Publications 2025

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
288, 117397
DOI 10.1016/j.ejmech.2025.117397, PubMed 39983556

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
68 (7), 7263-7279
DOI 10.1021/acs.jmedchem.4c02845, PubMed 40134122

Publications 2023

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
11 (10)
DOI 10.3390/biomedicines11102719, PubMed 37893093

Publications 2022

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
2 (4), 233-245
DOI 10.1158/2767-9764.CRC-22-0027, PubMed 36873622

Publications 2021

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
64 (24), 17936-17949
DOI 10.1021/acs.jmedchem.1c01264, PubMed 34878777

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
24 (7), 102807
DOI 10.1016/j.isci.2021.102807, PubMed 34337362

Publications 2020

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
12 (6)
DOI 10.3390/cancers12061630, PubMed 32575464

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
10 (9), 4927
DOI 10.1039/d0ra90007a, PubMed 35503286

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
44 (8), 1691-1702
DOI 10.1038/s41366-020-0573-z, PubMed 32317752

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
63 (13), 6834-6846
DOI 10.1021/acs.jmedchem.0c00208, PubMed 32511917

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
3 (1), 196
DOI 10.1038/s42003-020-0916-2, PubMed 32332858

Publications 2019

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
9 (63), 37092-37100
DOI 10.1039/c9ra08954c, PubMed 35539091

Publications 2018

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
51 (1), 3
DOI 10.1186/s40659-017-0151-6, PubMed 29316982

Publications 2017

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
60 (24), 10013-10025
DOI 10.1021/acs.jmedchem.7b00883, PubMed 29155568

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
16 (3), 543-553
DOI 10.1158/1541-7786.MCR-17-0362, PubMed 29222171

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

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
6, 37507
DOI 10.1038/srep37507, PubMed 27897190

Publications 2015

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
26 (2), 328-333
DOI 10.1016/j.bmcl.2015.12.018, PubMed 26706174

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
13 (11), 1487-501
DOI 10.1158/1541-7786.MCR-15-0125, PubMed 26124443

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
59 (3), 582-91
DOI 10.1007/s00125-015-3815-1, PubMed 26631215

Publications 2013

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
73 (10), 3132-44
DOI 10.1158/0008-5472.CAN-12-4562, PubMed 23539443

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
3 (1), 36-46
DOI 10.1002/cam4.170, PubMed 24403055

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
56 (7), 3012-23
DOI 10.1021/jm4000566, PubMed 23473363

Publications 2012

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
72 (11), 2822-32
DOI 10.1158/0008-5472.CAN-11-3336, PubMed 22440753

Publications 2011

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
71 (1), 197-205
DOI 10.1158/0008-5472.CAN-10-1282, PubMed 21199802