Discovery of small-molecule inhibitors of tyrosinase

Bioorg Med Chem Lett. 2007 Dec 15;17(24):6871-5. doi: 10.1016/j.bmcl.2007.10.014. Epub 2007 Oct 12.

Abstract

To identify novel inhibitors of tyrosinase, a fluorescent assay was developed which is suitable for high-throughput screening. In the assay, oxidation of the substrate by tyrosinase leads to the release of a fluorescent coumarin. Several small molecules were identified that inhibited mushroom tyrosinase in vitro and human tyrosinase in cell culture. These compounds may represent lead structures for therapies targeted at disorders of hyperpigmentation.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Agaricales / drug effects
  • Agaricales / enzymology
  • Catalysis
  • Cell Line
  • Enzyme Inhibitors / chemistry*
  • Enzyme Inhibitors / pharmacology*
  • Molecular Structure
  • Monophenol Monooxygenase / antagonists & inhibitors*
  • Monophenol Monooxygenase / metabolism
  • Oxidation-Reduction
  • Pigmentation / drug effects
  • Structure-Activity Relationship

Substances

  • Enzyme Inhibitors
  • Monophenol Monooxygenase