Discovery of a Highly Potent and Selective Dual PROTAC Degrader of CDK12 and CDK13

Author:

Yang Jianzhang1,Chang Yu12,Tien Jean Ching-Yi23,Wang Zhen4ORCID,Zhou Yang1ORCID,Zhang Pujuan4,Huang Weixue4,Vo Josh2,Apel Ingrid J.2ORCID,Wang Cynthia2,Zeng Victoria Zhixuan2,Cheng Yunhui2,Li Shuqin2,Wang George Xiaoju235,Chinnaiyan Arul M.23567,Ding Ke1489ORCID

Affiliation:

1. 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

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. State Key Laboratory of Bioorganic and Natural Products Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, #345 Ling Ling Road, Shanghai 200032, People’s Republic of China

5. Department of Computational Medicine and Bioinformatics, University of Michigan, Ann Arbor, Michigan 48109, United States

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

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

8. Institute of Basic Medicine and Cancer (IBMC), Chinese Academy of Sciences, Hangzhou, Zhejiang 310022, People’s Republic of China

9. The First Affiliated Hospital (Huaqiao Hospital), Jinan University, 601 Huangpu Avenue West, Guangzhou 510632, China

Funder

National Cancer Institute

Government of Guangdong Province

National Natural Science Foundation of China

National Institutes of Health

Prostate Cancer Foundation

LIVZON pharm

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

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