@article{Pawar2020-02-26Compe-48520,
  year={2020},
  doi={10.1021/acscentsci.9b01170},
  title={Competitive Metabolite Profiling of Natural Products Reveals Subunit Specific Inhibitors of the 20S Proteasome},
  number={2},
  volume={6},
  issn={2374-7943},
  journal={ACS Central Science},
  pages={241--246},
  author={Pawar, Atul and Basler, Michael and Goebel, Heike and Alvarez Salinas, Gerardo Omar and Gröttrup, Marcus and Böttcher, Thomas}
}

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    <dc:contributor>Alvarez Salinas, Gerardo Omar</dc:contributor>
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    <dc:creator>Goebel, Heike</dc:creator>
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    <dcterms:abstract xml:lang="eng">We have developed a syringolin-based chemical probe and explored its utility for the profiling of metabolite extracts as potent inhibitors of the 20S proteasome. Activity-guided fractionation by competitive labeling allowed us to isolate and identify glidobactin A and C as well as luminmycin A from a Burkholderiales strain. The natural products exhibited unique subunit specificities for the proteolytic subunits of human and mouse constitutive and immunoproteasome in the lower nanomolar range. In particular, glidobactin C displayed an unprecedented β2/β5 coinhibition profile with single-digit nanomolar potency in combination with sufficiently high cell permeability. These properties render glidobactin C a promising live cell proteasome inhibitor with potent activity against human breast cancer cell lines and comparably low immunotoxicity.</dcterms:abstract>
    <dc:creator>Böttcher, Thomas</dc:creator>
    <dc:contributor>Gröttrup, Marcus</dc:contributor>
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    <dc:contributor>Basler, Michael</dc:contributor>
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    <dcterms:title>Competitive Metabolite Profiling of Natural Products Reveals Subunit Specific Inhibitors of the 20S Proteasome</dcterms:title>
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    <dc:creator>Alvarez Salinas, Gerardo Omar</dc:creator>
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    <dc:creator>Gröttrup, Marcus</dc:creator>
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