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谷胱甘肽缀合物及其合成衍生物作为参与癌症和耐药性的谷胱甘肽依赖性酶的抑制剂。

Glutathione conjugates and their synthetic derivatives as inhibitors of glutathione-dependent enzymes involved in cancer and drug resistance.

作者信息

Burg Danny, Mulder Gerard J

机构信息

Division of Toxicology, Leiden/Amsterdam Center for Drug Research, Leiden University, Einsteinweg 55 2333CC, Leiden, The Netherlands.

出版信息

Drug Metab Rev. 2002 Nov;34(4):821-63. doi: 10.1081/dmr-120015695.

DOI:10.1081/dmr-120015695
PMID:12487151
Abstract

Alterations in levels of glutathione (GSH) and glutathione-dependent enzymes have been implicated in cancer and multidrug resistance of tumor cells. The activity of a number of these, the multidrug resistance-associated protein 1, glutathione S-transferase, DNA-dependent protein kinase, glyoxalase I, and gamma-glutamyl transpeptidase, can be inhibited by GSH-conjugates and synthetic analogs thereof. In this review we focus on the function of these enzymes and carriers in cancer and anti-cancer drug resistance, in relation to their inhibition by GSH-conjugate analogs.

摘要

谷胱甘肽(GSH)水平及谷胱甘肽依赖性酶的改变与癌症及肿瘤细胞的多药耐药性有关。其中多种酶,如多药耐药相关蛋白1、谷胱甘肽S-转移酶、DNA依赖性蛋白激酶、乙二醛酶I和γ-谷氨酰转肽酶的活性可被谷胱甘肽缀合物及其合成类似物所抑制。在本综述中,我们聚焦于这些酶和载体在癌症及抗癌药物耐药性方面的功能,以及它们与谷胱甘肽缀合物类似物抑制作用的关系。

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