Affiliation: University of Oulu
Nkizinkiko Y, Desantis J, Koivunen J, Haikarainen T, Murthy S, Sancineto L, et al
. 2-Phenylquinazolinones as dual-activity tankyrase-kinase inhibitors. Sci Rep. 2018;8:1680 pubmed publisher
..We also discovered a compound, which was able to inhibit tankyrases, CDK9 and Akt kinases with equal µM potency. ..
Haikarainen T, Murthy S, Maksimainen M, Lehtiö L. Small-Molecule Screening Assay for Mono-ADP-Ribosyltransferases. Methods Mol Biol. 2018;1813:237-244 pubmed publisher
..The assay is homogenous, robust, and cost-effective and, most importantly, applicable to mono-ADP-ribosyltransferases as well as poly-ADP-ribosyltransferases for screening of small-molecule inhibitors against the enzymes. ..
Nkizinkiko Y, Suneel Kumar B, Jeankumar V, Haikarainen T, Koivunen J, Madhuri C, et al
. Discovery of potent and selective nonplanar tankyrase inhibiting nicotinamide mimics. Bioorg Med Chem. 2015;23:4139-49 pubmed publisher
..They also inhibited Wnt/Î²-catenin pathway in a cell-based reporter assay demonstrating the potential usefulness of the identified new scaffolds for further development. ..
Murthy S, Desantis J, Verheugd P, Maksimainen M, Venkannagari H, Massari S, et al
. 4-(Phenoxy) and 4-(benzyloxy)benzamides as potent and selective inhibitors of mono-ADP-ribosyltransferase PARP10/ARTD10. Eur J Med Chem. 2018;156:93-102 pubmed publisher
Lehtiö L, Chi N, Krauss S. Tankyrases as drug targets. FEBS J. 2013;280:3576-93 pubmed publisher
..A highly potent dual-site inhibitor is also available. Within the last few years, tankyrase inhibitors have proved to be useful chemical probes and potential lead compounds, especially for specific cancers. ..
Haikarainen T, Waaler J, Ignatev A, Nkizinkiko Y, Venkannagari H, Obaji E, et al
. Development and structural analysis of adenosine site binding tankyrase inhibitors. Bioorg Med Chem Lett. 2016;26:328-333 pubmed publisher
..The structural analysis allows further rational development of this compound class as a potent and selective tankyrase inhibitor. ..
Venkannagari H, Verheugd P, Koivunen J, Haikarainen T, Obaji E, Ashok Y, et al
. Small-Molecule Chemical Probe Rescues Cells from Mono-ADP-Ribosyltransferase ARTD10/PARP10-Induced Apoptosis and Sensitizes Cancer Cells to DNA Damage. Cell Chem Biol. 2016;23:1251-1260 pubmed publisher
..Our study supports the proposed role of ARTD10 in DNA-damage repair and provides a tool compound for selective inhibition of ARTD10-mediated MARylation. ..
Haikarainen T, Schlesinger M, Obaji E, Fernández Villamil S, Lehtiö L. Structural and Biochemical Characterization of Poly-ADP-ribose Polymerase from Trypanosoma brucei. Sci Rep. 2017;7:3642 pubmed publisher
..Solution structures of activating and non-activating PARP-DNA complexes were determined with small-angle X-ray scattering revealing distinct differences in their DNA-binding modes. ..