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靶向药物至线粒体。

Targeting drugs to mitochondria.

机构信息

Department of Pharmaceutical Technology, University of Regensburg, Regensburg, Germany.

出版信息

Eur J Pharm Biopharm. 2012 Sep;82(1):1-18. doi: 10.1016/j.ejpb.2012.05.014. Epub 2012 Jun 9.

Abstract

Mitochondria are of an increasing interest in pharmaceutical and medical research since it has been reported that dysfunction of these organelles contributes to several diseases with a great diversity of clinical appearance. By the fact that mitochondria are located inside the cell and, in turn, origins of mitochondrial diseases or targets of drugs are located inside mitochondria, a drug molecule has to cross several barriers. This is a severe drawback for the selective accumulation of drug molecules in mitochondria. Therefore, targeting strategies such as direct drug modification or encapsulation into nanocarriers have to be applied to achieve an accumulation of drug molecules in these organelles. In this review, it will be demonstrated how properties and dysfunctions of mitochondria are generating a need for the development of mitochondria specific therapies. Furthermore, intracellular targets of mitochondrial diseases, strategies to utilize mitochondrial specificities and targeting approaches will be discussed. Finally, techniques to investigate mitochondrial characteristics and functionality are reviewed.

摘要

线粒体在药物和医学研究中越来越受到关注,因为据报道这些细胞器的功能障碍会导致多种临床表现多样的疾病。由于线粒体位于细胞内,并且线粒体疾病的起源或药物靶点位于线粒体内部,因此药物分子必须穿过多个屏障。这对于药物分子在线粒体中的选择性积累是一个严重的缺陷。因此,必须应用靶向策略,如直接药物修饰或封装到纳米载体中,以实现药物分子在这些细胞器中的积累。在这篇综述中,将展示线粒体的特性和功能障碍如何产生对开发线粒体特异性治疗方法的需求。此外,还将讨论线粒体疾病的细胞内靶点、利用线粒体特异性和靶向方法的策略以及研究线粒体特性和功能的技术。

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