Discovery of LLC0424 as a Potent and Selective in Vivo NSD2 PROTAC Degrader

Author:

Liu Lianchao1,Parolia Abhijit2345,Liu Yihan26,Hou Caiyun7,He Tongchen2,Qiao Yuanyuan23,Eyunni Sanjana238,Luo Jie23,Li Chungen1,Wang Yongxing9,Zhou Fengtao7ORCID,Huang Weixue1,Ren Xiaomei1,Wang Zhen1ORCID,Chinnaiyan Arul M.234510,Ding Ke1711ORCID

Affiliation:

1. State Key Laboratory of Chemical Biology, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, no. 345 Lingling Road., Shanghai 200032, People’s Republic of China

2. Michigan Center for Translational Pathology, University of Michigan, Ann Arbor, Michigan 48109, United States

3. Department of Pathology, University of Michigan, Ann Arbor, Michigan 48109, United States

4. Rogel Cancer Center, University of Michigan, Ann Arbor, Michigan 48109, United States

5. Department of Urology, University of Michigan, Ann Arbor, Michigan 48109, United States

6. Cancer Biology Program, University of Michigan, Ann Arbor, Michigan 48109, United States

7. International Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Discovery of Chinese Ministry of Education (MOE), Guangzhou City Key Laboratory of Precision Chemical Drug Development, College of Pharmacy, Jinan University, 855 Xingye Avenue East, Guangzhou 511400, People’s Republic of China

8. Molecular and Cellular Pathology Program, University of Michigan, Ann Arbor, Michigan 48109, United States

9. Livzon Research Institute, Livzon Pharmaceutical Group Inc., no. 38 Chuangye North Road, Jinwan District, Zhuhai 519000, China

10. Howard Hughes Medical Institute, University of Michigan, Ann Arbor, Michigan 48109, United States

11. Hangzhou Institute of Medicine (HlM), Chinese Academy of Sciences, Hangzhou, Zhejiang 310022, China

Funder

Howard Hughes Medical Institute

National Cancer Institute

Shenzhen Bay Laboratory

Shanghai Key Laboratory of Chemical Biology

American Cancer Society

Science and Technology Commission of Shanghai Municipality

National Natural Science Foundation of China

A. Alfred Taubman Medical Research Institute

Livzon Pharmaceutical Group Inc

Publisher

American Chemical Society (ACS)

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