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Molecules 2015, 20(7), 12076-12092; doi:10.3390/molecules200712076

Development of Radiolabeled Membrane Type-1 Matrix Metalloproteinase Activatable Cell Penetrating Peptide Imaging Probes

1
Department of Biomedical Engineering, Eindhoven University of Technology, High Tech Campus 11, Eindhoven 5656 AE, The Netherlands
2
Department of Oncology Solutions, Philips Research, High Tech Campus 11, Eindhoven 5656 AE, The Netherlands
3
Tagworks Pharmaceuticals, High Tech Campus 11, Eindhoven 5656 AE, The Netherlands
*
Author to whom correspondence should be addressed.
Academic Editor: Derek J. McPhee
Received: 29 April 2015 / Revised: 7 June 2015 / Accepted: 29 June 2015 / Published: 2 July 2015
(This article belongs to the Special Issue Cell Penetrating Peptides (CPPs))
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Abstract

Membrane type-1 matrix metalloproteinase (MT1-MMP or MMP-14) plays an important role in adverse cardiac remodelling. Here, we aimed to develop radiolabeled activatable cell penetrating peptides (ACPP) sensitive to MT1-MMP for the detection of elevated MT1-MMP levels in adverse cardiac remodelling. Three ACPP analogs were synthesized and the most potent ACPP analog was selected using MT1-MMP sensitivity and enzyme specificity assays. This ACPP, called ACPP-B, showed high sensitivity towards MT1-MMP, soluble MMP-2, and MT2-MMP, while limited sensitivity was measured for other members of the MMP family. In in vitro cell assays, radiolabeled ACPP-B showed efficient cellular uptake upon activation. A pilot in vivo study showed increased uptake of the radiolabeled probe in regions of infarcted myocardium compared to remote myocardium, warranting further in vivo evaluation. View Full-Text
Keywords: molecular imaging; activatable cell penetrating peptide; matrix metalloproteinase-14; membrane type-1 matrix metalloproteinase; radiolabeling; myocardial infarction; peptide chemistry molecular imaging; activatable cell penetrating peptide; matrix metalloproteinase-14; membrane type-1 matrix metalloproteinase; radiolabeling; myocardial infarction; peptide chemistry
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

van Duijnhoven, S.M.J.; Robillard, M.S.; Nicolay, K.; Grüll, H. Development of Radiolabeled Membrane Type-1 Matrix Metalloproteinase Activatable Cell Penetrating Peptide Imaging Probes. Molecules 2015, 20, 12076-12092.

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