title: Skin whitening agents: medicinal chemistry perspective of tyrosinase inhibitors.
abstract: Melanogenesis is a process to synthesize melanin, which is a primary responsible for the pigmentation of human skin, eye and hair. Although numerous enzymatic catalyzed and chemical reactions are involved in melanogenesis process, the enzymes such as tyrosinase and tyrosinase-related protein-1 (TRP-1) and TRP-2 played a major role in melanin synthesis. Specifically, tyrosinase is a key enzyme, which catalyzes a rate-limiting step of the melanin synthesis, and the downregulation of tyrosinase is the most prominent approach for the development of melanogenesis inhibitors. Therefore, numerous inhibitors that target tyrosinase have been developed in recent years. The review focuses on the recent discovery of tyrosinase inhibitors that are directly involved in the inhibition of tyrosinase catalytic activity and functionality from all sources, including laboratory synthetic methods, natural products, virtual screening and structure-based molecular docking studies.
authors.affiliation: a PharmaCenter Bonn , Pharmaceutical Institute, Pharmaceutical Chemistry I, University of Bonn , Bonn , Germany.
authors.forename: Thanigaimalai
authors.initials: T
authors.lastname: Pillaiyar
authors.affiliation: b College of Pharmacy and Institute of Drug Research and Development , Chungnam National University , Daejeon , Korea.
authors.forename: Manoj
authors.initials: M
authors.lastname: Manickam
authors.affiliation: a PharmaCenter Bonn , Pharmaceutical Institute, Pharmaceutical Chemistry I, University of Bonn , Bonn , Germany.
authors.forename: Vigneshwaran
authors.initials: V
authors.lastname: Namasivayam
mesh_terms: D000818:Animals; D002384:Catalysis; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D006801:Humans; D008543:Melanins / Q000037:antagonists & inhibitors / Q000096:biosynthesis; D014442:Monophenol Monooxygenase / Q000037:antagonists & inhibitors*; D062327:Skin Lightening Preparations
chemical_list: D004791:Enzyme Inhibitors; D008543:Melanins; D062327:Skin Lightening Preparations; D014442:Monophenol Monooxygenase
keywords: Parkinson’s disease; human tyrosinase; inhibitors; skin whitening agents; structure–activity relationships