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’.
Keywords: Mitochondria, targeting, metabolism, cancer, treatment, inhibitors, hexokinase, tricarboxylic acid cycle, respiratory
chain, electron transport chain.
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