Publications by Jo Waaler

25 publications found

Publications 2025

1. Bosetti C, Kampasis D, Brinch SA, Galera-Prat A, Karelou M, Dhakar SS, Alaviuhkola J, Waaler J, Lehtiö L, Kostakis IK (2025)
   Substitutions at the C-8 position of quinazolin-4-ones improve the potency of nicotinamide site binding tankyrase inhibitors
   Eur J Med Chem, 288, 117397
   DOI 10.1016/j.ejmech.2025.117397, PubMed 39983556
2. Sowa ST, Kücükdisli M, Mostinski Y, Schaller DA, Vinagreiro CS, Cirillo D, Bosetti C, Brinch SA, van Laar K, Wegert A, Leenders RGG, Krauss S, Waaler J, Volkamer A, Lehtiö L, Nazaré M (2025)
   Deconstruction of Dual-Site Tankyrase Inhibitors Provides Insights into Binding Energetics and Suggests Critical Hotspots for Ligand Optimization
   J Med Chem, 68 (7), 7263-7279
   DOI 10.1021/acs.jmedchem.4c02845, PubMed 40134122

Publications 2023

1. Tse J, O'Keefe R, Rigopolous A, Carli ALE, Waaler J, Krauss S, Ernst M, Buchert M (2023)
   A Mouse Model for the Rapid and Binomial Assessment of Putative WNT/β-Catenin Signalling Inhibitors
   Biomedicines, 11 (10)
   DOI 10.3390/biomedicines11102719, PubMed 37893093

Publications 2022

1. Brinch SA, Amundsen-Isaksen E, Espada S, Hammarström C, Aizenshtadt A, Olsen PA, Holmen L, Høyem M, Scholz H, Grødeland G, Sowa ST, Galera-Prat A, Lehtiö L, Meerts IATM, Leenders RGG, Wegert A, Krauss S, Waaler J (2022)
   The Tankyrase Inhibitor OM-153 Demonstrates Antitumor Efficacy and a Therapeutic Window in Mouse Models
   Cancer Res Commun, 2 (4), 233-245
   DOI 10.1158/2767-9764.CRC-22-0027, PubMed 36873622

Publications 2021

1. Leenders RGG, Brinch SA, Sowa ST, Amundsen-Isaksen E, Galera-Prat A, Murthy S, Aertssen S, Smits JN, Nieczypor P, Damen E, Wegert A, Nazaré M, Lehtiö L, Waaler J, Krauss S (2021)
   Development of a 1,2,4-Triazole-Based Lead Tankyrase Inhibitor: Part II
   J Med Chem, 64 (24), 17936-17949
   DOI 10.1021/acs.jmedchem.1c01264, PubMed 34878777
2. Mygland L, Brinch SA, Strand MF, Olsen PA, Aizenshtadt A, Lund K, Solberg NT, Lycke M, Thorvaldsen TE, Espada S, Misaghian D, Page CM, Agafonov O, Nygård S, Chi NW, Lin E, Tan J, Yu Y, Costa M, Krauss S, Waaler J (2021)
   Identification of response signatures for tankyrase inhibitor treatment in tumor cell lines
   iScience, 24 (7), 102807
   DOI 10.1016/j.isci.2021.102807, PubMed 34337362

