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Progress on Chemical Biology study of antitumor natural products
source:     author:LIU Jianmei     2014-11-07

  Eriocalyxin B, an ent-kaurene diterpenoid, possesses potent bioactivity of antitumor and anti-autoimmune. Related studies have been devoted to elucidating the underlying mechanisms of the bioactivities of EriB, among which the NF-κB signaling is largely involved. Though extensive investigations of the mechanism involved in the inhibition of NF-κB signaling by EriB have been reported, the direct targets of EriB remain unknown. 

  With close cooperation of LI Yan’s group, ZHAO Qinshi’s group and SUN Handong’s group, the direct target of Eriocalyxin B was investigated with activity-based probe profiling technology. p50 protein was identified as the direct target of EriB and the structural basis for the interaction was illustrated for the first time. The results highlight that p50 may be a very promising drug target for cancer therapy and EriB can be used as a natural chemical template for the development of therapeutic agents. These findings were recently published online on Oncotarget, entitled by “Identification and Validation of p50 as the Cellular Target of Eriocalyxin B”. This work was funded by the Ministry of Science and Technology, the National Natural Science Foundation of China, the Chinese Academy of Sciences and Yunnan Province.  

  http://www.impactjournals.com/oncotarget/index.php?journal=oncotarget&page=article&op=view&path%5B%5D=2461&path%5B%5D=4498 

Figure 1. Bioactive labeled probes of eriocalyxin B

Figure 2. Structural basis of the interaction between eriocalyxin B and p50 

(Image by KIB)


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