McNaughton Brian R, Gareiss Peter C, Jacobs Stacey E, Fricke Alex F, Scott Glynis A, Miller Benjamin L
Department of Chemistry, University of Rochester, Rochester, NY 14627 (USA).
ChemMedChem. 2009 Oct;4(10):1583-9. doi: 10.1002/cmdc.200900194.
Small molecules that increase the cellular level of melanin can be used to study melanogenesis, and have therapeutic potential for melanin-related diseases such as albinism. We describe the identification of a potent activator of melanogenesis from a targeted combinatorial library. Treating melanocytes with our most active molecule results in a 1.8-fold increase in melanin, and an increase in tyrosinase-catalyzed oxidation of L-tyrosine, a key step in melanin biosynthesis.
可提高细胞黑色素水平的小分子可用于研究黑色素生成,对诸如白化病等与黑色素相关的疾病具有治疗潜力。我们描述了从一个靶向组合文库中鉴定出一种有效的黑色素生成激活剂。用我们最具活性的分子处理黑素细胞,会使黑色素增加1.8倍,并使酪氨酸酶催化的L - 酪氨酸氧化增加,这是黑色素生物合成中的关键一步。