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Discovery of Potent and Exquisitely Selective Inhibitors of Kinase CK1 with Tunable Isoform Selectivity.

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第一作者： Václav,Němec

第一单位： Department of Chemistry, Faculty of Science, Masaryk University, Kamenice 5, Brno, 625 00, Czech Republic.;International Clinical Research Centre, St. Anne's University Hospital, Pekařská 53, Brno, 656 91, Czech Republic.

作者： Václav,Němec ^[1] ; Prashant,Khirsariya ^[1] ; Pavlína,Janovská ^[2] ; Paula Martín,Moyano ^[3] ; Lukáš,Maier ^[1] ; Petra,Procházková ^[2] ; Pavlína,Kebková ^[2] ; Tomáš,Gybel' ^[2] ; Benedict-Tilman,Berger ^[4] ; Apirat,Chaikuad ^[4] ; Maria,Reinecke ^[5] ; Bernhard,Kuster ^[6] ; Stefan,Knapp ^[4] ; Vítězslav,Bryja ^[2] ; Kamil,Paruch ^[1]

作者单位： Department of Chemistry, Faculty of Science, Masaryk University, Kamenice 5, Brno, 625 00, Czech Republic.;International Clinical Research Centre, St. Anne's University Hospital, Pekařská 53, Brno, 656 91, Czech Republic. ^[1] Department of Experimental Biology, Faculty of Science, Masaryk University, Kamenice 5, Brno, 625 00, Czech Republic. ^[2] Department of Chemistry, Faculty of Science, Masaryk University, Kamenice 5, Brno, 625 00, Czech Republic. ^[3] Institute for Pharmaceutical Chemistry, Structural Genomics Consortium, Johann Wolfgang Goethe-University, Max-von-Laue-Strasse 15, 60438, Frankfurt am Main, Germany. ^[4] Chair of Proteomics and Bioanalytics, TUM School of Life Sciences, Technical University of Munich, 85354, Freising, Germany. ^[5] Chair of Proteomics and Bioanalytics, TUM School of Life Sciences, Technical University of Munich, 85354, Freising, Germany.;Bavarian Center for Biomolecular Mass Spectrometry (BayBioMS), Technical University of Munich, 85354, Freising, Germany. ^[6]

关键词 CK1 Chemical Probe Inhibitor Isoform Selectivity Wnt Pathway

医学主题词酪蛋白激酶Ⅰ(Casein Kinase I);蛋白质亚型(Protein Isoforms);蛋白激酶抑制剂(Protein Kinase Inhibitors);信号传导(Signal Transduction);人类(Humans)

DOI 10.1002/anie.202217532

PMID 36625768

发布时间 2023-03-02

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