Publikation: Small-Molecule Inhibitors of the Tumor Suppressor Fhit
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2017
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ChemBioChem. 2017, 18(17), pp. 1707-1711. ISSN 1439-4227. eISSN 1439-7633. Available under: doi: 10.1002/cbic.201700226
Zusammenfassung
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.
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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. 2017, 18(17), pp. 1707-1711. ISSN 1439-4227. eISSN 1439-7633. Available under: doi: 10.1002/cbic.201700226BibTex
@article{Lange2017-09-05Small-40137,
year={2017},
doi={10.1002/cbic.201700226},
title={Small-Molecule Inhibitors of the Tumor Suppressor Fhit},
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}
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<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>
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