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THE QUARTERLY JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING
Rivista di Medicina Nucleare e Imaging Molecolare
A Journal on Nuclear Medicine and Molecular Imaging
Affiliated to the and to the International Research Group of Immunoscintigraphy
Indexed/Abstracted in: Current Contents/Clinical Medicine, EMBASE, PubMed/MEDLINE, Science Citation Index (SciSearch), Scopus
Impact Factor 2,413
RADIOPHARMACY AND RADIOPHARMACEUTICALS 2007 UPDATE
The Quarterly Journal of Nuclear Medicine and Molecular Imaging 2007 March;51(1):24-32
A 18F-radiolabeled analogue of CGS 27023A as a potential agent for assessment of matrix-metalloproteinase activity in vivo
Breyholz H. J. 1, Wagner S. 1, Levkau B. 2, Schober O. 1, Schäfers M. 1, 3, Kopka K. 1, 3
1 Department of Nuclear Medicine University Hospital Münster, Münster, Germany
2 Institute of Pathophysiology, Center of Internal Medicine University Hospital Essen, Essen, Germany
3 Interdisciplinary Center of Clinical Research (IZKF) Münster, Germany
Aim. The non-invasive measurement of activated matrix metalloproteinases (MMPs) in vivo, which are involved in many pathophysiological and pathological processes occurring in inflammation, cancer and atherosclerosis, is a clinical challenge. A diagnostic tool for the non-invasive detection of MMP activity in vivo is based on MMP inhibitor (MMPI) radiotracers.
Methods. We chose non-peptidyl broad-spectrum MMPI CGS 27023A 1 as a hydroxamic acid-based lead structure to design such a tracer.
Results. The radioligand HO-[123I]I-CGS 27023A was able to specifically visualize activated MMPs in vascular lesions of apolipoprotein E-deficient mice in vivo. Based upon this work the radiosynthesis of a fluorinated analogue of the MMP inhibitor CGS 27023A was developed. Its unlabeled counterpart was found to be a potent MMP inhibitor in vitro.
Conclusion. Application of this class of MMP-targeting agents in combination with molecular imaging modalities, such as positron emission tomography, may emerge as a novel clinical diagnostic tool in the management of human diseases with MMP misexpression and/or dysregulation.