MetMed Lab, Department of Chemistry, University of Florence, Florence, Italy.
Anticancer Agents Med Chem. 2011 Dec;11(10):929-39. doi: 10.2174/187152011797927607.
Gold compounds form an interesting class of antiproliferative agents of potential pharmacological use in cancer treatment. Indeed, a number of gold compounds, either gold(III) or gold(I), were recently described and characterised that manifested remarkable cytotoxic properties in vitro against cultured cancer cells; for some of them encouraging in vivo results were also reported toward a few relevant animal models of cancer. The molecular mechanisms through which gold compounds exert their biological effects are still largely unknown and the subject of intense investigations. Recent studies point out that the modes of action of cytotoxic gold compounds are essentially DNA-independent and cisplatin-unrelated, relying -most likely- on gold interactions with a variety of protein targets. Notably, a few cellular proteins playing relevant functional roles were proposed to represent effective targets for cytotoxic gold compounds but these hypotheses need adequate validation. The state of the art of this research area and the perspectives for future studies are herein critically analysed and discussed.
金化合物形成了一类有趣的抗增殖剂，具有在癌症治疗中潜在的药理学用途。事实上，最近已经描述并表征了许多金化合物，无论是三价金还是一价金，它们在体外对培养的癌细胞表现出显著的细胞毒性；对于其中一些化合物，在一些相关的癌症动物模型中也报告了令人鼓舞的体内结果。金化合物发挥其生物学效应的分子机制在很大程度上仍然未知，这是一个激烈研究的课题。最近的研究指出，细胞毒性金化合物的作用模式基本上与 DNA 无关，与顺铂无关，很可能依赖于金与多种蛋白质靶标的相互作用。值得注意的是，一些发挥重要功能作用的细胞蛋白被提出是细胞毒性金化合物的有效靶标，但这些假设需要充分验证。本文批判性地分析和讨论了该研究领域的最新进展和未来研究的前景。
