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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{
  "DOI": "10.1021/acs.jmedchem.6b01284", 
  "container_title": "J. Med. Chem.", 
  "title": "Radiolabeled Selective Matrix Metalloproteinase 13 (MMP-13) Inhibitors: (Radio)Syntheses and in Vitro and First in Vivo Evaluation.", 
  "issued": {
    "date-parts": [
      [
        2017, 
        1, 
        12
      ]
    ]
  }, 
  "abstract": "<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>", 
  "author": [
    {
      "family": "Hugenberg, Verena"
    }, 
    {
      "family": "Wagner, Stefan"
    }, 
    {
      "family": "Kopka, Klaus"
    }, 
    {
      "family": "Sch\u00e4fers, Michael"
    }, 
    {
      "family": "Schuit, Robert C"
    }, 
    {
      "family": "Windhorst, Albert D"
    }, 
    {
      "family": "Hermann, Sven"
    }
  ], 
  "page": "307\u2013321", 
  "volume": "60", 
  "type": "article-journal", 
  "issue": "1", 
  "id": "478813"
}
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