Design, synthesis, and biological evaluation of potent photoaffinity probes of oleanolic acid.
Design, synthesis, and biological evaluation of potent photoaffinity probes of oleanolic acid.
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DOI：
10.2174/1573406411309020012
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发表时间：
2013-02
期刊：
影响因子：
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通讯作者：
Li-ying Zhang;Jizhe Dong;Yingxia Zhang;Jun O. Liu;Luyong Zhang;Hongbin Sun
中科院分区：
文献类型：
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作者：
Li-ying Zhang;Jizhe Dong;Yingxia Zhang;Jun O. Liu;Luyong Zhang;Hongbin Sun
为了研究齐墩果酸的靶蛋白，设计并合成了一系列新型光亲和探针。对糖原磷酸化酶（齐墩果酸的已知靶蛋白）的酶抑制试验评估了它们对靶蛋白的亲和力。其中探针2的活性最强，IC50值为5.98 μM，是其母体齐墩果酸的2.5倍左右。结果表明，合成的光亲和探针对靶蛋白保持了良好的结合亲和性，可作为捕获齐墩果酸靶蛋白的有力工具。
To study the target proteins of oleanolic acid, a series of novel photoaffinity probes were designed and synthesized. Their affinity for the target proteins was evaluated in an enzyme inhibition assay against glycogen phosphorylase, a known target protein of oleanolic acid. Among these compounds, probe 2 exhibited the most potent activity with an IC50 value of 5.98 μM, which was about 2.5-fold more potent than its parent compound oleanolic acid. The results showed that the synthesized photoaffinity probes retained the binding affinity for their target proteins, and might be used as powerful tools to fish out the target proteins of oleanolic acid.