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Discovery of N-Benzylpiperidinol derivatives as USP7 inhibitors against Hematology

文献类型：期刊论文

作者Pan, Youlu4; Chen, Haifeng3; Fu, Jingfeng2; Zhang, Jingyu1,3; Wang, Peipei2; Chen, Runmei4; Geng, Shuangshuang3; Che, Jinxin3; Dong, Xiaowu3; Zhou, Yubo2
刊名BIOORGANIC CHEMISTRY
出版日期2024-12-01
卷号153页码:13
ISSN号0045-2068
DOI10.1016/j.bioorg.2024.107807
通讯作者Zhou, Yubo(ybzhou@simm.ac.cn) ; Huang, Wenhai(hwh@hmc.edu.cn)
英文摘要USP7 has been recognized as a potential target for the treatment of hematologic malignancies by stabilizing multiple cancer-relevant proteins. Nevertheless, drug-like USP7 inhibitors are still lacking. Herein, compound J21 (USP7 IC50: 41.35 +/- 2.16 nM) was discovered based on the structure of L55 and its co-crystal complex with USP7. Additionally, J21 exhibited greater metabolic stability (T-1/2: 1.25 h, C-max: 394.1 +/- 48.3 ng/mL, and AUC(0-t): 597.8 +/- 44.8 ng/mL center dot h) compared to L55. These findings may further pave the way for the
WOS关键词MUTANT P53 ; HAUSP ; BORTEZOMIB
资助项目National Natural Science Foundation of China[82304270] ; National Natural Science Foundation of China[82373705] ; National Natural Science Foundation of China[82173660] ; Zhejiang Provincial Key Research & Development Plan[2023C03111] ; Guangdong High-level new 1350 R D Institute[2023000003] ; Guangdong High-level new 1350 R D Institute[2019B090904008] ; Guangdong 1351 High-level Innovative Research Institute[2021B0909050003]
WOS研究方向Biochemistry & Molecular Biology ; Chemistry
语种英语
WOS记录号WOS:001318038000001
出版者ACADEMIC PRESS INC ELSEVIER SCIENCE
源URL[http://119.78.100.183/handle/2S10ELR8/313460]  
专题中国科学院上海药物研究所
通讯作者Zhou, Yubo; Huang, Wenhai
作者单位1.Zhejiang Univ, Hangzhou Peoples Hosp 1, Canc Ctr, Key Lab Clin Canc Pharmacol & Toxicol Res Zhejiang, Hangzhou 310006, Peoples R China
2.Chinese Acad Sci, Zhongshan Inst Drug Discovery, Shanghai Inst Mat Med, Zhongshan 528400, Guangdong, Peoples R China
3.Zhejiang Univ, Hangzhou Inst Innovat Med, Inst Drug Discovery & Design, Coll Pharmaceut Sci, Hangzhou 310058, Peoples R China
4.Hangzhou Med Coll, Key Lab Neuropsychiat Drug Res Zhejiang Prov, Hangzhou 310058, Peoples R China
推荐引用方式
GB/T 7714		 Pan, Youlu,Chen, Haifeng,Fu, Jingfeng,et al. Discovery of N-Benzylpiperidinol derivatives as USP7 inhibitors against Hematology[J]. BIOORGANIC CHEMISTRY,2024,153:13.
APA Pan, Youlu.,Chen, Haifeng.,Fu, Jingfeng.,Zhang, Jingyu.,Wang, Peipei.,...&Huang, Wenhai.(2024).Discovery of N-Benzylpiperidinol derivatives as USP7 inhibitors against Hematology.BIOORGANIC CHEMISTRY,153,13.
MLA Pan, Youlu,et al."Discovery of N-Benzylpiperidinol derivatives as USP7 inhibitors against Hematology".BIOORGANIC CHEMISTRY 153(2024):13.

入库方式： OAI收割

来源：上海药物研究所

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