Design and synthesis of novel photoaffinity probes for study of the target proteins of oleanolic acid.
Design and synthesis of novel photoaffinity probes for study of the target proteins of oleanolic acid.
复制标题
设计和合成新型光亲和探针，用于研究齐墩果酸的靶蛋白。
DOI：
10.1016/j.bmcl.2011.11.123
复制
发表时间：
2012
影响因子：
2.7
通讯作者：
Hongbin Sun
中科院分区：
文献类型：
--
作者：
Li;Yingxia Zhang;Jizhe Dong;Jun O. Liu;Luyong Zhang;Hongbin Sun
为了探索油酸的分子作用机制，在已有构效关系的基础上，合成了两种新型的光亲和探针。在针对兔肌糖原磷酸化酶a（RMGPa）（油酸的已知靶蛋白）的酶抑制测定中评价它们的效力。探针2的抑制活性仅比母体化合物油酸的抑制活性低约两倍。还进行了光亲和标记实验，并通过探针2特异性标记了两种蛋白质。结果表明，所合成的探针可作为分离和鉴定油酸靶蛋白的有力工具。
To explore the molecular mechanisms of oleanolic acid, two novel photoaffinity probes were synthesized based on the structure–activity relationship reported previously. Their potency were evaluated in an enzyme inhibition assay against rabbit muscle glycogen phosphorylase a (RMGPa), a known target protein of oleanolic acid. The inhibitory activity of probe 2 was only about two-fold less potent than the mother compound oleanolic acid. The photoaffinity labeling experiments were also performed and two proteins were specifically tagged by probe 2. The results suggest that the synthesized probes could be used as powerful tools to isolate and identify the target proteins of oleanolic acid.