Abstract
Cancer research is nowadays focused on the identification of possible new targets in order to try to develop new drugs for curing untreatable tumors. Ion channels have emerged as “oncogenic” proteins, since they have an aberrant expression in cancers compared to normal tissues and contribute to several hallmarks of cancer, such as metabolic re-programming, limitless proliferative potential, apoptosis-resistance, stimulation of neo-angiogenesis as well as cell migration and invasiveness. In recent years, not only the plasma membrane but also intracellular channels and transporters have arisen as oncological targets and were proposed to be associated with tumorigenesis. Therefore, the research is currently focusing on understanding the possible role of intracellular ion channels in cancer development and progression on one hand and, on the other, on developing new possible drugs able to modulate the expression and/or activity of these channels. In a few cases, the efficacy of channel-targeting drugs in reducing tumors has already been demonstrated in vivo in preclinical mouse models.
Highlights
In the last decades, cancer research has been focused on identifying novel targets for therapy, especially on trying to develop new strategies to fight untreatable tumors
Almost 20 years ago, ion channels were proposed as potential targets: they are often aberrantly expressed in cancer tissues compared to healthy ones, and, importantly, there are many pharmacological tools already available to manipulate them
Another relevant intracellular location is the endoplasmic reticulum (ER): ion channels and transporters of the ER modulate the cytosolic Ca2+ concentration by controlling the uptake and release of calcium from this intracellular store and impact several cellular pathways implicated in the determination of cell fate as well in cell metabolism
Summary
Cancer research has been focused on identifying novel targets for therapy, especially on trying to develop new strategies to fight untreatable tumors. Most of the identified “oncogenic” intracellular channels are located in the outer or inner mitochondrial membrane (OMM and IMM), since this organelle is a key point of control of important hallmarks of cancer, such as ATP-linked metabolism and apoptotic cell death. Another relevant intracellular location is the endoplasmic reticulum (ER): ion channels and transporters of the ER modulate the cytosolic Ca2+ concentration by controlling the uptake and release of calcium from this intracellular store and impact several cellular pathways implicated in the determination of cell fate as well in cell metabolism. We mention cases where pharmacological modulation of these channels points toward a possibility of exploiting them for treatment
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