Rational Design of Selective Allosteric Inhibitors of PHGDH and Serine Synthesis with Anti-tumor Activity

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• 作者：Qian Wang¹ ; ⁶ ; Maria V. Liberti² ; ³ ; ⁶ ; Pei Liu¹ ; Xiaobing Deng⁴ ; Ying Liu¹ ; ⁵ ; Jason W. Locasale² ; ^{jason.locasale@duke.edu} ; Luhua Lai¹ ; ⁴ ; ⁵ ; ⁷ ; ^{lhlai@pku.edu.cn}
• 关键词：cancer cell metabolism ; PHGDH ; de novo serine synthesis ; allosteric inhibitor ; rational design ; virtual screen ; anti-tumor ; in vivo
• 刊名：Cell Chemical Biology
• 出版年：2017
• 出版时间：19 January 2017
• 年：2017
• 卷：24
• 期：1
• 页码：55-65
• 全文大小：3042 K
• 卷排序：24

文摘

Two previously unknown allosteric sites on PHGDH were identified Inhibitors that bind to these sites were discovered Inhibitors bound to PHGDH in cells and reduced the synthesis of serine and glycine Inhibitors suppressed tumor growth in mice