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Discovery of ATP competitive PDHK1/2 dual inhibitors.

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第一作者： Hongtao,Xu

第一单位： China Innovation Center of Roche, No. 371 Lishizhen Road, Shanghai, 201203, China.

作者： Hongtao,Xu ^[1] ; Dong,Ding ^[1] ; Xingchun,Han ^[1] ; Kun,Miao ^[1] ; Chungen,Liang ^[1] ; Hongying,Yun ^[1] ; Wei,Zhu ^[1] ; Fabian,Dey ^[2] ; Dan,Zhao ^[1] ; Yao,Wu ^[1] ; Michael,Reutlinger ^[2] ; June,Yang ^[1] ; Guanglei,Zhai ^[1] ; Zhaohu,Lin ^[1] ; Chiho,Li ^[1] ; Waikong,Wu ^[1] ; Bruce,Xu ^[1] ; Li,Han ^[1] ; Shuai,Chen ^[1] ; Xinyi,Huang ^[1] ; Fabio,Casagrande ^[2] ; Manuel,Hilbert ^[2] ; Quentin,Strebel ^[2] ; Moreno,Wichert ^[2] ; Paul,Westwood ^[2] ; Ramona,Schäfer ^[2] ; Doris,Roth ^[2] ; Dominik,Heer ^[2] ; Xiaojun,Tian ^[1] ; Tiantian,Ma ^[1] ; Tong,Zhang ^[1] ; Jie,Zhao ^[1] ; Eduard,Urich ^[1] ; Guliang,Xia ^[1] ; Kara,Lassen ^[2] ; Hong C,Shen ^[1] ; Ge,Zou ^[3]

作者单位： China Innovation Center of Roche, No. 371 Lishizhen Road, Shanghai, 201203, China. ^[1] Pharmaceutical Research and Early Development, F. Hoffmann-La Roche AG, Roche Innovation Center Basel, Grenzacherstrasse 124, 4070 Basel, Switzerland. ^[2] China Innovation Center of Roche, No. 371 Lishizhen Road, Shanghai, 201203, China. Electronic address: ge.zou@roche.com. ^[3]

关键词 Covalent inhibitor Kinase inhibitors for immunometabolism Structure based design

医学主题词人类(Humans);腺苷三磷酸(Adenosine Triphosphate);剂量效应关系, 药物(Dose-Response Relationship, Drug);药物发现(Drug Discovery);分子结构(Molecular Structure);蛋白激酶抑制剂(Protein Kinase Inhibitors);构效关系(Structure-Activity Relationship)

DOI 10.1016/j.bmcl.2025.130190

PMID 40107630

发布时间 2025-09-09

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