Article
JND4135, a New Type II TRK Inhibitor, Overcomes TRK xDFG and Other Mutation Resistance In Vitro and In Vivo.
Molecules (Basel, Switzerland) - 1 Oct 2022
Wang Jie, Zhou Yang, Tang Xia, Yu Xiuwen, Wang Yongjin, Chan Shingpan, Song Xiaojuan, Tu Zhengchao, Zhang Zhimin, Lu Xiaoyun, Zhang Zhang, Ding Ke
Abstract excerpt
The tropomyosin receptor kinases (TRKs) have been validated as effective targets in anticancer drug discovery. Two first-generation TRK inhibitors have been approved into market and displayed an encouraging therapeutic response in cancer patients harboring TRK fusion proteins. However, acquired resistance mediated by secondary TRK mutations especially in the xDFG motif remains an unsolved challenge in the clinic....
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