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


MARC21 XML Export

<?xml version='1.0' encoding='UTF-8'?>
<record xmlns="http://www.loc.gov/MARC21/slim">
  <leader>00000nam##2200000uu#4500</leader>
  <datafield tag="942" ind1=" " ind2=" ">
    <subfield code="a">2018-01-12</subfield>
  </datafield>
  <datafield tag="653" ind1=" " ind2=" ">
    <subfield code="a">Selective matrix metalloproteinase inhibitors</subfield>
  </datafield>
  <datafield tag="653" ind1=" " ind2=" ">
    <subfield code="a">selective MMP-13 inhibitors</subfield>
  </datafield>
  <datafield tag="653" ind1=" " ind2=" ">
    <subfield code="a">positron emission tomography</subfield>
  </datafield>
  <datafield tag="653" ind1=" " ind2=" ">
    <subfield code="a">radiotracer</subfield>
  </datafield>
  <controlfield tag="005">20191104071249.0</controlfield>
  <controlfield tag="001">478813</controlfield>
  <datafield tag="700" ind1=" " ind2=" ">
    <subfield code="u">Department of Nuclear Medicine, University Hospital Münster, Albert-Schweitzer-Campus 1, Building A1, D-48149 Münster, Germany</subfield>
    <subfield code="a">Wagner, Stefan</subfield>
  </datafield>
  <datafield tag="700" ind1=" " ind2=" ">
    <subfield code="u">Department of Nuclear Medicine, University Hospital Münster, Albert-Schweitzer-Campus 1, Building A1, D-48149 Münster, Germany</subfield>
    <subfield code="a">Kopka, Klaus</subfield>
  </datafield>
  <datafield tag="700" ind1=" " ind2=" ">
    <subfield code="u">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</subfield>
    <subfield code="a">Schäfers, Michael</subfield>
  </datafield>
  <datafield tag="700" ind1=" " ind2=" ">
    <subfield code="u">Department of Radiology &amp; Nuclear Medicine, VU University Medical Center Amsterdam, De Boelelaan 1117, 1081 HZ Amsterdam, The Netherlands</subfield>
    <subfield code="a">Schuit, Robert C</subfield>
  </datafield>
  <datafield tag="700" ind1=" " ind2=" ">
    <subfield code="u">Department of Radiology &amp; Nuclear Medicine, VU University Medical Center Amsterdam, De Boelelaan 1117, 1081 HZ Amsterdam, The Netherlands</subfield>
    <subfield code="a">Windhorst, Albert D</subfield>
  </datafield>
  <datafield tag="700" ind1=" " ind2=" ">
    <subfield code="u">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</subfield>
    <subfield code="a">Hermann, Sven</subfield>
  </datafield>
  <datafield tag="856" ind1="4" ind2=" ">
    <subfield code="s">1961061</subfield>
    <subfield code="z">md5:6a97ceea5235860f98980996dca53ea3</subfield>
    <subfield code="u">https://zenodo.org/record/478813/files/Hugenberg_JMedChem_2017-P01-AAM.pdf</subfield>
  </datafield>
  <datafield tag="542" ind1=" " ind2=" ">
    <subfield code="l">open</subfield>
  </datafield>
  <datafield tag="260" ind1=" " ind2=" ">
    <subfield code="c">2017-01-12</subfield>
  </datafield>
  <datafield tag="909" ind1="C" ind2="O">
    <subfield code="p">user-ecfunded</subfield>
    <subfield code="p">user-inmind</subfield>
    <subfield code="o">oai:zenodo.org:478813</subfield>
  </datafield>
  <datafield tag="909" ind1="C" ind2="4">
    <subfield code="c">307–321</subfield>
    <subfield code="n">1</subfield>
    <subfield code="p">J. Med. Chem.</subfield>
    <subfield code="v">60</subfield>
  </datafield>
  <datafield tag="100" ind1=" " ind2=" ">
    <subfield code="u">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</subfield>
    <subfield code="a">Hugenberg, Verena</subfield>
  </datafield>
  <datafield tag="245" ind1=" " ind2=" ">
    <subfield code="a">Radiolabeled Selective Matrix Metalloproteinase 13 (MMP-13) Inhibitors: (Radio)Syntheses and in Vitro and First in Vivo Evaluation.</subfield>
  </datafield>
  <datafield tag="980" ind1=" " ind2=" ">
    <subfield code="a">user-ecfunded</subfield>
  </datafield>
  <datafield tag="980" ind1=" " ind2=" ">
    <subfield code="a">user-inmind</subfield>
  </datafield>
  <datafield tag="536" ind1=" " ind2=" ">
    <subfield code="c">278850</subfield>
    <subfield code="a">Imaging of Neuroinflammation in Neurodegenerative Diseases</subfield>
  </datafield>
  <datafield tag="540" ind1=" " ind2=" ">
    <subfield code="u">http://creativecommons.org/licenses/by/4.0/legalcode</subfield>
    <subfield code="a">Creative Commons Attribution 4.0 International</subfield>
  </datafield>
  <datafield tag="650" ind1="1" ind2="7">
    <subfield code="a">cc-by</subfield>
    <subfield code="2">opendefinition.org</subfield>
  </datafield>
  <datafield tag="520" ind1=" " ind2=" ">
    <subfield code="a">&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;</subfield>
  </datafield>
  <datafield tag="024" ind1=" " ind2=" ">
    <subfield code="a">10.1021/acs.jmedchem.6b01284</subfield>
    <subfield code="2">doi</subfield>
  </datafield>
  <datafield tag="980" ind1=" " ind2=" ">
    <subfield code="a">publication</subfield>
    <subfield code="b">article</subfield>
  </datafield>
</record>
12
60
views
downloads
Views 12
Downloads 60
Data volume 117.7 MB
Unique views 12
Unique downloads 58

Share

Cite as