Journal article Open Access

Radiolabeled Selective Matrix Metalloproteinase 13 (MMP-13) Inhibitors: (Radio)Syntheses and in Vitro and First in Vivo Evaluation.

Hugenberg, Verena; Wagner, Stefan; Kopka, Klaus; Schäfers, Michael; Schuit, Robert C; Windhorst, Albert D; Hermann, Sven


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    "embargo_date": "2018-01-12", 
    "doi": "10.1021/acs.jmedchem.6b01284", 
    "description": "<p>The noninvasive imaging of MMP activity in vivo could have a<br>\nhigh impact in basic research as well as in clinical applications. This approach<br>\ncan be established using radiolabeled MMP inhibitors (MMPIs) as tracers for<br>\nthe detection of activated MMPs by means of PET. However, the complexity of<br>\ndiseases associated with dysregulated MMP expression necessitates the imaging<br>\nof distinct MMPs or MMP subgroups to distinguish their individual role in<br>\nspecific diseases. To this end, selective and potent MMP-13 inhibitors based on<br>\na N,N\u2032-bis(benzyl)pyrimidine-4,6-dicarboxamide core have been synthesized<br>\nand successfully radiolabeled with carbon-11, fluorine-18, and gallium-68.<br>\nSelected radiolabeled candidates were evaluated in vitro and in vivo regarding<br>\ntheir pharmacokinetic properties and metabolic stability.</p>", 
    "license": {
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    "title": "Radiolabeled Selective Matrix Metalloproteinase 13 (MMP-13) Inhibitors: (Radio)Syntheses and in Vitro and First in Vivo Evaluation.", 
    "journal": {
      "volume": "60", 
      "issue": "1", 
      "pages": "307\u2013321", 
      "title": "J. Med. Chem."
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    "keywords": [
      "Selective matrix metalloproteinase inhibitors", 
      "selective MMP-13 inhibitors", 
      "positron emission tomography", 
      "radiotracer"
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    "publication_date": "2017-01-12", 
    "creators": [
      {
        "affiliation": "European Institute for Molecular Imaging, University of M\u00fcnster, Waldeyerstr. 15, D-48149 M\u00fcnster, Germany and Department of Nuclear Medicine, University Hospital M\u00fcnster, Albert-Schweitzer-Campus 1, Building A1, D-48149 M\u00fcnster, Germany", 
        "name": "Hugenberg, Verena"
      }, 
      {
        "affiliation": "Department of Nuclear Medicine, University Hospital M\u00fcnster, Albert-Schweitzer-Campus 1, Building A1, D-48149 M\u00fcnster, Germany", 
        "name": "Wagner, Stefan"
      }, 
      {
        "affiliation": "Department of Nuclear Medicine, University Hospital M\u00fcnster, Albert-Schweitzer-Campus 1, Building A1, D-48149 M\u00fcnster, Germany", 
        "name": "Kopka, Klaus"
      }, 
      {
        "affiliation": "European Institute for Molecular Imaging, University of M\u00fcnster, Waldeyerstr. 15, D-48149 M\u00fcnster, Germany; Department of Nuclear Medicine, University Hospital M\u00fcnster, Albert-Schweitzer-Campus 1, Building A1, D-48149 M\u00fcnster, Germany and DFG EXC 1003 Cluster of Excellence 'Cells in Motion', University of M\u00fcnster, D-48149 M\u00fcnster, Germany", 
        "name": "Sch\u00e4fers, Michael"
      }, 
      {
        "affiliation": "Department of Radiology & Nuclear Medicine, VU University Medical Center Amsterdam, De Boelelaan 1117, 1081 HZ Amsterdam, The Netherlands", 
        "name": "Schuit, Robert C"
      }, 
      {
        "affiliation": "Department of Radiology & Nuclear Medicine, VU University Medical Center Amsterdam, De Boelelaan 1117, 1081 HZ Amsterdam, The Netherlands", 
        "name": "Windhorst, Albert D"
      }, 
      {
        "affiliation": "European Institute for Molecular Imaging, University of M\u00fcnster, Waldeyerstr. 15, D-48149 M\u00fcnster, Germany and DFG EXC 1003 Cluster of Excellence 'Cells in Motion', University of M\u00fcnster, D-48149 M\u00fcnster, Germany", 
        "name": "Hermann, Sven"
      }
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      "title": "Journal article"
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