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. Epub 2021 Aug 3.

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.

MeSH terms

  • Drug Design / methods*
  • Drug Discovery / methods*
  • Enzyme Inhibitors / pharmacology
  • Enzyme Inhibitors / therapeutic use*
  • Humans
  • Models, Molecular
  • Structure-Activity Relationship

Substances

  • Enzyme Inhibitors