The search for mitochondria-targeted drugs has dramatically risen over the last decade. Mitochondria are essential organelles serving not only as a powerhouse of the cell but also as a key player in cell proliferation and cell death. Their central role in the energetic metabolism, calcium homeostasis and apoptosis makes them an intriguing field of interest for cancer pharmacology. In cancer cells, many mitochondrial signaling and metabolic pathways are altered. These changes contribute to cancer development and progression. Due to changes in mitochondrial metabolism and changes in membrane potential, cancer cells are more susceptible to mitochondria-targeted therapy. The loss of functional mitochondria leads to the arrest of cancer progression and/or a cancer cell death. Identification of mitochondrial changes specific for tumor growth and progression, rational development of new mitochondria-targeted drugs and research on delivery agents led to the advance of this promising area. This review will highlight the current findings in mitochondrial biology, which are important for cancer initiation, progression and resistance, and discuss approaches of cancer pharmacology with a special focus on the anti-cancer drugs referred to as ‘mitocans’.

在过去十年中，对线粒体靶向药物的研究急剧增加。线粒体是必不可少的细胞器，不仅是细胞的动力源，而且是细胞增殖和细胞死亡的关键参与者。它们在能量代谢、钙稳态和细胞凋亡中的核心作用使它们成为癌症药理学的一个有趣的研究领域。在癌细胞中，许多线粒体信号和代谢途径发生了改变。这些变化有助于癌症的发展和进展。由于线粒体代谢的变化和膜电位的变化，癌细胞更容易受到线粒体靶向治疗的影响。功能性线粒体的丧失导致癌症进展和/或癌细胞死亡的停滞。识别特定于肿瘤生长和进展的线粒体变化，合理开发新的线粒体靶向药物以及对递送剂的研究，推动了这一有前景的领域的发展。这篇综述将重点介绍线粒体生物学的最新发现，这些发现对癌症的发生、进展和抵抗很重要，并讨论了癌症药理学的方法，特别关注被称为“线粒体”的抗癌药物。