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Molecular imaging of matrix metalloproteinases in vivo using small molecule inhibitors for SPECT and PET
S Wagner1, H-J Breyholz, A Faust
1Department of Nuclear Medicine, University Hospital Münster, Münster, Germany. stwagner@uni-muenster.de
Abstract:
Matrix metalloproteinases (MMPs) are a family of zinc- and calcium-dependent secreted or membrane anchored endopeptidases. MMPs are involved in many physiological processes but also take part in the pathophysiological mechanisms responsible for a wide range of diseases. Pathological expression and activation of MMPs are associated with cancer, atherosclerosis, stroke, arthritis, periodontal disease, multiple sclerosis and liver fibrosis. Thus, noninvasive visualisation and quantification of MMP activity in vivo are of great interest in basic research and clinical application. This can be achieved by scintigraphic molecular imaging techniques such as single photon emission computed tomography (SPECT) and positron emission tomography (PET) provided suitable radiolabelled tracers exist, e.g. radioactive inhibitors of matrix metalloproteinases (MMPIs). The approach to monitor MMP activity in vivo using radiolabelled small molecule inhibitors suitable for SPECT and PET is summarised in this review. Briefly, latest advances in scintigraphic imaging are introduced and followed by a report about the enzyme class of MMPs. The involvement of MMPs in cancer and atherosclerosis is exemplified and small molecule MMPIs are classified. Subsequently, the development of radiolabelled small molecule MMPIs, their synthesis and in vitro and in vivo evaluation is reviewed. Finally, an outlook on the clinical potential of labelled MMPIs in diagnostic algorithms is given.
Insights
This review covers radiolabeled small molecule inhibitors for imaging matrix metalloproteinase (MMP) activity using SPECT and PET. These tools offer potential for diagnosing diseases like cancer and atherosclerosis.
Area of Science:
- Biochemistry and Molecular Imaging
- Enzyme activity and disease mechanisms
Background:
- Matrix metalloproteinases (MMPs) are crucial enzymes in physiological processes.
- Dysregulated MMP activity is implicated in various diseases, including cancer, atherosclerosis, and arthritis.
- Noninvasive in vivo monitoring of MMP activity is essential for research and clinical applications.
Purpose of the Study:
- To review the development and application of radiolabeled small molecule inhibitors for imaging MMP activity.
- To highlight the potential of these tracers in scintigraphic molecular imaging techniques like SPECT and PET.
- To provide an outlook on the clinical utility of labeled MMP inhibitors in diagnostic strategies.
Main Methods:
- Review of recent advances in scintigraphic imaging techniques.
- Classification and discussion of small molecule MMP inhibitors (MMPIs).
- Examination of the synthesis and in vitro/in vivo evaluation of radiolabeled MMPIs.
Main Results:
- Radiolabeled small molecule MMPIs are viable tracers for SPECT and PET imaging of MMP activity.
- MMP involvement in cancer and atherosclerosis is well-established, making them key targets for imaging.
- The development of these tracers facilitates in vivo quantification and visualization of MMPs.
Conclusions:
- Radiolabeled MMPIs represent a promising approach for noninvasive assessment of MMP activity in vivo.
- These imaging agents hold significant potential for improving diagnostic algorithms in various pathological conditions.
- Further clinical translation of labeled MMPIs is anticipated for enhanced disease management.
