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首页> 外文期刊>Medicinal research reviews >Platinum-based anticancer agents: Innovative design strategies and biological perspectives.
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Platinum-based anticancer agents: Innovative design strategies and biological perspectives.

机译：铂基抗癌剂：创新的设计策略和生物学观点。

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The impact of cisplatin on cancer chemotherapy cannot be denied. Over the past 20 years, much effort has been dedicated to discover new platinum-based anticancer agents that are superior to cisplatin or its analogue, carboplatin. Most structural modifications are based on changing one or both of the ligand types coordinated to platinum. Altering the leaving group can influence tissue and intracellular distribution of the drug, whereas the carrier ligand usually determines the structure of adducts formed with DNA. DNA-Pt adducts produced by cisplatin and many of its classical analogues are almost identical, and would explain their similar patterns of tumor sensitivity and susceptibility to resistance. Recently some highly innovative design strategies have emerged, aimed at overcoming platinum resistance and/or to introduce novel mechanisms of antitumor action. Platinum compounds bearing the 1,2-diaminocyclohexane carrier ligand; and those of multinuclear Pt complexes giving rise to radically different DNA-Pt adducts, have resulted in novel anticancer agents capable of circumventing cisplatin resistance. Other strategies have focused on integrating biologically active ligands with platinum moieties intended to selectively localizing the anticancer properties. With the rapid advance in molecular biology, combined with innovation, it is possible new Pt-based anticancer agents will materialize in the near future.
机译：顺铂对癌症化疗的影响不可否认。在过去的20年中，人们一直致力于发现优于顺铂或其类似物卡铂的新型铂基抗癌药。大多数结构修饰是基于改变与铂配位的一种或两种配体类型。改变离去基团可以影响药物的组织和细胞内分布，而载体配体通常决定与DNA形成的加合物的结构。顺铂及其许多经典类似物产生的DNA-Pt加合物几乎相同，这可以解释它们相似的肿瘤敏感性和耐药性模式。最近，出现了一些高度创新的设计策略，旨在克服铂的抗性和/或引入新的抗肿瘤作用机制。带有1,2-二氨基环己烷载体配体的铂化合物;以及那些多核Pt配合物产生根本不同的DNA-Pt加合物的方法，已经产生了能够规避顺铂耐药性的新型抗癌药。其他策略集中于整合生物活性配体与旨在选择性定位抗癌特性的铂部分。随着分子生物学的飞速发展和创新，在不久的将来可能会出现新的基于Pt的抗癌药。

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