Liu Bo, Alluri Prasanna G, Yu Peng, Kodadek Thomas
Departments of Internal Medicine and Molecular Biology and Center for Biomedical Inventions, University of Texas Southwestern Medical Center, 5323 Harry Hines Boulevard, Dallas, TX 75390, USA.
J Am Chem Soc. 2005 Jun 15;127(23):8254-5. doi: 10.1021/ja0515295.
Transcriptional coactivator-binding peptoids were isolated from a large combinatorial library. One of these molecules is shown to function as a potent activation domain surrogate in mammalian cells. Up to a 900-fold increase in expression of a Gal4-responsive reporter gene is observed when a steroid conjugate of the peptoid is incubated with HeLa cells expressing a Gal4 DNA-binding domain (DBD)-glucocorticoid receptor ligand-binding domain (GRLBD) fusion protein.
从一个大型组合文库中分离出转录共激活因子结合类肽。其中一种分子在哺乳动物细胞中表现为一种有效的激活域替代物。当类肽的类固醇共轭物与表达Gal4 DNA结合结构域（DBD）-糖皮质激素受体配体结合结构域（GRLBD）融合蛋白的HeLa细胞一起孵育时，观察到Gal4反应性报告基因的表达增加了900倍。
