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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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  <identifier identifierType="URL">https://zenodo.org/record/478813</identifier>
  <creators>
    <creator>
      <creatorName>Hugenberg, Verena</creatorName>
      <givenName>Verena</givenName>
      <familyName>Hugenberg</familyName>
      <affiliation>European Institute for Molecular Imaging, University of Münster, Waldeyerstr. 15, D-48149 Münster, Germany and Department of Nuclear Medicine, University Hospital Münster, Albert-Schweitzer-Campus 1, Building A1, D-48149 Münster, Germany</affiliation>
    </creator>
    <creator>
      <creatorName>Wagner, Stefan</creatorName>
      <givenName>Stefan</givenName>
      <familyName>Wagner</familyName>
      <affiliation>Department of Nuclear Medicine, University Hospital Münster, Albert-Schweitzer-Campus 1, Building A1, D-48149 Münster, Germany</affiliation>
    </creator>
    <creator>
      <creatorName>Kopka, Klaus</creatorName>
      <givenName>Klaus</givenName>
      <familyName>Kopka</familyName>
      <affiliation>Department of Nuclear Medicine, University Hospital Münster, Albert-Schweitzer-Campus 1, Building A1, D-48149 Münster, Germany</affiliation>
    </creator>
    <creator>
      <creatorName>Schäfers, Michael</creatorName>
      <givenName>Michael</givenName>
      <familyName>Schäfers</familyName>
      <affiliation>European Institute for Molecular Imaging, University of Münster, Waldeyerstr. 15, D-48149 Münster, Germany; Department of Nuclear Medicine, University Hospital Münster, Albert-Schweitzer-Campus 1, Building A1, D-48149 Münster, Germany and DFG EXC 1003 Cluster of Excellence 'Cells in Motion', University of Münster, D-48149 Münster, Germany</affiliation>
    </creator>
    <creator>
      <creatorName>Schuit, Robert C</creatorName>
      <givenName>Robert C</givenName>
      <familyName>Schuit</familyName>
      <affiliation>Department of Radiology &amp; Nuclear Medicine, VU University Medical Center Amsterdam, De Boelelaan 1117, 1081 HZ Amsterdam, The Netherlands</affiliation>
    </creator>
    <creator>
      <creatorName>Windhorst, Albert D</creatorName>
      <givenName>Albert D</givenName>
      <familyName>Windhorst</familyName>
      <affiliation>Department of Radiology &amp; Nuclear Medicine, VU University Medical Center Amsterdam, De Boelelaan 1117, 1081 HZ Amsterdam, The Netherlands</affiliation>
    </creator>
    <creator>
      <creatorName>Hermann, Sven</creatorName>
      <givenName>Sven</givenName>
      <familyName>Hermann</familyName>
      <affiliation>European Institute for Molecular Imaging, University of Münster, Waldeyerstr. 15, D-48149 Münster, Germany and DFG EXC 1003 Cluster of Excellence 'Cells in Motion', University of Münster, D-48149 Münster, Germany</affiliation>
    </creator>
  </creators>
  <titles>
    <title>Radiolabeled Selective Matrix Metalloproteinase 13 (MMP-13) Inhibitors: (Radio)Syntheses and in Vitro and First in Vivo Evaluation.</title>
  </titles>
  <publisher>Zenodo</publisher>
  <publicationYear>2017</publicationYear>
  <subjects>
    <subject>Selective matrix metalloproteinase inhibitors</subject>
    <subject>selective MMP-13 inhibitors</subject>
    <subject>positron emission tomography</subject>
    <subject>radiotracer</subject>
  </subjects>
  <dates>
    <date dateType="Issued">2017-01-12</date>
  </dates>
  <resourceType resourceTypeGeneral="Text">Journal article</resourceType>
  <alternateIdentifiers>
    <alternateIdentifier alternateIdentifierType="url">https://zenodo.org/record/478813</alternateIdentifier>
  </alternateIdentifiers>
  <relatedIdentifiers>
    <relatedIdentifier relatedIdentifierType="DOI" relationType="IsIdenticalTo">10.1021/acs.jmedchem.6b01284</relatedIdentifier>
    <relatedIdentifier relatedIdentifierType="URL" relationType="IsPartOf">https://zenodo.org/communities/ecfunded</relatedIdentifier>
    <relatedIdentifier relatedIdentifierType="URL" relationType="IsPartOf">https://zenodo.org/communities/inmind</relatedIdentifier>
  </relatedIdentifiers>
  <rightsList>
    <rights rightsURI="http://creativecommons.org/licenses/by/4.0/legalcode">Creative Commons Attribution 4.0 International</rights>
    <rights rightsURI="info:eu-repo/semantics/openAccess">Open Access</rights>
  </rightsList>
  <descriptions>
    <description descriptionType="Abstract">&lt;p&gt;The noninvasive imaging of MMP activity in vivo could have a&lt;br&gt;
high impact in basic research as well as in clinical applications. This approach&lt;br&gt;
can be established using radiolabeled MMP inhibitors (MMPIs) as tracers for&lt;br&gt;
the detection of activated MMPs by means of PET. However, the complexity of&lt;br&gt;
diseases associated with dysregulated MMP expression necessitates the imaging&lt;br&gt;
of distinct MMPs or MMP subgroups to distinguish their individual role in&lt;br&gt;
specific diseases. To this end, selective and potent MMP-13 inhibitors based on&lt;br&gt;
a N,N′-bis(benzyl)pyrimidine-4,6-dicarboxamide core have been synthesized&lt;br&gt;
and successfully radiolabeled with carbon-11, fluorine-18, and gallium-68.&lt;br&gt;
Selected radiolabeled candidates were evaluated in vitro and in vivo regarding&lt;br&gt;
their pharmacokinetic properties and metabolic stability.&lt;/p&gt;</description>
  </descriptions>
  <fundingReferences>
    <fundingReference>
      <funderName>European Commission</funderName>
      <funderIdentifier funderIdentifierType="Crossref Funder ID">10.13039/501100000780</funderIdentifier>
      <awardNumber awardURI="info:eu-repo/grantAgreement/EC/FP7/278850/">278850</awardNumber>
      <awardTitle>Imaging of Neuroinflammation in Neurodegenerative Diseases</awardTitle>
    </fundingReference>
  </fundingReferences>
</resource>
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