Epigenetic siRNA and Chemical Screens Identify SETD8 Inhibition as a Therapeutic Strategy for p53 Activation in High-Risk Neuroblastoma

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• 作者：Veronica Veschi¹ ; Zhihui Liu¹ ; Ty C. Voss² ; Laurent Ozbun² ; Berkley Gryder³ ; Chunhua Yan⁴ ; Ying Hu⁴ ; Anqi Ma⁵ ; Jian Jin⁵ ; Sharlyn J. Mazur⁷ ; Norris Lam¹ ; Barbara K. Souza¹ ; Giuseppe Giannini⁹ ; Gordon L. Hager⁸ ; Cheryl H. Arrowsmith⁶ ; Javed Khan³ ; Ettore Appella⁷ ; Carol J. Thiele¹ ; ¹⁰ ; ^{ct47a@nih.gov}
• 关键词：SETD8 ; p53 ; neuroblastoma ; epigenetics ; differentiation ; siRNA screen
• 刊名：Cancer Cell
• 出版年：2017
• 出版时间：9 January 2017
• 年：2017
• 卷：31
• 期：1
• 页码：50-63
• 全文大小：3157 K
• 卷排序：31

文摘

We identified 53 epigenetic regulators that control NB growth and/or differentiation SETD8 inhibition activates the p53 pathway by decreasing p53K382me1 levels UNC0379 is a small-molecule inhibitor of SETD8 that activates the p53 pathway SETD8 is validated as a druggable therapeutic target in NB