Structure-Guided Development of Small-Molecule PRC2 Inhibitors Targeting EZH2–EED Interaction

Author:

Du Daohai12,Xu Dandan34,Zhu Licheng567,Stazi Giulia8,Zwergel Clemens8ORCID,Liu Yanli569,Luo Zhongyuan12,Li Yuanqing24,Zhang Yuanyuan2ORCID,Zhu Kongkai10,Ding Yiluan11,Liu Jingqiu2,Fan Shijie2,Zhao Kaiyan34,Zhang Naixia11ORCID,Kong Xiangqian12,Jiang Hualiang2,Chen Kaixian2,Zhao Kehao13,Valente Sergio8ORCID,Min Jinrong56,Duan Wenhu34ORCID,Luo Cheng1241314ORCID

Affiliation:

1. School of Chinese Materia Medica, Nanjing University of Chinese Medicine, Nanjing 210023 Jiangsu, China

2. Drug Discovery and Design Center, the Center for Chemical Biology, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 210203, China

3. Department of Medicinal Chemistry, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China

4. University of Chinese Academy of Sciences, Beijing 100049, China

5. Structural Genomics Consortium and Department of Physiology, University of Toronto, Toronto M5G1L7 Ontario, Canada

6. Hubei Key Laboratory of Genetic Regulation and Integrative Biology, School of Life Sciences, Central China Normal University, Wuhan 430079, China

7. School of Life Sciences, Jinggangshan University, Ji’an 343009 Jiangxi, China

8. Department of Drug Chemistry and Technologies, Sapienza University of Rome, Rome 00185, Italy

9. College of Pharmaceutical Sciences, Soochow University, Suzhou 215123 Jiangsu, China

10. School of Biological Science and Technology, University of Jinan; Jinan 250022, China

11. Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China

12. Guangdong Provincial Key Laboratory of Biocomputing, Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences, Guangzhou 510530, China

13. School of Pharmacy, Key Laboratory of Molecular Pharmacology and Drug Evaluation (Yantai University), Ministry of Education; Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in Universities of Shandong, Yantai University, Yantai 264005, China

14. School of Pharmaceutical Science and Technology, Hangzhou Institute for Advanced Study, University of Chinese Academy of Sciences, Hangzhou 310024, China

Funder

Ministry of Science and Technology of the People's Republic of China

K. C. Wong Education Foundation

Science and Technology Commission of Shanghai Municipality

National Natural Science Foundation of China

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

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