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首页> 外文期刊>Dalton transactions: An international journal of inorganic chemistry >Pre-association of polynuclear platinum anticancer agents on a protein, human serum albumin. Implications for drug design
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Pre-association of polynuclear platinum anticancer agents on a protein, human serum albumin. Implications for drug design

机译：将多核铂抗癌剂与蛋白质，人血清白蛋白预先关联。对药物设计的影响

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摘要

The interactions of polynuclear platinum complexes with human serum albumin were studied. The compounds examined were the "non-covalent" analogs of the trinuclear BBR3464 as well as the dinuclear spermidine-bridged compounds differing in only the presence or absence of a central -NH2-(+) ( BBR3571 and analogs). Thus, closely-related compounds could be compared. Evidence for pre-association, presumably through electrostatic and hydrogen-bonding, was obtained from fluorescence and circular dichroism spectroscopy and Electrospray Ionization Mass Spectrometry ( ESI-MS). In the case of those compounds containing Pt-Cl bonds, further reaction took place presumably through displacement by sulfur nucleophiles. The implications for protein pre-association and plasma stability of polynuclear platinum compounds are discussed.
机译：研究了多核铂配合物与人血清白蛋白的相互作用。所检查的化合物是三核BBR3464的“非共价”类似物，以及双核亚精胺桥接的化合物，仅在存在或不存在中心-NH2-（+）时有所不同（BBR3571和类似物）。因此，可以比较密切相关的化合物。预缔合的证据大概是通过静电键和氢键，是从荧光和圆二色光谱法和电喷雾电离质谱法（ESI-MS）获得的。在那些含有Pt-Cl键的化合物的情况下，推测进一步的反应是通过被硫亲核试剂取代而发生的。讨论了对蛋白质预缔合和多核铂化合物血浆稳定性的影响。

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