Abstract
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.