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当前位置: 北京大学化学与分子工程学院正文
标 题:Uncovered the novel mode of action for Ainsliadimer A
发布时间:2015-04-14 阅读次数:1985

The latest research breakthrough from Prof. Lei’s laboratory on the chemical biology studies of complex natural product has been recently published on Nature Communications.

Dong, T.; Li, C.; Wang, X.; Dian, L.; Zhang, X.; Chen, X.; Li, L.; Cao, R.; Huang, N.; He, S.*; Lei, X.* “Ainsliadimer A selectively inhibits IKKα/β by covalently binding a conserved cysteineNature Commun. 2015, 6, 6522

Original Link: http://www.nature.com/ncomms/2015/150327/ncomms7522/full/ncomms7522.html

Aberrant activation of NF-kB is associated with the development of cancer and autoimmune and inflammatory diseases. IKKs are well recognized as key regulators in the NF-kB pathway and therefore represent attractive targets for intervention with small molecule inhibitors. Herein, we report that a complex natural product ainsliadimer A is a potent inhibitor of the NF-kB pathway. Ainsliadimer A selectively binds to the conserved cysteine 46 residue of IKKa/b and suppresses their activities through an allosteric effect, leading to the inhibition of both canonical and non-canonical NF-kB pathways. Remarkably, ainsliadimer A induces cell death of various cancer cells and represses in vivo tumour growth and endotoxin-mediated inflammatory responses. Ainsliadimer A is thus a natural product targeting the cysteine 46 of IKKa/b to block NF-kB signaling. Therefore, it has great potential for use in the development of anticancer and anti-inflammatory therapies.

 

This discovery has also been highlighted by a news story on C&E News.

“Chemists Explore Ways To Manipulate The Immune System”

http://cen.acs.org/articles/93/i15/Chemists-Explore-Ways-Manipulate-Immune.html


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