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核苷/碱基转运蛋白:未来的药物靶点?

Nucleoside/nucleobase transporters: drug targets of the future?

机构信息

Faculty of Pharmacy, University of Sydney, NSW 2006, Australia.

出版信息

Future Med Chem. 2009 May;1(2):303-26. doi: 10.4155/fmc.09.29.

Abstract

BACKGROUND

Nucleoside/nucleobase transporters have been investigated since the 1960s. In particular, equilibrative nucleoside transporters were thought to be valuable drug targets, since they are involved in various kinds of viral and parasitic diseases as well as cancers.

DISCUSSION

In the postgenomic era multiple transporters, including different subtypes, have been cloned and characterized on the molecular level. In this article we summarize recent advances regarding structure, function and localization of nucleoside/nucleobase transporters as well as the pharmacological profile of selected drugs.

CONCLUSION

Knowledge of the different kinetic properties and structural features of nucleoside transporters can either be used for the rational design of therapeutics directly targeting the transporter itself or for the delivery of drugs using the transporter as a port of entry into the target cell. Equilibrative nucleoside transporters are of considerable pharmacological interest as drug targets for the development of drugs tailored to each patient's need for the treatment of cardiac disease, cancer and viral infections.

摘要

背景

自 20 世纪 60 年代以来,核苷/碱基转运体一直受到研究。特别是,平衡核苷转运体被认为是有价值的药物靶点,因为它们参与了各种病毒和寄生虫疾病以及癌症。

讨论

在后基因组时代,已经在分子水平上克隆和表征了多种转运体,包括不同的亚型。在本文中,我们总结了关于核苷/碱基转运体的结构、功能和定位以及选定药物的药理学特征的最新进展。

结论

对核苷转运体的不同动力学特性和结构特征的了解,既可以用于直接针对转运体本身的治疗药物的合理设计,也可以用于利用转运体作为进入靶细胞的入口来输送药物。平衡核苷转运体作为药物靶点具有相当大的药理学意义,可用于开发针对每个患者心脏病、癌症和病毒感染治疗需求的药物。

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