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Exploration of the nicotinamide-binding site of the tankyrases, identifying 3-arylisoquinolin-1-ones as potent and selective inhibitors in vitro.
Paine HA, Nathubhai A, Woon EC, Sunderland PT, Wood PJ, Mahon MF, Lloyd MD, Thompson AS, Haikarainen T, Narwal M, Lehtiö L, Threadgill MD. Paine HA, et al. Among authors: haikarainen t. Bioorg Med Chem. 2015 Sep 1;23(17):5891-908. doi: 10.1016/j.bmc.2015.06.061. Epub 2015 Jul 2. Bioorg Med Chem. 2015. PMID: 26189030
Highly Potent and Isoform Selective Dual Site Binding Tankyrase/Wnt Signaling Inhibitors That Increase Cellular Glucose Uptake and Have Antiproliferative Activity.
Nathubhai A, Haikarainen T, Koivunen J, Murthy S, Koumanov F, Lloyd MD, Holman GD, Pihlajaniemi T, Tosh D, Lehtiö L, Threadgill MD. Nathubhai A, et al. Among authors: haikarainen t. J Med Chem. 2017 Jan 26;60(2):814-820. doi: 10.1021/acs.jmedchem.6b01574. Epub 2017 Jan 9. J Med Chem. 2017. PMID: 27983846 Free article.
47 results