Discovery of potent PROTAC degraders of Pin1 for the treatment of acute myeloid leukemia

Author:

Shi Yunkai12ORCID,Liu Minmin34,Li Mengna5,Mao Yiwen12,Ma Jingkun326,Long Ruikai12,Xu Miaomiao32,Yang Yaxi1327,Wang Wenlong4,Zhou Yubo13265,Li Jia13267,Zhou Bing13275ORCID

Affiliation:

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

2. University of Chinese Academy of Sciences, 19 Yuquan Road, Beijing, 100049, China

3. State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Shanghai, 201203, China

4. School of Pharmaceutical Science, Jiangnan University, Wuxi, 214122, China

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

6. Zhongshan Institute for Drug Discovery, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Zhongshan Tsuihang New District, Guangdong, 528400, China

7. Shandong Laboratory of Yantai Drug Discovery, Bohai Rim Advanced Research Institute for Drug Discovery, Yantai, Shandong, 264117, China

Abstract

The first PROTAC degrader of Pin1 was developed and exhibited potent degradation-dependent anti-proliferative activities in acute myeloid leukemia cells.

Funder

Natural Science Foundation of Shanghai Municipality

Natural Science Foundation of Shandong Province

National Natural Science Foundation of China

Taishan Scholar Foundation of Shandong Province

Science and Technology Commission of Shanghai Municipality

Publisher

Royal Society of Chemistry (RSC)

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