Design and discovery of mushroom tyrosinase inhibitors and their therapeutic applications.
BACKGROUND
Tyrosinase inhibitors could have a huge importance in medicine, cosmetics and agriculture. Although many tyrosinase inhibitors are available, they have demonstrated only mild efficacy and safety concerns. This has led to the discovery of novel tyrosinase inhibitors that are more safe, potent and efficacious.


METHODS
The authors provide an overview of the recent scientific accounts describing the design of new molecules. These compounds belong to different chemical families. The review emphasizes the rationale behind the discovery, the study of structure-activity relationships, the study of the mechanism and kinetic of inhibition and the cellular effect of the inhibitors. The article is based on the literature published from 2007 onward related with the development of synthetic tyrosinase inhibitors.


CONCLUSIONS
Although a great number of tyrosinase inhibitors have been published in the literature, none, as of yet, have reached the potency and safety requirements needed to enter clinical trials. The emergence of new in vitro and in vivo tests will finally allow the arrival of new compounds that are more potent and safe.
Universidade de Lisboa, Instituto de Investigação do Medicamento (iMed.ULisboa), Faculdade de Farmácia, Department of Toxicological and Bromatological Sciences , Av. Prof. Gama Pinto, 1649-003 Lisboa , Portugal ermendes@ff.ul.pt.
Eduarda
E
Mendes
Maria de Jesus
Mde J
Perry
Ana Paula
AP
Francisco
D000363:Agaricales / Q000737:chemistry*; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D014442:Monophenol Monooxygenase / Q000037:antagonists & inhibitors*
D004791:Enzyme Inhibitors; D014442:Monophenol Monooxygenase