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The Ca 2+  signaling toolkit is currently under investigation as a potential target for addressing the threat of cancer. A growing body of evidence suggests that calcium signaling plays a crucial role in promoting various aspects of cancer, including cell proliferation, progression, drug resistance, and migration-related activities. Consequently, focusing on these altered Ca 2+  transporting proteins has emerged as a promising area of research for cancer treatment. This review highlights the existing research on the role of Ca 2+ -transporting proteins in cancer progression. It discusses the current studies evaluating Ca 2+  channel/transporter/pump blockers, inhibitors, or regulators as potential anticancer drugs. Additionally, the review addresses specific gaps in our understanding of the field that may require further investigation. Targeting specific Ca 2+  signaling cascades could disrupt normal cellular activities, making cancer therapy complex and elusive. Therefore, there is a need for improvements in current Ca 2+  signaling pathway focused medicines. While synthetic molecules and plant compounds show promise, they also come with certain limitations. Hence, exploring the framework of targeted drug delivery, structure-rationale-based designing, and repurposing potential drugs to target Ca 2+  transporting proteins could potentially lead to a significant breakthrough in cancer treatment.

New frontiers in the design and discovery of therapeutics that target calcium ion signaling: a novel approach in the fight against cancer