Publications 2020

1. Kierulf-Vieira KS, Sandberg CJ, Waaler J, Lund K, Skaga E, Saberniak BM, Panagopoulos I, Brandal P, Krauss S, Langmoen IA, Vik-Mo EO (2020)
   A Small-Molecule Tankyrase Inhibitor Reduces Glioma Stem Cell Proliferation and Sphere Formation
   Cancers (Basel), 12 (6)
   DOI 10.3390/cancers12061630, PubMed 32575464
2. Lien VT, Kristiansen MK, Pettersen S, Haugen MH, Krauss S, Olberg DE, Waaler J, Klaveness J (2020)
   Correction: Towards dual inhibitors of the MET kinase and WNT signaling pathway; design, synthesis and biological evaluation
   RSC Adv, 10 (9), 4927
   DOI 10.1039/d0ra90007a, PubMed 35503286
3. Wang H, Kuusela S, Rinnankoski-Tuikka R, Dumont V, Bouslama R, Ramadan UA, Waaler J, Linden AM, Chi NW, Krauss S, Pirinen E, Lehtonen S (2020)
   Tankyrase inhibition ameliorates lipid disorder via suppression of PGC-1α PARylation in db/db mice
   Int J Obes (Lond), 44 (8), 1691-1702
   DOI 10.1038/s41366-020-0573-z, PubMed 32317752
4. Waaler J, Leenders RGG, Sowa ST, Alam Brinch S, Lycke M, Nieczypor P, Aertssen S, Murthy S, Galera-Prat A, Damen E, Wegert A, Nazaré M, Lehtiö L, Krauss S (2020)
   Preclinical Lead Optimization of a 1,2,4-Triazole Based Tankyrase Inhibitor
   J Med Chem, 63 (13), 6834-6846
   DOI 10.1021/acs.jmedchem.0c00208, PubMed 32511917
5. Waaler J, Mygland L, Tveita A, Strand MF, Solberg NT, Olsen PA, Aizenshtadt A, Fauskanger M, Lund K, Brinch SA, Lycke M, Dybing E, Nygaard V, Bøe SL, Heintz KM, Hovig E, Hammarström C, Corthay A, Krauss S (2020)
   Tankyrase inhibition sensitizes melanoma to PD-1 immune checkpoint blockade in syngeneic mouse models
   Commun Biol, 3 (1), 196
   DOI 10.1038/s42003-020-0916-2, PubMed 32332858

Publications 2019

1. Lien VT, Kristiansen MK, Pettersen S, Haugen MH, Olberg DE, Waaler J, Klaveness J (2019)
   Towards dual inhibitors of the MET kinase and WNT signaling pathway; design, synthesis and biological evaluation
   RSC Adv, 9 (63), 37092-37100
   DOI 10.1039/c9ra08954c, PubMed 35539091

Publications 2018

1. Norum JH, Skarpen E, Brech A, Kuiper R, Waaler J, Krauss S, Sørlie T (2018)
   The tankyrase inhibitor G007-LK inhibits small intestine LGR5⁺ stem cell proliferation without altering tissue morphology
   Biol Res, 51 (1), 3
   DOI 10.1186/s40659-017-0151-6, PubMed 29316982

Publications 2017

1. Anumala UR, Waaler J, Nkizinkiko Y, Ignatev A, Lazarow K, Lindemann P, Olsen PA, Murthy S, Obaji E, Majouga AG, Leonov S, von Kries JP, Lehtiö L, Krauss S, Nazaré M (2017)
   Discovery of a Novel Series of Tankyrase Inhibitors by a Hybridization Approach
   J Med Chem, 60 (24), 10013-10025
   DOI 10.1021/acs.jmedchem.7b00883, PubMed 29155568
2. Solberg NT, Waaler J, Lund K, Mygland L, Olsen PA, Krauss S (2017)
   TANKYRASE Inhibition Enhances the Antiproliferative Effect of PI3K and EGFR Inhibition, Mutually Affecting β-CATENIN and AKT Signaling in Colorectal Cancer
   Mol Cancer Res, 16 (3), 543-553
   DOI 10.1158/1541-7786.MCR-17-0362, PubMed 29222171
3. Vehus T, Waaler J, Krauss S, Lundanes E, Wilson SR (2017)
   Combining HIC, SEC, and IEX with Fluorescence Polarization for Drug Target Discovery
   LC GC Eur., 30 (5), 232-239

