Discovery of a Potent, selective and orally bioavailable CDK9 degrader for targeting transcription regulation in Triple-Negative breast cancer.

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第一作者： Hui-Jun,Nie

第一单位： School of Pharmaceutical Science and Technology, Hangzhou Institute for Advanced Study, University of Chinese Academy of Sciences, Hangzhou, China; State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.

作者： Hui-Jun,Nie ^[1] ; Ben-Fu,Li ^[2] ; Jingya,Sun ^[3] ; Yali,Yuan ^[4] ; Zhi-Gao,Zhang ^[5] ; Hao,Hu ^[6] ; Wen-Jing,Wang ^[5] ; Ziqiang,Chen ^[7] ; Simei,Wang ^[7] ; Wensi,Huang ^[4] ; Xingxing,Diao ^[4] ; Jinghua,Yu ^[8] ; Ruimin,Huang ^[9] ; Xiao-Hua,Chen ^[10]

作者单位： School of Pharmaceutical Science and Technology, Hangzhou Institute for Advanced Study, University of Chinese Academy of Sciences, Hangzhou, China; State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China. ^[1] State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China; University of Chinese Academy of Sciences, Beijing 100049, China. ^[2] Center for Drug Safety Evaluation and Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China. ^[3] Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China. ^[4] School of Pharmaceutical Science and Technology, Hangzhou Institute for Advanced Study, University of Chinese Academy of Sciences, Hangzhou, China; University of Chinese Academy of Sciences, Beijing 100049, China. ^[5] State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China. ^[6] Center for Drug Safety Evaluation and Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China; University of Chinese Academy of Sciences, Beijing 100049, China. ^[7] Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China. Electronic address: yujinghua2@simm.ac.cn. ^[8] Center for Drug Safety Evaluation and Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China; University of Chinese Academy of Sciences, Beijing 100049, China. Electronic address: rmhuang@simm.ac.cn. ^[9] School of Pharmaceutical Science and Technology, Hangzhou Institute for Advanced Study, University of Chinese Academy of Sciences, Hangzhou, China; State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China; University of Chinese Academy of Sciences, Beijing 100049, China. Electronic address: xhchen@simm.ac.cn. ^[10]

关键词 Cyclin-dependent Kinase 9 Orally bioavailable degrader PROTAC Targeting transcription regulation Triple-negative breast cancer