“Zipper” Molecular Beacons: A Generalized Strategy to Optimize the Performance of Activatable Protease Probes
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- 作者：Juan Chen ; Tracy W. B. Liu ; Pui-Chi Lo ; Brian C. Wilson ; Gang Zheng
- 刊名：Bioconjugate Chemistry
- 出版年：2009
- 出版时间：October 21, 2009
- 年：2009
- 卷：20
- 期：10
- 页码：1836-1842
- 全文大小：282K
- 年卷期：v.20,no.10(October 21, 2009)
- ISSN：1520-4812
文摘
We report the proof-of-principle concept for zipper molecular beacons (ZMB) comprising an asymmetrical polyarginine/polyglutamate electrostatic “zipper” hairpin-linked fluorophore−quencher pair. The objective is to balance maximal quenching efficiency and optimal two-step activation (protease cleavage/zipper dissociation), while enhancing target cell uptake. This strategy also eliminates the peptide sequence dependence of conventional protease beacons. This ZMB concept is a generalizable approach to improve the functionality of a wide range of diagnostic/therapeutic probes through a simple switching of substrate sequences.