Mitochondria are a major intracellular organelle for drug targeting due to its functional roles in cellular metabolism and cell signaling for proliferation and cell death. Mitochondria-targeted treatment strategy could be promising to improve the therapeutic efficacy of cancer while minimizing the adverse side effects. Over the last decades, several studies have explored and focused on mitochondrial functions, which has led to the emergence of mitochondria-specific therapies. Molecules in the mitochondria are considered to be prime targets, and a wide range of molecular strategies have been designed for targeting mitochondria compared with that of the cytosol. In this review, we focused on the molecular mechanisms of mitochondria-specific ligand targeting and selective drug action strategies for targeting mitochondria, including those premised on mitochondrial targeting of signal peptides (MTS), cell-penetrating peptides (CPPs), and use of lipophilic cations. Furthermore, most research has concentrated on specific conjugation of ligands to therapeutic molecules to enhance their effectiveness. There are several variations for the ideal design and development for mitochondrial-targeted drugs, such as selecting a suitable ligand and linker targets. However, some challenges related to drug solubility and selectivity could be resolved using the nanocarrier system. Nanoparticles yield excellent advantages for targeting and transmitting therapeutic drugs, and they offer elegant platforms for mitochondria-specific drug delivery. We explain many of the advanced and proven strategies for multifunctional mitochondria-specific targets, which should contribute to achieving better anticancer therapies in a promising future.

线粒体是药物靶向的主要细胞内细胞器，因为它在细胞代谢以及增殖和细胞死亡的细胞信号传导中发挥着功能作用。线粒体靶向治疗策略有望提高癌症的治疗效果，同时最大限度地减少不良副作用。在过去的几十年里，多项研究探索并关注线粒体功能，这导致了线粒体特异性疗法的出现。线粒体中的分子被认为是主要靶标，与细胞质相比，已经设计了多种针对线粒体的分子策略。在这篇综述中，我们重点关注线粒体特异性配体靶向的分子机制和靶向线粒体的选择性药物作用策略，包括以线粒体靶向信号肽（MTS）、细胞穿透肽（CPP）和使用亲脂性药物为前提的策略。阳离子。此外，大多数研究都集中在配体与治疗分子的特异性缀合上，以增强其有效性。线粒体靶向药物的理想设计和开发有多种变化，例如选择合适的配体和接头靶点。然而，使用纳米载体系统可以解决与药物溶解度和选择性相关的一些挑战。纳米颗粒在靶向和传输治疗药物方面具有卓越的优势，并且为线粒体特异性药物输送提供了优雅的平台。我们解释了许多针对多功能线粒体特异性靶标的先进且经过验证的策略，这些策略应有助于在充满希望的未来实现更好的抗癌疗法。