Small-Molecule Inhibitors of the Tumor Suppressor Fhit

Lange, Sandra; Hacker, Stephan M.; Schmid, Philipp; Scheffner, Martin; Marx, Andreas

Small-Molecule Inhibitors of the Tumor Suppressor Fhit

Dateien

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Datum

2017

Open Access-Veröffentlichung

Open Access Green

Sammlungen

Chemie
Biologie

Publikationstyp

Zeitschriftenartikel

Publikationsstatus

Published

Erschienen in

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.

Fachgebiet (DDC)

540 Chemie

Zitieren

ISO 690

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.201700226

BibTex

@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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