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Bioconjug Chem. 2009 Oct 21;20(10):1836-42. doi: 10.1021/bc900207k. Epub 2009 Sep 14.

"Zipper" molecular beacons: a generalized strategy to optimize the performance of activatable protease probes.

Author information

1
Department of Medical Biophysics, Ontario Cancer Institute, University of Toronto, Toronto, Ontario, Canada.

Abstract

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.

PMID:
19754039
DOI:
10.1021/bc900207k
[Indexed for MEDLINE]

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