3 years ago

Discovery of a Highly Selective Tankyrase Inhibitor Displaying Growth Inhibition Effects against a Diverse Range of Tumor Derived Cell Lines

Discovery of a Highly Selective Tankyrase Inhibitor Displaying Growth Inhibition Effects against a Diverse Range of Tumor Derived Cell Lines
Jana Krause, R. Edward Benson, Elsa Salzer, John T. Moore, Gerard Drewes, Birgit Duempelfeld, Douglas W. Thomson, Katrin Mueller, Carsten Hopf, Christina Rau, Anne J. Wagner, John G. Emery, Marcus Bantscheff, Marcel Muelbaier, Lisa Shewchuk, Daniel Poeckel, Lars Dittus
The availability of high quality probes for specific protein targets is fundamental to the investigation of their function and their validation as therapeutic targets. We report the utilization of a dedicated chemoproteomic assay platform combining affinity enrichment technology with high-resolution protein mass spectrometry to the discovery of a novel nicotinamide isoster, the tetrazoloquinoxaline 41, a highly potent and selective tankyrase inhibitor. We also describe the use of 41 to investigate the biology of tankyrase, revealing the compound induced growth inhibition of a number of tumor derived cell lines, demonstrating the potential of tankyrase inhibitors in oncology.

Publisher URL: http://dx.doi.org/10.1021/acs.jmedchem.7b00137

DOI: 10.1021/acs.jmedchem.7b00137

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