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Page 1
Piperazin-1-ylpyridazine Derivatives Are a Novel Class of Human dCTP Pyrophosphatase 1 Inhibitors.
Llona-Minguez S, Höglund A, Ghassemian A, Desroses M, Calderón-Montaño JM, Burgos Morón E, Valerie NCK, Wiita E, Almlöf I, Koolmeister T, Mateus A, Cazares-Körner C, Sanjiv K, Homan E, Loseva O, Baranczewski P, Darabi M, Mehdizadeh A, Fayezi S, Jemth AS, Warpman Berglund U, Sigmundsson K, Lundbäck T, Jenmalm Jensen A, Artursson P, Scobie M, Helleday T. Llona-Minguez S, et al. Among authors: koolmeister t. J Med Chem. 2017 May 25;60(10):4279-4292. doi: 10.1021/acs.jmedchem.7b00182. Epub 2017 May 16. J Med Chem. 2017. PMID: 28508636
Correction to Piperazin-1-ylpyridazine Derivatives Are a Novel Class of Human dCTP Pyrophosphatase 1 Inhibitors.
Llona-Minguez S, Höglund A, Ghassemian A, Desroses M, Calderón-Montaño JM, Burgos Morón E, Valerie NCK, Wiita E, Almlöf I, Koolmeister T, Mateus A, Cazares-Körner C, Sanjiv K, Homan E, Loseva O, Baranczewski P, Darabi M, Mehdizadeh A, Fayezi S, Jemth AS, Warpman Berglund U, Sigmundsson K, Lundbäck T, Jenmalm Jensen A, Artursson P, Scobie M, Helleday T. Llona-Minguez S, et al. Among authors: koolmeister t. J Med Chem. 2017 Sep 14;60(17):7614. doi: 10.1021/acs.jmedchem.7b01137. Epub 2017 Sep 1. J Med Chem. 2017. PMID: 28862438 No abstract available.
Validation and development of MTH1 inhibitors for treatment of cancer.
Warpman Berglund U, Sanjiv K, Gad H, Kalderén C, Koolmeister T, Pham T, Gokturk C, Jafari R, Maddalo G, Seashore-Ludlow B, Chernobrovkin A, Manoilov A, Pateras IS, Rasti A, Jemth AS, Almlöf I, Loseva O, Visnes T, Einarsdottir BO, Gaugaz FZ, Saleh A, Platzack B, Wallner OA, Vallin KS, Henriksson M, Wakchaure P, Borhade S, Herr P, Kallberg Y, Baranczewski P, Homan EJ, Wiita E, Nagpal V, Meijer T, Schipper N, Rudd SG, Bräutigam L, Lindqvist A, Filppula A, Lee TC, Artursson P, Nilsson JA, Gorgoulis VG, Lehtiö J, Zubarev RA, Scobie M, Helleday T. Warpman Berglund U, et al. Among authors: koolmeister t. Ann Oncol. 2016 Dec;27(12):2275-2283. doi: 10.1093/annonc/mdw429. Epub 2016 Nov 8. Ann Oncol. 2016. PMID: 27827301 Free article.
MTH1 inhibition eradicates cancer by preventing sanitation of the dNTP pool.
Gad H, Koolmeister T, Jemth AS, Eshtad S, Jacques SA, Ström CE, Svensson LM, Schultz N, Lundbäck T, Einarsdottir BO, Saleh A, Göktürk C, Baranczewski P, Svensson R, Berntsson RP, Gustafsson R, Strömberg K, Sanjiv K, Jacques-Cordonnier MC, Desroses M, Gustavsson AL, Olofsson R, Johansson F, Homan EJ, Loseva O, Bräutigam L, Johansson L, Höglund A, Hagenkort A, Pham T, Altun M, Gaugaz FZ, Vikingsson S, Evers B, Henriksson M, Vallin KS, Wallner OA, Hammarström LG, Wiita E, Almlöf I, Kalderén C, Axelsson H, Djureinovic T, Puigvert JC, Häggblad M, Jeppsson F, Martens U, Lundin C, Lundgren B, Granelli I, Jensen AJ, Artursson P, Nilsson JA, Stenmark P, Scobie M, Berglund UW, Helleday T. Gad H, et al. Among authors: koolmeister t. Nature. 2014 Apr 10;508(7495):215-21. doi: 10.1038/nature13181. Epub 2014 Apr 2. Nature. 2014. PMID: 24695224
Chemical strategies for development of ATR inhibitors.
Llona-Minguez S, Höglund A, Jacques SA, Koolmeister T, Helleday T. Llona-Minguez S, et al. Among authors: koolmeister t. Expert Rev Mol Med. 2014 May 9;16:e10. doi: 10.1017/erm.2014.10. Expert Rev Mol Med. 2014. PMID: 24810715 Review.
dUTPase inhibition augments replication defects of 5-Fluorouracil.
Hagenkort A, Paulin CBJ, Desroses M, Sarno A, Wiita E, Mortusewicz O, Koolmeister T, Loseva O, Jemth AS, Almlöf I, Homan E, Lundbäck T, Gustavsson AL, Scobie M, Helleday T. Hagenkort A, et al. Among authors: koolmeister t. Oncotarget. 2017 Apr 4;8(14):23713-23726. doi: 10.18632/oncotarget.15785. Oncotarget. 2017. PMID: 28423595 Free PMC article.
Development of a chemical probe against NUDT15.
Zhang SM, Desroses M, Hagenkort A, Valerie NCK, Rehling D, Carter M, Wallner O, Koolmeister T, Throup A, Jemth AS, Almlöf I, Loseva O, Lundbäck T, Axelsson H, Regmi S, Sarno A, Krämer A, Pudelko L, Bräutigam L, Rasti A, Göttmann M, Wiita E, Kutzner J, Schaller T, Kalderén C, Cázares-Körner A, Page BDG, Krimpenfort R, Eshtad S, Altun M, Rudd SG, Knapp S, Scobie M, Homan EJ, Berglund UW, Stenmark P, Helleday T. Zhang SM, et al. Among authors: koolmeister t. Nat Chem Biol. 2020 Oct;16(10):1120-1128. doi: 10.1038/s41589-020-0592-z. Epub 2020 Jul 20. Nat Chem Biol. 2020. PMID: 32690945 Free PMC article.
Crystal structures of NUDT15 variants enabled by a potent inhibitor reveal the structural basis for thiopurine sensitivity.
Rehling D, Zhang SM, Jemth AS, Koolmeister T, Throup A, Wallner O, Scaletti E, Moriyama T, Nishii R, Davies J, Desroses M, Rudd SG, Scobie M, Homan E, Berglund UW, Yang JJ, Helleday T, Stenmark P. Rehling D, et al. Among authors: koolmeister t. J Biol Chem. 2021 Jan-Jun;296:100568. doi: 10.1016/j.jbc.2021.100568. Epub 2021 Mar 19. J Biol Chem. 2021. PMID: 33753169 Free PMC article.
27 results