Quantitative comparison of the relative cell permeability of cyclic and linear peptides
Quantitative comparison of the relative cell permeability of cyclic and linear peptides
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DOI：
10.1016/j.chembiol.2007.05.006
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发表时间：
2007-06-01
影响因子：
--
通讯作者：
Kodadek, Thomas
中科院分区：
文献类型：
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作者：
Kwon, Yong-Uk;Kodadek, Thomas
环肽作为潜在的蛋白质配体具有相当大的兴趣。据推测，环状分子可能比它们的线性对应物更具有细胞渗透性，这是由于它们的构象柔性降低。我们报告了一项研究，测试这一假设，通过使用定量，报告基因为基础的测定，测量相对细胞渗透性的类固醇共轭分子的利益。我们证明，环肽，事实上，一般不超过其线性对应物的渗透性。
Cyclic peptides are of considerable interest as potential protein ligands. It has been postulated that cyclic molecules might be more cell permeable than their linear counterparts due to their reduced conformational flexibility. We report a study that tests this hypothesis by using a quantitative, reporter gene-based assay that measures the relative cell permeability of steroid conjugates of molecules of interest. We demonstrate that cyclic peptides are, in fact, not generally more permeable than their linear counterparts.