〓probe and its efficiency in affinity labeling of a target protein for jasmonate
〓probe and its efficiency in affinity labeling of a target protein for jasmonate
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〓探针及其亲和标记茉莉酸靶蛋白的效率
DOI：
10.1016/j.bmcl.2012.10.124
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发表时间：
2013
影响因子：
2.7
通讯作者：
Ueda M
中科院分区：
文献类型：
--
作者：
Tamura S;Inomata S;Ebine M;Genji T;Iwakura I;Mukai M;Shoji M;Sugai T;Ueda M
在利用分子探针探索生物活性小分子的靶点的方法中，长的或刚性的接头部分被认为是有效标记靶蛋白的关键因素。我们以前报道的茉莉酸酯葡萄糖苷探针的合成与一个高度刚性的接头组成的三唑基-苯基（TAzP）部分，这种探针表现出有效的目标标签。在这里，我们比较了TAzP探针与其他刚性或柔性探针的目标标记效率，疏水参数，水溶性，二面角周围的联芳基连接的经验和计算方法相结合。TAzP探针的刚性联芳基连接具有影响其水溶性的偏斜构象。包括刚性和良好的水溶性的这些特征导致高效的靶标记。这些发现为设计更好的接头以改善分子探针性能提供了有希望的指导。
In methods employing molecular probes to explore the targets of bioactive small molecules, long or rigid linker moieties are thought to be critical factors for efficient tagging of target protein. We previously reported the synthesis of a jasmonate glucoside probe with a highly rigid linker consisting of a triazoyl–phenyl (TAzP) moiety, and this probe demonstrated effective target tagging. Here we compare the TAzP probe with other rigid or flexible probes with respect to target tagging efficiency, hydrophobic parameters, aqueous solubility, and dihedral angles around the biaryl linkage by a combination of empirical and calculation methods. The rigid biaryl linkage of the TAzP probe has a skewed conformation that influences its aqueous solubility. Such features that include rigidness and good aqueous solubility resulted in highly efficient target tagging. These findings provide a promising guideline toward designing of better linkers for improving molecular probe performance.