Therapeutic Approach in Cancer: The Role of Ion Channels and Transporters

Over the previous 20 years, knowledge of ion channels and transporters in cancer biology has significantly evolved, transforming them into promising therapeutic targets. These membrane-bound proteins control the ion flux, including calcium, sodium, potassium, chloride, and metal ions, which are key contributors to tumorigenesis and influence critical cellular processes. The TRPM7 channel, for example, has been associated with a negative outlook and aggressive breast cancer. Cancer cells often exhibit altered expression and functionality of these channels, offering a therapeutic advantage by allowing selective targeting. Ion channels also interact with oxidative stress pathways, immune responses, cellular metabolism, and signal transduction networks, making them central to cancer cell survival and adaptation. In preclinical studies, various modulators, including natural products, existing drugs, and novel synthetic inhibitors, have demonstrated significant anticancer activity. However, translating these findings into clinical success faces challenges, particularly regarding specificity and side effects. Thus, this chapter delves into the innovative strategies, including conformation-specific inhibitors, antibody-based targeting, peptide toxins, and using ligands to deliver cytotoxic drugs directly to cancer cells. Also, discuss how combining these ionic modulators with conventional treatments is a promising approach in enhancing efficacy, reducing dosage requirements, minimizing side effects, and preventing therapeutic resistance.