Issue 4, 2017

Enzyme-triggered compound release using functionalized antimicrobial peptide derivatives


Controlled release is one of the key technologies for medical innovation, and many stimulus-responsive nanocarriers have been developed to utilize this technology. Enzyme activity is one of the most useful stimuli, because many enzymes are specifically activated in diseased tissues. However, controlled release stimulated by enzyme activity has not been frequently reported. One of the reasons for this is the lack of versatility of carriers. Most of the reported stimulus-responsive systems involve a sophisticated design and a complicated process for the synthesis of stimulus-responsive nanocarrier components. The purpose of this study was to develop versatile controlled release systems triggered by various stimuli, including enzyme activity, without modifying the nanocarrier components. We developed two controlled release systems, both of which comprised a liposome as the nanocarrier and a membrane-damaging peptide, temporin L (TL), and its derivatives as the release-controllers. One system utilized branched peptides for proteases, and the other utilized phosphopeptides for phosphatases. In our systems, the target enzymes converted the non-membrane-damaging TL derivatives into membrane-damaging peptides and released the liposome inclusion. We demonstrated the use of our antimicrobial peptide-based controlled release systems for different enzymes and showed the promise of this technology as a novel theranostic tool.

Graphical abstract: Enzyme-triggered compound release using functionalized antimicrobial peptide derivatives

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Article information

Article type
Edge Article
05 Oct 2016
07 Feb 2017
First published
20 Feb 2017
This article is Open Access

All publication charges for this article have been paid for by the Royal Society of Chemistry
Creative Commons BY license

Chem. Sci., 2017,8, 3047-3053

Enzyme-triggered compound release using functionalized antimicrobial peptide derivatives

S. Mizukami, M. Kashibe, K. Matsumoto, Y. Hori and K. Kikuchi, Chem. Sci., 2017, 8, 3047 DOI: 10.1039/C6SC04435B

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