Construction of a Shape-Diverse Fragment Set: Design, Synthesis and Screen against Aurora-A Kinase.

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作者： Rong,Zhang ^[1] ; Patrick J,McIntyre ^[2] ; Patrick M,Collins ^[3] ; Daniel J,Foley ^[4] ; Christopher,Arter ^[1] ; Frank,von Delft ^[2] ; Richard,Bayliss ^[1] ; Stuart,Warriner ^[2] ; Adam,Nelson ^[4]

作者单位： Astbury Centre for Structural Molecular Biology, University of Leeds, Leeds, LS2 9JT, UK. ^[1] School of Chemistry, University of Leeds, Leeds, LS2 9JT, UK. ^[2] Department of Molecular and Cell Biology, Henry Wellcome Building, University of Leicester, Leicester, LE1 9HN, UK. ^[3] Diamond Light Source Ltd., Harwell Science and Innovation Campus, Didcot, OX11 0DE, UK. ^[4] Structural Genomics Consortium, Nuffield Department of Medicine, University of Oxford, Oxford, OX3 7DQ, UK. ^[5] Department of Biochemistry, University of Johannesburg, Aukland Park, 2006, South Africa. ^[6] School of Molecular and Cellular Biology, University of Leeds, Leeds, LS2 9JT, UK. ^[7]

关键词 diversity-oriented synthesis fragments molecular shape

主题词别构调节(Allosteric Regulation);结合部位(Binding Sites);结晶学, X线(Crystallography, X-Ray);药物设计(Drug Design);蛋白质结合(Protein Binding);蛋白激酶抑制剂(Protein Kinase Inhibitors);蛋白质结构, 三级(Protein Structure, Tertiary)

DOI 10.1002/chem.201900815

PMID 31026091

发布时间 2019-05-17

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