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Discovery of small-molecule inhibitors of tyrosinase |
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| Authors: | Germanas Juris P Wang Shugauang Miner Andrew Hao Wayne Ready Joseph M |
| Affiliation: | aDepartment of Dermatology, University of Texas Southwestern Medical Center, Dallas, TX 75390-9038, USA bHigh Throughput Screening Facility, University of Texas Southwestern Medical Center, Dallas, TX 75390-9038, USA cDepartment of Biochemistry, University of Texas Southwestern Medical Center, Dallas, TX 75390-9038, USA |
| 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. |
| Keywords: | High-throughput screening Fluorescence Tyrosinase inhibitors Pigmentation Thiazoles |
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