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一种新方法用于测定喜树碱及其类似物与人血清白蛋白的亲和力。

A new approach to determine camptothecin and its analogues affinity to human serum albumin.

机构信息

Department of Medicinal Chemistry, Faculty of Pharmacy, Collegium Medicum, Nicolaus Copernicus University, M. Skłodowskiej-Curie 9, 85-094 Bydgoszcz, Poland.

出版信息

J Pharm Sci. 2011 Mar;100(3):1142-6. doi: 10.1002/jps.22318. Epub 2010 Aug 25.

Abstract

A novel and fast method for the determination of the binding kinetic data of ligand to protein has been developed. A new tool including human serum albumin-coated magnetic beads (HSA-MB) was used to determine the affinity of camptothecin (CPT) and its analogues to HSA. From the biological activity point of view, these compounds have potential anticancer activity. However, the numerous studies indicate that some of these analogues have a strong affinity to plasma proteins stopping their effective therapy. Thus, the problem of plasma protein binding behavior of CPT's analogues was the subject of this study.

摘要

一种新的快速测定配体与蛋白质结合动力学数据的方法已经建立。本研究使用包括人血清白蛋白包被的磁性珠(HSA-MB)的新工具来测定喜树碱(CPT)及其类似物与人血清白蛋白的亲和力。从生物活性的角度来看,这些化合物具有潜在的抗癌活性。然而,大量的研究表明,其中一些类似物对血浆蛋白具有很强的亲和力,从而阻止了它们的有效治疗。因此,CPT 类似物的血浆蛋白结合行为问题是本研究的主题。

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