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Structure-Based Engineering of Irreversible Inhibitors against Histone Lysine Demethylase KDM5A.

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第一作者： John R,Horton

第一单位： Department of Molecular and Cellular Oncology , The University of Texas MD Anderson Cancer Center , Houston , Texas 77030 , United States.;Department of Biochemistry , Emory University School of Medicine , Atlanta , Georgia 30322 , United States.

作者： John R,Horton ^[1] ; Clayton B,Woodcock ^[2] ; Qin,Chen ^[2] ; Xu,Liu ^[3] ; Xing,Zhang ^[2] ; John,Shanks ^[3] ; Ganesha,Rai ^[4] ; Bryan T,Mott ^[4] ; Daniel J,Jansen ^[4] ; Stephen C,Kales ^[4] ; Mark J,Henderson ^[4] ; Matthew,Cyr ^[4] ; Katherine,Pohida ^[4] ; Xin,Hu ^[4] ; Pranav,Shah ^[4] ; Xin,Xu ^[4] ; Ajit,Jadhav ^[4] ; David J,Maloney ^[4] ; Matthew D,Hall ^[4] ; Anton,Simeonov ^[4] ; Haian,Fu ^[1] ; Paula M,Vertino ; Xiaodong,Cheng

作者单位： Department of Molecular and Cellular Oncology , The University of Texas MD Anderson Cancer Center , Houston , Texas 77030 , United States.;Department of Biochemistry , Emory University School of Medicine , Atlanta , Georgia 30322 , United States. ^[1] Department of Molecular and Cellular Oncology , The University of Texas MD Anderson Cancer Center , Houston , Texas 77030 , United States. ^[2] Department of Biochemistry , Emory University School of Medicine , Atlanta , Georgia 30322 , United States. ^[3] National Center for Advancing Translational Sciences , National Institutes of Health , 9800 Medical Center Drive , Rockville , Maryland 20850 , United States. ^[4]

医学主题词丙烯酰胺(Acrylamide);细胞系(Cell Line);药物设计(Drug Design);酶抑制剂(Enzyme Inhibitors);人类(Humans);模型, 分子(Models, Molecular);蛋白质构象(Protein Conformation);视网膜母细胞瘤结合蛋白2(Retinoblastoma-Binding Protein 2)

DOI 10.1021/acs.jmedchem.8b01219

PMID 30392349

发布时间 2025-05-29

基金项目

P30 CA016672/CA/NCI NIH HHS/United States R01 GM114306/GM/NIGMS NIH HHS/United States S10 OD012304/OD/NIH HHS/United States HHSN261200800001C/RC/CCR NIH HHS/United States HHSN261200800001E/CA/NCI NIH HHS/United States

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