Noninvasive Detection of Matrix Metalloproteinase Activity In Vivo using a Novel Magnetic Resonance Imaging Contrast Agent with a Solubility Switch

We have developed novel proteinase-modulated contrast agents (PCAs) to detect the activity of proteinases in vivo using magnetic resonance imaging. The PCAs are based on the concept of a solubility switch, from hydrophilic to hydrophobic, that significantly modifies the pharmacokinetic properties of...

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Main Authors: Martin Lepage, William C. Dow, Marco Melchior, Ying You, Barbara Fingleton, C. Chad Quarles, Claude Pépin, John C. Gore, Lynn M. Matrisian, J. Oliver McIntyre
Format: Article
Language:English
Published: SAGE Publishing 2007-11-01
Series:Molecular Imaging
Online Access:https://doi.org/10.2310/7290.2007.00035
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author Martin Lepage
William C. Dow
Marco Melchior
Ying You
Barbara Fingleton
C. Chad Quarles
Claude Pépin
John C. Gore
Lynn M. Matrisian
J. Oliver McIntyre
author_facet Martin Lepage
William C. Dow
Marco Melchior
Ying You
Barbara Fingleton
C. Chad Quarles
Claude Pépin
John C. Gore
Lynn M. Matrisian
J. Oliver McIntyre
author_sort Martin Lepage
collection DOAJ
description We have developed novel proteinase-modulated contrast agents (PCAs) to detect the activity of proteinases in vivo using magnetic resonance imaging. The PCAs are based on the concept of a solubility switch, from hydrophilic to hydrophobic, that significantly modifies the pharmacokinetic properties of the agent as revealed by the slow efflux kinetics from the activity site. Our compound PCA7-switch detects the activity of the secreted matrix-degrading proteinase matrix-metalloproteinase 7 (MMP-7) in living, tumor-bearing mice. Control experiments were performed using an agent that was not cleaved by MMP-7 (PCA7-scrambled), an agent that could be cleaved by MMP-7 but lacked the solubility switch (PCA7-B), and a standard contrast agent (gadolinium–diethylenetriaminepentaacetic acid). PCA7-switch detected a reduction in MMP-7 activity in tumor-bearing mice treated with a synthetic MMP inhibitor, demonstrating its effectiveness in noninvasive functional imaging of proteolytic activity in vivo.
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institution Kabale University
issn 1536-0121
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publisher SAGE Publishing
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series Molecular Imaging
spelling doaj-art-9e994925d1524712bfd45a3008b4ca0f2025-01-02T02:59:18ZengSAGE PublishingMolecular Imaging1536-01212007-11-01610.2310/7290.2007.0003510.2310_7290.2007.00035Noninvasive Detection of Matrix Metalloproteinase Activity In Vivo using a Novel Magnetic Resonance Imaging Contrast Agent with a Solubility SwitchMartin LepageWilliam C. DowMarco MelchiorYing YouBarbara FingletonC. Chad QuarlesClaude PépinJohn C. GoreLynn M. MatrisianJ. Oliver McIntyreWe have developed novel proteinase-modulated contrast agents (PCAs) to detect the activity of proteinases in vivo using magnetic resonance imaging. The PCAs are based on the concept of a solubility switch, from hydrophilic to hydrophobic, that significantly modifies the pharmacokinetic properties of the agent as revealed by the slow efflux kinetics from the activity site. Our compound PCA7-switch detects the activity of the secreted matrix-degrading proteinase matrix-metalloproteinase 7 (MMP-7) in living, tumor-bearing mice. Control experiments were performed using an agent that was not cleaved by MMP-7 (PCA7-scrambled), an agent that could be cleaved by MMP-7 but lacked the solubility switch (PCA7-B), and a standard contrast agent (gadolinium–diethylenetriaminepentaacetic acid). PCA7-switch detected a reduction in MMP-7 activity in tumor-bearing mice treated with a synthetic MMP inhibitor, demonstrating its effectiveness in noninvasive functional imaging of proteolytic activity in vivo.https://doi.org/10.2310/7290.2007.00035
spellingShingle Martin Lepage
William C. Dow
Marco Melchior
Ying You
Barbara Fingleton
C. Chad Quarles
Claude Pépin
John C. Gore
Lynn M. Matrisian
J. Oliver McIntyre
Noninvasive Detection of Matrix Metalloproteinase Activity In Vivo using a Novel Magnetic Resonance Imaging Contrast Agent with a Solubility Switch
Molecular Imaging
title Noninvasive Detection of Matrix Metalloproteinase Activity In Vivo using a Novel Magnetic Resonance Imaging Contrast Agent with a Solubility Switch
title_full Noninvasive Detection of Matrix Metalloproteinase Activity In Vivo using a Novel Magnetic Resonance Imaging Contrast Agent with a Solubility Switch
title_fullStr Noninvasive Detection of Matrix Metalloproteinase Activity In Vivo using a Novel Magnetic Resonance Imaging Contrast Agent with a Solubility Switch
title_full_unstemmed Noninvasive Detection of Matrix Metalloproteinase Activity In Vivo using a Novel Magnetic Resonance Imaging Contrast Agent with a Solubility Switch
title_short Noninvasive Detection of Matrix Metalloproteinase Activity In Vivo using a Novel Magnetic Resonance Imaging Contrast Agent with a Solubility Switch
title_sort noninvasive detection of matrix metalloproteinase activity in vivo using a novel magnetic resonance imaging contrast agent with a solubility switch
url https://doi.org/10.2310/7290.2007.00035
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