Publications 2016

1. Vehus T, Roberg-Larsen H, Waaler J, Aslaksen S, Krauss S, Wilson SR, Lundanes E (2016)
   Versatile, sensitive liquid chromatography mass spectrometry - Implementation of 10 μm OT columns suitable for small molecules, peptides and proteins
   Sci Rep, 6, 37507
   DOI 10.1038/srep37507, PubMed 27897190

Publications 2015

1. Haikarainen T, Waaler J, Ignatev A, Nkizinkiko Y, Venkannagari H, Obaji E, Krauss S, Lehtiö L (2015)
   Development and structural analysis of adenosine site binding tankyrase inhibitors
   Bioorg Med Chem Lett, 26 (2), 328-333
   DOI 10.1016/j.bmcl.2015.12.018, PubMed 26706174
2. Thorvaldsen TE, Pedersen NM, Wenzel EM, Schultz SW, Brech A, Liestøl K, Waaler J, Krauss S, Stenmark H (2015)
   Structure, Dynamics, and Functionality of Tankyrase Inhibitor-Induced Degradasomes
   Mol Cancer Res, 13 (11), 1487-501
   DOI 10.1158/1541-7786.MCR-15-0125, PubMed 26124443
3. Zhong L, Ding Y, Bandyopadhyay G, Waaler J, Börgeson E, Smith S, Zhang M, Phillips SA, Mahooti S, Mahata SK, Shao J, Krauss S, Chi NW (2015)
   The PARsylation activity of tankyrase in adipose tissue modulates systemic glucose metabolism in mice
   Diabetologia, 59 (3), 582-91
   DOI 10.1007/s00125-015-3815-1, PubMed 26631215

Publications 2013

1. Lau T, Chan E, Callow M, Waaler J, Boggs J, Blake RA, Magnuson S, Sambrone A, Schutten M, Firestein R, Machon O, Korinek V, Choo E, Diaz D, Merchant M, Polakis P, Holsworth DD, Krauss S, Costa M (2013)
   A novel tankyrase small-molecule inhibitor suppresses APC mutation-driven colorectal tumor growth
   Cancer Res, 73 (10), 3132-44
   DOI 10.1158/0008-5472.CAN-12-4562, PubMed 23539443
2. Stratford EW, Daffinrud J, Munthe E, Castro R, Waaler J, Krauss S, Myklebost O (2013)
   The tankyrase-specific inhibitor JW74 affects cell cycle progression and induces apoptosis and differentiation in osteosarcoma cell lines
   Cancer Med, 3 (1), 36-46
   DOI 10.1002/cam4.170, PubMed 24403055
3. Voronkov A, Holsworth DD, Waaler J, Wilson SR, Ekblad B, Perdreau-Dahl H, Dinh H, Drewes G, Hopf C, Morth JP, Krauss S (2013)
   Structural basis and SAR for G007-LK, a lead stage 1,2,4-triazole based specific tankyrase 1/2 inhibitor
   J Med Chem, 56 (7), 3012-23
   DOI 10.1021/jm4000566, PubMed 23473363

Publications 2012

1. Waaler J, Machon O, Tumova L, Dinh H, Korinek V, Wilson SR, Paulsen JE, Pedersen NM, Eide TJ, Machonova O, Gradl D, Voronkov A, von Kries JP, Krauss S (2012)
   A novel tankyrase inhibitor decreases canonical Wnt signaling in colon carcinoma cells and reduces tumor growth in conditional APC mutant mice
   Cancer Res, 72 (11), 2822-32
   DOI 10.1158/0008-5472.CAN-11-3336, PubMed 22440753

Publications 2011

1. Waaler J, Machon O, von Kries JP, Wilson SR, Lundenes E, Wedlich D, Gradl D, Paulsen JE, Machonova O, Dembinski JL, Dinh H, Krauss S (2011)
   Novel synthetic antagonists of canonical Wnt signaling inhibit colorectal cancer cell growth
   Cancer Res, 71 (1), 197-205
   DOI 10.1158/0008-5472.CAN-10-1282, PubMed 21199802