KOPS - The Institutional Repository of the University of Konstanz

Competitive Metabolite Profiling of Natural Products Reveals Subunit Specific Inhibitors of the 20S Proteasome

Competitive Metabolite Profiling of Natural Products Reveals Subunit Specific Inhibitors of the 20S Proteasome

Cite This

Files in this item

Checksum: MD5:c3fac2b2c93e71c5f9e001221239c7a1

PAWAR, Atul, Michael BASLER, Heike GOEBEL, Gerardo Omar ALVAREZ SALINAS, Marcus GROETTRUP, Thomas BÖTTCHER, 2020. Competitive Metabolite Profiling of Natural Products Reveals Subunit Specific Inhibitors of the 20S Proteasome. In: ACS Central Science. American Chemical Society (ACS). 6(2), pp. 241-246. ISSN 2374-7943. eISSN 2374-7951. Available under: doi: 10.1021/acscentsci.9b01170

@article{Pawar2020-02-26Compe-48520, title={Competitive Metabolite Profiling of Natural Products Reveals Subunit Specific Inhibitors of the 20S Proteasome}, year={2020}, doi={10.1021/acscentsci.9b01170}, 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 Groettrup, Marcus and Böttcher, Thomas} }

<rdf:RDF xmlns:dcterms="http://purl.org/dc/terms/" xmlns:dc="http://purl.org/dc/elements/1.1/" xmlns:rdf="http://www.w3.org/1999/02/22-rdf-syntax-ns#" xmlns:bibo="http://purl.org/ontology/bibo/" xmlns:dspace="http://digital-repositories.org/ontologies/dspace/0.1.0#" xmlns:foaf="http://xmlns.com/foaf/0.1/" xmlns:void="http://rdfs.org/ns/void#" xmlns:xsd="http://www.w3.org/2001/XMLSchema#" > <rdf:Description rdf:about="https://kops.uni-konstanz.de/rdf/resource/123456789/48520"> <dc:creator>Goebel, Heike</dc:creator> <dc:contributor>Goebel, Heike</dc:contributor> <dc:contributor>Böttcher, Thomas</dc:contributor> <dc:contributor>Groettrup, Marcus</dc:contributor> <foaf:homepage rdf:resource="http://localhost:8080/jspui"/> <dc:language>eng</dc:language> <dcterms:available rdf:datatype="http://www.w3.org/2001/XMLSchema#dateTime">2020-02-05T10:56:07Z</dcterms:available> <void:sparqlEndpoint rdf:resource="http://localhost/fuseki/dspace/sparql"/> <dspace:isPartOfCollection rdf:resource="https://kops.uni-konstanz.de/rdf/resource/123456789/28"/> <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> <dspace:isPartOfCollection rdf:resource="https://kops.uni-konstanz.de/rdf/resource/123456789/29"/> <dc:date rdf:datatype="http://www.w3.org/2001/XMLSchema#dateTime">2020-02-05T10:56:07Z</dc:date> <dcterms:rights rdf:resource="https://rightsstatements.org/page/InC/1.0/"/> <dc:contributor>Basler, Michael</dc:contributor> <dc:creator>Groettrup, Marcus</dc:creator> <dc:contributor>Pawar, Atul</dc:contributor> <dcterms:hasPart rdf:resource="https://kops.uni-konstanz.de/bitstream/123456789/48520/1/Pawar_2-2erpbpd9qo5z1.pdf"/> <dcterms:isPartOf rdf:resource="https://kops.uni-konstanz.de/rdf/resource/123456789/29"/> <dspace:hasBitstream rdf:resource="https://kops.uni-konstanz.de/bitstream/123456789/48520/1/Pawar_2-2erpbpd9qo5z1.pdf"/> <dcterms:title>Competitive Metabolite Profiling of Natural Products Reveals Subunit Specific Inhibitors of the 20S Proteasome</dcterms:title> <dcterms:issued>2020-02-26</dcterms:issued> <dc:contributor>Alvarez Salinas, Gerardo Omar</dc:contributor> <bibo:uri rdf:resource="https://kops.uni-konstanz.de/handle/123456789/48520"/> <dc:rights>terms-of-use</dc:rights> <dc:creator>Alvarez Salinas, Gerardo Omar</dc:creator> <dcterms:isPartOf rdf:resource="https://kops.uni-konstanz.de/rdf/resource/123456789/28"/> <dc:creator>Pawar, Atul</dc:creator> <dc:creator>Böttcher, Thomas</dc:creator> <dc:creator>Basler, Michael</dc:creator> </rdf:Description> </rdf:RDF>

Downloads since Feb 5, 2020 (Information about access statistics)

Pawar_2-2erpbpd9qo5z1.pdf 21

This item appears in the following Collection(s)

Search KOPS


Browse

My Account