用于细胞周期蛋白依赖性激酶5（CDK5）的新型铽敏化肽底物及其在发光激酶测定中的应用
Novel terbium-sensitizing peptide substrates for cyclin-dependent kinase 5 (CDK5) and their demonstration in luminescence kinase assays.
作者信息
Heier Jason L, Boselli Dylan J, Parker Laurie L
机构信息
Department of Biochemistry, Molecular Biology and Biophysics, University of Minnesota Minneapolis 55455 USA
出版信息
RSC Chem Biol. 2025 Sep 11. doi: 10.1039/d5cb00189g.
Abstract
Novel time-resolved terbium luminescence assays were developed for CDK5 and CDK2 by designing synthetic substrates which incorporate phospho-inducible terbium sensitizing motifs with kinase substrate consensus sequences. A substrate designed for CDK5 showed no phosphorylation by CDK2, opening the possibility for CDK5-specific assay development for selective drug discovery.
摘要
通过设计合成底物开发了用于CDK5和CDK2的新型时间分辨铽发光测定法，这些底物将磷酸诱导的铽敏化基序与激酶底物共有序列结合在一起。为CDK5设计的一种底物未显示出被CDK2磷酸化，这为开发用于选择性药物发现的CDK5特异性测定法提供了可能性。
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