Targeting Tyrosinase: Heterocyclic Compounds in the Spotlight

Tyrosinase (TYR) is a multifunctional, glycosylated, copper-containing oxidase and metalloenzyme that falls within the type-3 copper protein family. The primary function of tyrosinase is the catalytic oxidation of two consecutive steps involved in the biosynthesis of melanin. TYR is responsible for the enzymatic browning of fruits and vegetables and hyperpigmentation in human skin, which results in economic loss as well as skin cancer in humans. Consequently, tyrosinase inhibitors (TYRIs) emerge as potential chemotherapeutic skin whitening and browning inhibitors in fruits, as well as anti-melanogenic substances for treating melanoma. The development of novel inhibitors with lesser side effects or without side effects remains a current topic in medicinal chemistry because already reported tyrosinase inhibitors showed side effects. Heterocycles emerged as novel tyrosinase inhibitors that possess different bioactive functionalities and substitution patterns that play a fundamental role in their anti-tyrosinase activity. Therefore, focusing this chapter on TYRI-bearing heterocycles proves to be valuable and inspirational for the scientific community, as it offers insights for designing new generations of molecules capable of inhibiting or even degrading tyrosinase. The researchers are encouraged to develop new efficient and potent heterocyclic tyrosinase inhibitors for use in foods, cosmetics, and to treat skin cancer.