Quantitative comparison of the relative cell permeability of cyclic and linear peptides

被引:95
作者
Kwon, Yong-Uk
Kodadek, Thomas
机构
[1] Univ Texas, SW Med Ctr, Div Translat Res, Dallas, TX 75390 USA
[2] Univ Texas, SW Med Ctr, Dept Internal Med, Dallas, TX 75390 USA
来源
CHEMISTRY & BIOLOGY | 2007年 / 14卷 / 06期
关键词
D O I
10.1016/j.chembiol.2007.05.006
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
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.
引用
收藏
页码:671 / 677
页数:7
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