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On November 30, 2021, the research group of Professor Deng Xianming from the State Key Laboratory of Cellular Stress Biology, the National and Local Joint Engineering Laboratory for Targeted Drugs from Natural Product Sources, and the School of Life Sciences of Xiamen University jointly published a title in "EMBO Molecular Medicine" For the research paper "A new ALK inhibitor overcomes resistance to first- and second-generation inhibitors in NSCLC" ( http://doi.
org/10.
15252/emmm.
202114296), a new generation of ALK inhibitor XMU-MP- 5.
It can effectively overcome the clinical drug resistance mutation of non-small cell lung cancer caused by the first and second generation ALK inhibitors
.
This study provides a new lead compound for the development of a new generation of ALK-targeted drugs, which is expected to bring new hope to patients with clinical resistance to ALK inhibitors
The fusion gene EML4-ALK produced by chromosomal rearrangement is one of the important oncogenes in non-small cell lung cancer
.
Since the FDA approved Crizotinib as the first-generation small molecule inhibitor of EML4-ALK in 2011, the currently used ALK inhibitors have achieved significant clinical efficacy, but with the prolongation of medication time, patients inevitably develop Resistance mutations to existing drugs
The paper was completed by our laboratory, the School of Life Science and Technology of Jinan University, the School of Basic Medicine of Peking University, and the National Center for Translational Medicine of Shanghai Jiaotong University.
Sheng Zhuang Zhongji is responsible for the design, synthesis and optimization of this series of compounds.
Professor Zhang Jianming, Professor Yunhong, Professor Chen Liang and Professor Deng Xianming are the co-corresponding authors
.
The research was funded by the key research and development program of the Ministry of Science and Technology, the National Natural Science Foundation of China, and the basic scientific research business expenses of central universities
【Professor Deng Xianming's team profile】
Professor Deng Xianming's team carried out innovative drug discovery research around "novel kinases" targeting pathways and targets related to major diseases
.
In the past five years, relevant results have been published in Cell , Sci.
Original link: http://doi.
(Photo/Wen Deng Xianming's research group)
