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
Eur J Med Chem, 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
J Med Chem (in press)
DOI 10.1021/acs.jmedchem.4c02845, PubMed 40134122

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
Cancer Res Commun, 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
J Med Chem, 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
iScience, 24 (7), 102807
DOI 10.1016/j.isci.2021.102807, PubMed 34337362

Publications 2020

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