Lee Kyeong, Lee Jeong Hyung, Boovanahalli Shanthaveerappa K, Jin Yinglan, Lee Mijeoung, Jin Xuejun, Kim Jin Hwan, Hong Young-Soo, Lee Jung Joon
Molecular Cancer Research Center, Korea Research Institute of Bioscience and Biotechnology, Daejeon, Korea, 305-806.
J Med Chem. 2007 Apr 5;50(7):1675-84. doi: 10.1021/jm0610292. Epub 2007 Mar 1.
Structural modification of a compound discovered during screening using an HRE-dependent reporter assay has revealed a novel class of HIF-1 inhibitors, which potently inhibit the HIF-1alpha protein accumulation and its target gene expression under hypoxic conditions in human hepatocellular carcinoma Hep3B cells.
使用依赖于缺氧反应元件(HRE)的报告基因检测法在筛选过程中发现的一种化合物的结构修饰,揭示了一类新型的缺氧诱导因子-1(HIF-1)抑制剂,这类抑制剂在人肝癌Hep3B细胞的缺氧条件下能有效抑制HIF-1α蛋白的积累及其靶基因的表达。