Discovery of small-molecule inhibitors of tyrosinase

被引：57
|
作者：
Germanas, Juris P. [1 ]
Wang, Shugauang [2 ]
Miner, Andrew [1 ]
Hao, Wayne [2 ]
Ready, Joseph M. [3 ]
机构：
[1] Univ Texas SW Med Ctr Dallas, Dept Dermatol, Dallas, TX 75390 USA
[2] Univ Texas SW Med Ctr Dallas, High Throughput Screening Facil, Dallas, TX 75390 USA
[3] Univ Texas SW Med Ctr Dallas, Dept Biochem, Dallas, TX 75390 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 24期
关键词：
high-throughput screening; fluorescence; tyrosinase inhibitors; pigmentation; thiazoles;
D O I：
10.1016/j.bmcl.2007.10.014
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
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. (c) 2007 Elsevier Ltd. All rights reserved.
引用
收藏
页码：6871 / 6875
页数：5
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