1.Discovery of WS-157 as a highly potent, selective and orally active EGFR inhibitor.
Pengxing HE ; Shenghui NIU ; Shuai WANG ; Xiaojing SHI ; Siqi FENG ; Linna DU ; Xuyang ZHANG ; Zhilu MA ; Bin YU ; Hongmin LIU
Acta Pharmaceutica Sinica B 2019;9(6):1193-1203
EGFR tyrosine kinase inhibitor (EGFR-TKI) has been used successfully in clinic for the treatment of solid tumors. In the present study, we reported the discovery of from our in-house diverse compound library, which was validated to be a potent and selective EGFR-TKI. showed excellent inhibitory activities against EGFR (IC = 0.81 nmol/L), EGFR (IC = 1.2 nmol/L) and EGFR (IC = 1.1 nmol/L), but was less effective or even inactive against other nine kinases. also displayed excellent antiproliferative activities against a panel of human cancer cell lines, and exhibited the ability to reduce colony formation and wound healing the same as gefitinib. We found that upon oral administration showed better anti-tumor activity in A431 bearing xenograft mouse models compared to gefitinib. In addition, showed better intestinal absorption than gefitinib and had favorable pharmacokinetic properties and microsomal metabolic stability in different species. These studies indicate that has strong antitumor activity and , and could be used for the development of anti-lung cancer agent targeting EGFR.
2.Expert consensus on microbiome sequencing and analysis.
Yunfeng DUAN ; Shengyue WANG ; Yubao CHEN ; Ruifu YANG ; Houkai LI ; Huaiqiu ZHU ; Yigang TONG ; Wenbin WU ; Yu FU ; Songnian HU ; Jun WANG ; Yuhua XIN ; Fangqing ZHAO ; Yiming BAO ; Wen ZHANG ; Juan LI ; Ming ZENG ; Haitao NIU ; Xin ZHOU ; Yan LI ; Shenghui CUI ; Jing YUAN ; Junhua LI ; Jiayi WANG ; Donglai LIU ; Ming NI ; Qing SUN ; Ye DENG ; Baoli ZHU
Chinese Journal of Biotechnology 2020;36(12):2516-2524
In the past ten years, the research and application of microbiome has continued to increase. The microbiome has gradually become the research focus in the fields of life science, environmental science, and medicine. Meanwhile, many countries and organizations around the world are launching their own microbiome projects and conducting a multi-faceted layout, striving to gain a strategic position in this promising field. In addition, whether it is scientific research or industrial applications, there has been a climax of research and a wave of investment and financing, accordingly, products and services related to the microbiome are constantly emerging. However, due to the rapid development of microbiome sequencing and analysis related technologies and methods, the research and application from various countries have not yet unified on the standards of technology, programs, and data. Domestic industry participants also have insufficient understanding of the microbiome. New methods, technologies, and theories have not yet been fully accepted and used. In addition, some of the existing standards and guidelines are too general with poor practicality. This not only causes obstacles in the integration of scientific research data and waste of resources, but also gives related companies unfair competition opportunity. More importantly, China still lacks national standards related to the microbiome, and the national microbiome project is still in the process of preparation. In this context, the experts and practitioners of the microbiome worked together and developed the consensus of experts. It can not only guide domestic scientific research and industrial institutions to regulate the production, learning and research of the microbiome, the application can also provide reference technical basis for the relevant national functional departments, protect the scale and standardized corporate company's interests, strengthen industry self-discipline, avoid unregulated enterprises from disrupting the market, and ultimately promote the benign development of microbiome-related industries.
China
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Consensus
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Humans
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Industry
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Microbiota