Simple mimetics of a nuclear localization signal (NLS).
Simple mimetics of a nuclear localization signal (NLS).
复制标题
核定位信号（NLS）的简单模拟。
DOI：
10.1021/ol034640t
复制
发表时间：
2003
期刊：
影响因子：
--
通讯作者：
Standaert,RobertF
中科院分区：
文献类型：
--
作者：
Park,SeungBum;Ho,ThaiH;Reedy,BrianM;Connolly,MichaelD;Standaert,RobertF
使用分子建模来设计HIV-1基质蛋白核定位信号（NLS）的模拟物，其中通过二酰胺接头连接的两个间苯二酚单元的支架呈现3-氨基丙基醚代替赖氨酸侧链。合成了具有6、8、10或12个原子的接头的预期模拟物，并在与核输入受体亚基karyopherin α结合的竞争测定中进行了比较，显示10个原子的接头是最好的，较短的接头无效。
Molecular modeling was used to design mimetics of the HIV-1 matrix protein nuclear localization signal (NLS) in which a scaffold of two resorcinol units joined by a diamide linker presents 3-aminopropyl ethers in place of lysine side chains. Prospective mimetics with linkers of 6, 8, 10, or 12 atoms were synthesized and compared in a competition assay for binding to the nuclear import receptor subunit karyopherin α, showing the 10-atom linker to be best and shorter ones ineffective.