Yuxiao Tang , Xiaobin Zhuo , Yan Cao , Diya Lv , Langdong Chen , Yinyin Zhang , Jianxin Yang , Hui Shen , Xin Dong , Dongyao Wang
{"title":"Target identification of baicalein derivative using DNA-programmed photoaffinity labeling","authors":"Yuxiao Tang , Xiaobin Zhuo , Yan Cao , Diya Lv , Langdong Chen , Yinyin Zhang , Jianxin Yang , Hui Shen , Xin Dong , Dongyao Wang","doi":"10.1016/j.crchbi.2021.100014","DOIUrl":null,"url":null,"abstract":"<div><p>The natural product baicalein derivative baicalein-8-sulfonic acid (BaSO<sub>3</sub>H) 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 BaSO<sub>3</sub>H. Among these, BaSO<sub>3</sub>H bound with c-Jun N-terminal kinase 2 (JNK2) at an affinity of 33.1 nM (K<sub>d</sub>) to induce apoptosis and autophagy in hepatocarcinoma cells.</p></div>","PeriodicalId":72747,"journal":{"name":"Current research in chemical biology","volume":"2 ","pages":"Article 100014"},"PeriodicalIF":0.0000,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2666246921000148/pdfft?md5=4996c9ae5a35f9273d5c3400c69c3b7b&pid=1-s2.0-S2666246921000148-main.pdf","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Current research in chemical biology","FirstCategoryId":"1085","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S2666246921000148","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 0
Abstract
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.