结构变化对磷酸氨基酸位置处肽的 Polo 样激酶 1 Polo 盒结构域结合亲和力的影响。
Effects on polo-like kinase 1 polo-box domain binding affinities of peptides incurred by structural variation at the phosphoamino acid position.
机构信息
Chemical Biology Laboratory, Frederick National Laboratory for Cancer Research, National Cancer Institute, National Institutes of Health, Frederick, MD 21702, USA.
出版信息
Bioorg Med Chem. 2013 Jul 15;21(14):3996-4003. doi: 10.1016/j.bmc.2012.05.036. Epub 2012 May 26.
Abstract
Protein-protein interactions (PPIs) mediated by the polo-box domain (PBD) of polo-like kinase 1 (Plk1) serve important roles in cell proliferation. Critical elements in the high affinity recognition of peptides and proteins by PBD are derived from pThr/pSer-residues in the binding ligands. However, there has been little examination of pThr/pSer mimetics within a PBD context. Our current paper compares the abilities of a variety of amino acid residues and derivatives to serve as pThr/pSer replacements by exploring the role of methyl functionality at the pThr β-position and by replacing the phosphoryl group by phosphonic acid, sulfonic acid and carboxylic acids. This work sheds new light on structure activity relationships for PBD recognition of phosphoamino acid mimetics.
摘要
由 polo 样激酶 1 (Plk1) 的 polo 框域 (PBD) 介导的蛋白质-蛋白质相互作用 (PPIs) 在细胞增殖中起着重要作用。PBD 对肽和蛋白质的高亲和力识别的关键元件来自于结合配体中的 pThr/pSer 残基。然而，在 PBD 背景下对 pThr/pSer 类似物的研究甚少。我们目前的论文通过探索 pThr β 位甲基化功能以及用膦酸、磺酸和羧酸取代磷酸基团，比较了各种氨基酸残基和衍生物作为 pThr/pSer 替代物的能力，从而探讨了 pThr/pSer 类似物在 PBD 识别中的作用。这项工作为 PBD 识别磷酸氨基酸类似物的结构活性关系提供了新的线索。
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