Recent advances in the design and discovery of synthetic tyrosinase inhibitors

  • Eur J Med Chem. 2021 Nov 15;224:113744. doi: 10.1016/j.ejmech.2021.113744.
Jin Li  1 ,  Lu Feng  1 ,  Li Liu  1 ,  Fang Wang  1 ,  Liang Ouyang  1 ,  Lan Zhang  2 ,  Xiuying Hu  3 ,  Guan Wang  4
Affiliations
  • 1. Innovation Center of Nursing Research, Nursing Key Laboratory of Sichuan Province, State Key Laboratory of Biotherapy and Cancer Center, National Clinical Research Center for Geriatrics, West China Hospital, and College of Chemistry, Sichuan University, Chengdu, Sichuan, 610041, China.
  • 2. School of Life Science and Engineering, Southwest Jiaotong University, Chengdu, 610031, China. Electronic address: [email protected].
  • 3. Innovation Center of Nursing Research, Nursing Key Laboratory of Sichuan Province, State Key Laboratory of Biotherapy and Cancer Center, National Clinical Research Center for Geriatrics, West China Hospital, and College of Chemistry, Sichuan University, Chengdu, Sichuan, 610041, China. Electronic address: [email protected].
  • 4. Innovation Center of Nursing Research, Nursing Key Laboratory of Sichuan Province, State Key Laboratory of Biotherapy and Cancer Center, National Clinical Research Center for Geriatrics, West China Hospital, and College of Chemistry, Sichuan University, Chengdu, Sichuan, 610041, China. Electronic address: [email protected].
PMID: 34365131 DOI: 10.1016/j.ejmech.2021.113744
Abstract

Tyrosinase is a copper-containing metalloenzyme that is responsible for the rate-limiting catalytic step in the melanin biosynthesis and enzymatic browning. As a promising target, Tyrosinase inhibitors can be used as skin whitening agents and food Preservatives, thus having broad potential in the fields of food, cosmetics, agriculture and medicine. From 2015 to 2020, numerous synthetic inhibitors of Tyrosinase have been developed to overcome the challenges of low efficacy and side effects. This review summarizes the enzyme structure and biological functions of Tyrosinase and demonstrates the recent advances of synthetic Tyrosinase inhibitors from the perspective of medicinal chemistry, providing a better understanding of the catalytic mechanisms and more effective Tyrosinase inhibitors.

Keywords
Inhibitors; Medicinal chemistry; Structure-activity relationships; Tyrosinase.
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