Discovery of small-molecule inhibitors of tyrosinase.
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.
Germanas
Juris P
JP
Department of Dermatology, University of Texas Southwestern Medical Center, Dallas, TX 75390-9038, USA.
Wang
Shugauang
S
Miner
Andrew
A
Hao
Wayne
W
Ready
Joseph M
JM
D000363:Agaricales / Q000187:drug effects / Q000201:enzymology; D002384:Catalysis; D002460:Cell Line; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D015394:Molecular Structure; D014442:Monophenol Monooxygenase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D010084:Oxidation-Reduction; D010858:Pigmentation / Q000187:drug effects; D013329:Structure-Activity Relationship
D004791:Enzyme Inhibitors; D014442:Monophenol Monooxygenase