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J Med Chem. 2017 Jul 13;60(13):5455-5471. doi: 10.1021/acs.jmedchem.7b00137. Epub 2017 Jun 27.

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

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Cellzome GmbH, A GlaxoSmithKline Company , Meyerhofstra├če 1, 69117 Heidelberg, Germany.
GlaxoSmithKline , Research Triangle Park, 5 Moore Drive, North Carolina 27709, United States.
Protein, Cellular & Structural Sciences, GlaxoSmithKline , 1250 South Collegeville Road, Upper Providence, Pennsylvania 19426, United States.
Virtual Proof of Concept DPU, GlaxoSmithKline , 709 Swedeland Road, King of Prussia, Pennsylvania 19406, United States.


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.

[Indexed for MEDLINE]

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