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Increasing attention is being focused on skin health currently, especially the excessive deposition of melanin in the skin. Tyrosinase, the rate-limiting enzyme in melanin biosynthesis, is a crucial enzyme in melanin synthesis. However, existing tyrosinase inhibitors pose some degree of toxicity to humans. Therefore, the development of more efficient and low-toxicity tyrosinase inhibitors is urgently needed. This review briefly depicts the melanin biosynthesis process and the crystal structure and catalytic mechanism of tyrosinase. The latest research progress regarding small-molecule tyrosinase inhibitors is also reviewed. Moreover, the structure–function relationships are analyzed and summarized. This is expected to provide new and more scientific insights to enable researchers to explore safer and more potent tyrosinase inhibitors.
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1 School of Pharmacy, Hangzhou Normal University, Hangzhou 311121, China; Key Laboratory of Elemene Class Anti-Tumor Chinese Medicines, Engineering Laboratory of Development and Application of Traditional Chinese Medicines, Collaborative Innovation Center of Traditional Chinese Medicines of Zhejiang Province, Hangzhou Normal University, Hangzhou 311121, China