Cheng-Yao Chiang, Min Zhang, Junrong Huang, Juan Zeng, Chunlan Chen, Dongmei Pan, Heng Yang, Tiantian Zhang, Min Yang, Qiangqiang Han, Zou Wang, Tian Xiao, Yangchao Chen, Yongdong Zou, Feng Yin, Zigang Li, Lizhi Zhu, Duo Zheng
Extracellular regulated protein kinases 1/2 (ERK1/2) are key members of multiple signaling pathways, including the ErbB axis. Ectopic ERK1/2 activation contributes to various types of cancer, especially drug resistance to inhibitors of RTK, RAF and MEK, and specific ERK1/2 inhibitors are scarce. In this study, we identified a potential novel covalent ERK inhibitor, Laxiflorin B, which is a herbal compound with anticancer activity. However, Laxiflorin B is present at low levels in herbs; therefore, we adopted a semi-synthetic process for the efficient production of Laxiflorin B to improve the yield...
October 10, 2023: Acta Pharmacologica Sinica