Small-Molecule Inhibitors of the Tumor Suppressor Fhit

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LANGE, Sandra, Stephan M. HACKER, Philipp SCHMID, Martin SCHEFFNER, Andreas MARX, 2017. Small-Molecule Inhibitors of the Tumor Suppressor Fhit. In: ChemBioChem. 18(17), pp. 1707-1711. ISSN 1439-4227. eISSN 1439-7633. Available under: doi: 10.1002/cbic.201700226

@article{Lange2017-09-05Small-40137, title={Small-Molecule Inhibitors of the Tumor Suppressor Fhit}, year={2017}, doi={10.1002/cbic.201700226}, number={17}, volume={18}, issn={1439-4227}, journal={ChemBioChem}, pages={1707--1711}, author={Lange, Sandra and Hacker, Stephan M. and Schmid, Philipp and Scheffner, Martin and Marx, Andreas} }

<rdf:RDF xmlns:dcterms="" xmlns:dc="" xmlns:rdf="" xmlns:bibo="" xmlns:dspace="" xmlns:foaf="" xmlns:void="" xmlns:xsd="" > <rdf:Description rdf:about=""> <dc:creator>Schmid, Philipp</dc:creator> <dspace:isPartOfCollection rdf:resource=""/> <dcterms:issued>2017-09-05</dcterms:issued> <dspace:isPartOfCollection rdf:resource=""/> <dcterms:isPartOf rdf:resource=""/> <dc:contributor>Hacker, Stephan M.</dc:contributor> <dc:creator>Marx, Andreas</dc:creator> <dcterms:rights rdf:resource=""/> <dcterms:abstract xml:lang="eng">The tumor suppressor Fhit and its substrate diadenosine triphosphate (Ap3 A) are important factors in cancer development and progression. Fhit has Ap3 A hydrolase activity and cleaves Ap3 A into adenosine monophosphate (AMP) and adenosine diphosphate (ADP); this is believed to terminate Fhit-mediated signaling. How the catalytic activity of Fhit is regulated and how the Fhit⋅Ap3 A complex might exert its growth-suppressive function remain to be discovered. Small-molecule inhibitors of the enzymatic activity of Fhit would provide valuable tools for the elucidation of its tumor-suppressive functions. Here we describe the development of a high-throughput screen for the identification of such small-molecule inhibitors of Fhit. Two clusters of inhibitors that decreased the activity of Fhit by at least 90 % were identified. Several derivatives were synthesized and exhibited in vitro IC50 values in the nanomolar range.</dcterms:abstract> <dc:creator>Lange, Sandra</dc:creator> <dc:creator>Hacker, Stephan M.</dc:creator> <dc:contributor>Lange, Sandra</dc:contributor> <bibo:uri rdf:resource=""/> <dc:contributor>Scheffner, Martin</dc:contributor> <dc:contributor>Schmid, Philipp</dc:contributor> <dc:rights>terms-of-use</dc:rights> <dcterms:hasPart rdf:resource=""/> <dcterms:available rdf:datatype="">2017-09-21T08:16:12Z</dcterms:available> <dc:creator>Scheffner, Martin</dc:creator> <dcterms:title>Small-Molecule Inhibitors of the Tumor Suppressor Fhit</dcterms:title> <dspace:hasBitstream rdf:resource=""/> <dc:date rdf:datatype="">2017-09-21T08:16:12Z</dc:date> <dc:language>eng</dc:language> <dcterms:isPartOf rdf:resource=""/> <dc:contributor>Marx, Andreas</dc:contributor> <foaf:homepage rdf:resource="http://localhost:8080/jspui"/> <void:sparqlEndpoint rdf:resource="http://localhost/fuseki/dspace/sparql"/> </rdf:Description> </rdf:RDF>

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