Copper overload within the body may lead to cancer, neurodegenerative diseases, inflammation or fibrosis, among others. Copper chelation is an effective strategy to counteract this potential overload; mitochondria play an important role, as they are the main copper-using organelles in the cells. Copper chelators have been developed, but they have shown some undesired off-target effects and low specificity, which suggests the need for new therapies in the field.