Exploration of the nicotinamide-binding site of the tankyrases, identifying 3-arylisoquinolin-1-ones as potent and selective inhibitors in vitro

[Display omitted] Tankyrases-1 and -2 (TNKS-1 and TNKS-2) have three cellular roles which make them important targets in cancer. Using NAD+ as a substrate, they poly(ADP-ribosyl)ate TRF1 (regulating lengths of telomeres), NuMA (facilitating mitosis) and axin (in wnt/β-catenin signalling). Using mole...

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Veröffentlicht in:Bioorganic & medicinal chemistry 2015-09, Vol.23 (17), p.5891-5908
Hauptverfasser: Paine, Helen A., Nathubhai, Amit, Woon, Esther C.Y., Sunderland, Peter T., Wood, Pauline J., Mahon, Mary F., Lloyd, Matthew D., Thompson, Andrew S., Haikarainen, Teemu, Narwal, Mohit, Lehtiö, Lari, Threadgill, Michael D.
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Sprache:eng
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