Yuxiao Tang , Xiaobin Zhuo , Yan Cao , Diya Lv , Langdong Chen , Yinyin Zhang , Jianxin Yang , Hui Shen , Xin Dong , Dongyao Wang
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引用次数: 0
摘要
天然产物黄芩素衍生物黄芩素-8-磺酸(baicalein-8-sulfonic acid, BaSO3H)对肝癌细胞活力和集落形成有明显的抑制作用，但其分子靶点和机制尚不清楚。使用dna编程光亲和标记方法，我们鉴定了12个与BaSO3H特异性结合的靶标。其中，BaSO3H以33.1 nM (Kd)的亲和力与c-Jun n -末端激酶2 (JNK2)结合，诱导肝癌细胞凋亡和自噬。
Target identification of baicalein derivative using DNA-programmed photoaffinity labeling
The natural product baicalein derivative baicalein-8-sulfonic acid (BaSO3H) showed significant inhibitory effects on hepatocarcinoma cells viabilities and colony formation, but its molecular target(s) and mechanism were still not clearly elucidated. Using a DNA-programmed photoaffinity labeling method, we identified 12 targets that specifically bound with BaSO3H. Among these, BaSO3H bound with c-Jun N-terminal kinase 2 (JNK2) at an affinity of 33.1 nM (Kd) to induce apoptosis and autophagy in hepatocarcinoma cells.
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