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重组人受体蛋白FKBP12与新型神经生长促进剂非共价键复合物的电喷雾质谱 总被引:2,自引:0,他引:2
系统地用电喷雾质谱(ESI-MS)研究了重组人受体蛋白FKBP12(rhFKBP12)和其小分子神经生长促进剂配体的非共价键相互作用, 从52个化合物中筛选出3个有非共价键结合的化合物000107, 000308和A2B12, 并通过竞争实验测定了它们与rhFKBP12的结合位点和相对结合强度. 清华大学对其中的两个000107, 000308做出了复合物X射线晶体衍射的三维结构, 与ESI-MS的结果相同, 其中000308有较好的促神经生长的活性. 相似文献
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An ESI-MS method for studying the non-covalent bond complex of rhFKBP12 with its nonimmunosuppressive ligands was developed. The method was used to screen out three compounds capable of binding to rhFKBP12 non-covalently from 52 compounds. By competing binding experiment, the binding site and the relative binding strength of these three compounds 000107, 000308 and A2B12 with rhFKBP12 were measured. All of them have the same binding site as FK506 does. X-ray crystalline diffraction experiment of non-covalent bond complex of 000107, 000308 with rhFKBP12 by Tsinghua University showed the same results. Among them 000308 has good effect on stimulating neurite to grow in chicken sensory neuronal cultures. 相似文献
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The drug FK506 is a powerful immunosuppressive agent. FKBP12 which has a molecular weight of 12 kD is one of the important members of FK506 binding proteins[1]. After finding it in 1989 scientists began to study its role in mediating responses to immunosuppressant drugs[2—4]. In 1992, it was reported that the level of FKBP12 is 50-fold more abundant in nervous system than that in immune tissues and the immunosuppressive agent FK506 mediated by FKBP12 can pro-mote neurite outgrowth both… 相似文献
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