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Novel hybrid molecule overcomes the limited response of solid tumours to HDAC inhibitors via suppressing JAK1-STAT3-BCL2 signalling

作者:Zhi Huang, Wei Zhou, Yongtao Li, Mei Cao, Tianqi Wang, Yakun Ma, Qingxiang Guo, Xin Wang, Chao Zhang, Chenglan Zhang, Wenzhi Shen, Yanhua Liu, Yanan Chen, Jian‐Yu Zheng, Shengyong Yang, Yan Fan, Rong Xiang · 发表于:Theranostics · 年份:2018 · DOI:10.7150/thno.26627 · 被引用次数:67 · 研究领域:Histone Deacetylase Inhibitors Research、Protein Degradation and Inhibitors、Click Chemistry and Applications

Concurrent inhibition of HDAC and CDK using Roxyl-zhc-84 with additional JAK1 targeting resolved the limited response of traditional HDAC inhibitors in solid tumours via overcoming JAK1-STAT3-BCL2-mediated drug resistance, providing a rational multi-target treatment to sensitize solid tumours to HDACi therapy.