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铂化合物的发展及其可能的组合。

The development of platinum compounds and their possible combination.

作者信息

Pasetto Lara Maria, D'Andrea Mario Rosario, Brandes Alba Ariela, Rossi Elena, Monfardini Silvio

机构信息

Medical Oncology Division, Azienda Ospedale-Università, Via Gattamelata 64, 35128 Padova, Italy.

出版信息

Crit Rev Oncol Hematol. 2006 Oct;60(1):59-75. doi: 10.1016/j.critrevonc.2006.02.003. Epub 2006 Jun 27.

DOI:10.1016/j.critrevonc.2006.02.003
PMID:16806960
Abstract

Cisplatin plays a central role in cancer chemotherapy in spite of its toxicity. To circumvent this toxicity and to enhance its therapeutic index a lot of preclinical and clinical studies have been conducted and several thousand analogues have been synthesized. Much more analysis remains to be done, but nowadays, the absence of any definitive, biologically interpretable molecular predictor of activity is consistent with the idea that platinum compounds have multiple intracellular targets and that cells can have multiple mechanisms of resistance. This review analyses a part of these platinum compounds analyzed to date, their mechanism of action, resistance and the future trends in this sector.

摘要

尽管顺铂具有毒性,但它在癌症化疗中起着核心作用。为了规避这种毒性并提高其治疗指数,已经进行了大量的临床前和临床研究,并合成了数千种类似物。仍有更多分析有待完成,但如今,缺乏任何明确的、具有生物学可解释性的活性分子预测指标,这与铂化合物具有多个细胞内靶点且细胞可具有多种耐药机制的观点是一致的。本综述分析了迄今为止已分析的部分铂化合物、它们的作用机制、耐药性以及该领域的未来趋势。

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The development of platinum compounds and their possible combination.铂化合物的发展及其可能的组合。
Crit Rev Oncol Hematol. 2006 Oct;60(1):59-75. doi: 10.1016/j.critrevonc.2006.02.003. Epub 2006 Jun 27.
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Molecular mechanisms of platinum resistance: still searching for the Achilles' heel.铂耐药的分子机制:仍在寻找阿喀琉斯之踵。
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