑對於ATM或p53缺陷的癌症細胞能夠促進DNA損傷藥物的療效。本技術係揭示式 (I) 或式 (II) 兩系列黃酮類架構化合物或所形成之藥學組合物，可抑制ATR與FANCD2之DNA複製、細胞週期監測點和DNA修復的功能，而具備改善DNA損傷類之抗癌藥物的敏感性，以及預後不良之症狀。 DNA damage caused during cancer treatment can rapidly activate the ataxia telangiectasia-mutated (ATM)/Rad3-related (ATR)-dependent phosphorylation of Chk2 and Chk1 kinases, which are hallmarks of DNA damage response (DDR). Pharmacological inhibition of ATR causes a synthetic lethal effect on ATM or p53 defective cancers suggest that such inhibition is an effective way of improving the sensitivity of cancers to DNA-damaging agents. This invention is announcing a composition of flavonoid skeleton in the formula (I) or formula (II) compound, which inhibites functions of ATR and FANCD2 on DNA replication, damage checkpoint, and repair; therefore, this composition can improve the cancer sensitivity and poor prognosis to DNA-damaging theraputices.

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連絡單位 (專責單位/部門名稱)

智財保護與科技管理組

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07-3138030

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