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Since the success of cisplatin and auranofin, transition metal\u2010based compounds have become a prospective source for drug development, particularly in cancer treatment. In recent years, extensive studies have shown that numerous transition metal\u2010based compounds could modulate autophagy, promising a new therapeutic strategy for metal\u2010related diseases and the design of metal\u2010based agents. Copper, zinc, and manganese, which are common components in physiological pathways, play important roles in the progression of cancer, neurodegenerative diseases, and cardiovascular diseases. Furthermore, enrichment of copper, zinc, or manganese can regulate autophagy. 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