P-type ATPases operate as molecular pumps in cells and transport various substrates across biological membranes using ATP as the energy source. They play a key role in a broad range of cellular functions such as generating vitally important ion gradients, uptake or extrusion of heavy metals or polyamines, controlling lipid asymmetry and vesicle formation in membranes. Therefore, they allow interaction between the extracellular and intracellular environment and serve as critical mediators of physiological activities of cells and organelles.

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The members of the P-type ATPases share a general characteristic architecture and working mechanism but, at the same time, are unique proteins through their specificity to the substrate, mode of regulation, subcellular localization and tissue distribution. Not only dysregulation or dysfunction of P-type ATPases, but also mutations in their genes are often associated with human diseases. Hence, these proteins represent important therapeutic targets for drug discovery .