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Updated: May 14, 2026
Non-invasive In Vivo Fluorescence Optical Imaging of Inflammatory MMP Activity Using an Activatable Fluorescent Imaging Agent
Published on: May 8, 2017
Probes for non-invasive matrix metalloproteinase-targeted imaging with PET and SPECT
Nathalie Matusiak1, Aren van Waarde, Rainer Bischoff
1Department of Nuclear Medicine and Molecular Imaging, University Medical Center Groningen, Hanzeplein 1, 9700 RB Groningen, The Netherlands. n.matusiak@umcg.nl
Abstract:
Dysregulation of matrix metalloproteinase (MMP) activity can lead to a wide range of disease states such as atherosclerosis, inflammation or cancer. The ability to image MMP activity non-invasively in vivo, by radiolabelled synthetic inhibitors, would allow the characterization of atherosclerotic plaques, inflammatory lesions or tumors. Here we present an overview of radiolabelled MMP inhibitors (MMPIs) and MMP peptides for positron emission tomography (PET) and single photon emission computed tomography (SPECT) for the detection of proteolytic activity of MMPs. So far, most studies are at a preliminary stage; however, some hydroxamate-based tracers such as the peptidomimetics [¹¹¹In]-DTPA-RP782, [99mTc]-(HYNIC-RP805)(tricine)(TPPTS), or Marimastat-ArB[¹⁸F]F₃ and the picolyl- benzenesulfonamide [¹²³I]I-HO-CGS 27023A identified specifically the enzymatic action of MMPs in animal models of various pathologies. The development of new compounds that may lead to novel tracers (e.g. modification of zinc-binding group, variation of substituents attached to the S1', S2' and S3' pockets of the MMP inhibitors) and the use of antibodies and cell penetrating peptides are also discussed. In general, preclinical studies with atherosclerosis models proved to be more successful than those with oncological models.
Insights
Radiolabeled matrix metalloproteinase inhibitors (MMPIs) offer a novel way to image proteolytic activity in diseases like atherosclerosis. Preclinical studies show promise, especially in atherosclerosis models, for non-invasive diagnostic imaging.
Area of Science:
- Biomedical Imaging
- Radiochemistry
- Molecular Biology
Background:
- Matrix metalloproteinase (MMP) dysregulation is implicated in diseases including atherosclerosis, inflammation, and cancer.
- Non-invasive in vivo imaging of MMP activity could aid in characterizing various pathological conditions.
Purpose of the Study:
- To provide an overview of radiolabeled MMP inhibitors (MMPIs) and MMP peptides for PET and SPECT imaging.
- To discuss the potential of these agents for detecting MMP proteolytic activity.
Main Methods:
- Review of existing literature on radiolabeled MMPIs and MMP peptides.
- Discussion of specific tracer examples like hydroxamate-based and picolyl-benzenesulfonamide compounds.
- Exploration of future directions including novel compound development and antibody-based tracers.
Main Results:
- Several radiolabeled MMPIs and peptides have shown the ability to detect MMP activity in animal models.
- Hydroxamate-based tracers ([¹¹¹In]-DTPA-RP782, [99mTc]-(HYNIC-RP805)(tricine)(TPPTS), Marimastat-ArB[¹⁸F]F₃) and a picolyl-benzenesulfonamide ([¹²³I]I-HO-CGS 27023A) have demonstrated specificity.
- Preclinical studies in atherosclerosis models have yielded more successful outcomes than those in oncological models.
Conclusions:
- Radiolabeled MMPIs and peptides are emerging tools for imaging MMP activity.
- Further development of novel tracers and strategies is ongoing.
- Current preclinical data suggests greater success in atherosclerosis imaging compared to cancer detection.
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