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Nitazoxanide and related thiazolides induce cell death in cancer cells by targeting the 20S proteasome with novel binding modes

Nitazoxanide and related thiazolides induce cell death in cancer cells by targeting the 20S proteasome with novel binding modes

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LÜ, Zirui, Xiaona LI, Kebin LI, Paola RIPANI, Xiaomeng SHI, Fengrong XU, Mopei WANG, Thomas BRUNNER, Ping XU, Yan NIU, 2022. Nitazoxanide and related thiazolides induce cell death in cancer cells by targeting the 20S proteasome with novel binding modes. In: Biochemical pharmacology. Elsevier. 197, 114913. eISSN 1873-2968. Available under: doi: 10.1016/j.bcp.2022.114913

@article{Lu2022-01-12Nitaz-56364, title={Nitazoxanide and related thiazolides induce cell death in cancer cells by targeting the 20S proteasome with novel binding modes}, year={2022}, doi={10.1016/j.bcp.2022.114913}, volume={197}, journal={Biochemical pharmacology}, author={Lü, Zirui and Li, Xiaona and Li, Kebin and Ripani, Paola and Shi, Xiaomeng and Xu, Fengrong and Wang, Mopei and Brunner, Thomas and Xu, Ping and Niu, Yan}, note={Article Number: 114913} }

<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/123456789/56364"> <dc:contributor>Brunner, Thomas</dc:contributor> <dc:contributor>Ripani, Paola</dc:contributor> <dc:contributor>Wang, Mopei</dc:contributor> <dc:contributor>Xu, Fengrong</dc:contributor> <dc:contributor>Niu, Yan</dc:contributor> <dc:creator>Xu, Fengrong</dc:creator> <bibo:uri rdf:resource="https://kops.uni-konstanz.de/handle/123456789/56364"/> <dcterms:abstract xml:lang="eng">Nitazoxanide and related thiazolides are a novel class of anti-infectious agents against protozoan parasites, bacteria and viruses. In recent years, it is demonstrated that thiazolides can also induce cell cycle arrest and apoptotic cell death in cancer cells. Due to their fast proliferating nature, cancer cells highly depend on the proteasome system to remove aberrant proteins. Many of these aberrant proteins are regulators of cell cycle progression and apoptosis, such as the cyclins, BCL2 family members and nuclear factor of κB (NF-κB). Here, we demonstrate at both molecular and cellular levels that the 20S proteasome is a direct target of NTZ and related thiazolides. By concurrently inhibiting the multiple catalytic subunits of 20S proteasome, NTZ promotes cell cycle arrest and triggers cell death in colon cancer cells, either directly or as a sensitizer to other anti-tumor agents, especially doxorubicin. We further show that the binding mode of NTZ in the β5 subunit of the 20S proteasome is different from that of bortezomib and other existing proteasome inhibitors. These findings provide new insights in the design of novel small molecular proteasome inhibitors as anti-tumor agents suitable for solid tumor treatment in an oral dosing form.</dcterms:abstract> <dcterms:rights rdf:resource="https://rightsstatements.org/page/InC/1.0/"/> <dc:contributor>Lü, Zirui</dc:contributor> <dc:creator>Shi, Xiaomeng</dc:creator> <dc:creator>Wang, Mopei</dc:creator> <dc:language>eng</dc:language> <dc:contributor>Shi, Xiaomeng</dc:contributor> <dspace:isPartOfCollection rdf:resource="https://kops.uni-konstanz.de/rdf/resource/123456789/28"/> <dc:creator>Li, Xiaona</dc:creator> <dc:creator>Brunner, Thomas</dc:creator> <dcterms:issued>2022-01-12</dcterms:issued> <dcterms:isPartOf rdf:resource="https://kops.uni-konstanz.de/rdf/resource/123456789/28"/> <dcterms:available rdf:datatype="http://www.w3.org/2001/XMLSchema#dateTime">2022-01-26T11:03:46Z</dcterms:available> <dcterms:title>Nitazoxanide and related thiazolides induce cell death in cancer cells by targeting the 20S proteasome with novel binding modes</dcterms:title> <dc:date rdf:datatype="http://www.w3.org/2001/XMLSchema#dateTime">2022-01-26T11:03:46Z</dc:date> <dc:creator>Xu, Ping</dc:creator> <dc:creator>Niu, Yan</dc:creator> <dc:rights>terms-of-use</dc:rights> <dc:contributor>Li, Xiaona</dc:contributor> <dc:creator>Lü, Zirui</dc:creator> <dc:creator>Li, Kebin</dc:creator> <dc:contributor>Li, Kebin</dc:contributor> <foaf:homepage rdf:resource="http://localhost:8080/jspui"/> <dc:contributor>Xu, Ping</dc:contributor> <void:sparqlEndpoint rdf:resource="http://localhost/fuseki/dspace/sparql"/> <dc:creator>Ripani, Paola</dc:creator> </rdf:Description> </rdf:RDF>

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