XAV939 稳定 AXIN
中文名称
通路描述
XAV939 结合到 tankyrase 1 和 2 的催化位点并抑制 AXIN1 和 2 的 ADP-核糖基化。用 XAV939 处理细胞可显著增加 AXIN1 和 2 的蛋白水平，但不增加 mRNA 水平，并支持 GSK3β-AXIN 复合物的显著增加。这些细胞还显示β-猫enin 磷酸化增加、β-猫enin 蛋白水平降低和β-猫enin 依赖性转录相应降低。用 XAV939 处理 DLD-1 细胞已被证明抑制增殖（Huang 等，2009）。XAV939 尚未在临床环境中进行测试。
英文描述
XAV939 stabilizes AXIN XAV939 binds to the catalytic sites of tankyrase 1 and 2 and inhibits the ADP-ribosylation of AXIN1 and 2. Treatment of cells with XAV939 significantly increases the protein, but not the mRNA levels of AXIN1 and 2 and supports a strong increase in the level of GSK3beta-AXIN complexes. These cells also show increased phosphorylation of beta-catenin, decreased beta-catenin protein levels and a corresponding decrease in beta-catenin dependent transcription. Treatment of DLD-1 cells with XAV939 has also been shown to inhibit proliferation (Huang et al, 2009). XAV939 has not been tested in a clinical setting.
所含基因
2 个基因