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An important class of nanomaterials exploited for theranostics is metal nanoclusters (NCs). In contrast to gold and silver NCs, copper is an essential trace element for humans. It can be more easily removed from the body. This, along with the low cost of copper that offers potential large\u2010scale nanotechnology applications, means that copper NCs have attracted great interest in recent years. The latest advances in the design, synthesis, surface engineering, and applications of copper NCs in disease diagnosis, monitoring, and treatment are reviewed. Strategies to control and enhance the emission of copper NCs are considered. 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