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奥沙利铂与顺铂:它们与溶菌酶结合的竞争实验

Oxaliplatin vs. cisplatin: competition experiments on their binding to lysozyme.

作者信息

Marasco Daniela, Messori Luigi, Marzo Tiziano, Merlino Antonello

机构信息

Department of Pharmacy, University of Naples Federico II, via Montesano 12, 80120, Napoli, Italy.

出版信息

Dalton Trans. 2015 Jun 14;44(22):10392-8. doi: 10.1039/c5dt01279a.

Abstract

The model protein hen egg white lysozyme was challenged with oxaliplatin and cisplatin. ESI mass spectrometry, surface plasmon resonance and thermal shift analyses demonstrate the formation of a bis-platinum adduct, though in very small amounts. Crystals of the bis-platinum adduct were obtained using two different preparations and the X-ray structures were solved at 1.85 Å and 1.95 Å resolution. Overall, the obtained data point out that, under the analyzed conditions, the two Pt drugs have similar affinities for the protein, but bind on its surface at two non-overlapping sites. In other words, these two drugs manifest a significantly different reactivity with this model protein and do not compete for the same protein binding sites.

摘要

用奥沙利铂和顺铂对模型蛋白鸡蛋清溶菌酶进行处理。电喷雾电离质谱、表面等离子体共振和热迁移分析表明形成了双铂加合物,尽管量非常少。使用两种不同的制剂获得了双铂加合物的晶体,并在1.85 Å和1.95 Å分辨率下解析了X射线结构。总体而言,所获得的数据表明,在分析的条件下,这两种铂类药物对该蛋白具有相似的亲和力,但在其表面的两个不重叠位点结合。换句话说,这两种药物与该模型蛋白表现出明显不同的反应性,并且不会竞争相同的蛋白结合位点。

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