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Page 1
Formate overflow drives toxic folate trapping in MTHFD1 inhibited cancer cells.
Green AC, Marttila P, Kiweler N, Chalkiadaki C, Wiita E, Cookson V, Lesur A, Eiden K, Bernardin F, Vallin KSA, Borhade S, Long M, Ghahe EK, Jiménez-Alonso JJ, Jemth AS, Loseva O, Mortusewicz O, Meyers M, Viry E, Johansson AI, Hodek O, Homan E, Bonagas N, Ramos L, Sandberg L, Frödin M, Moussay E, Slipicevic A, Letellier E, Paggetti J, Sørensen CS, Helleday T, Henriksson M, Meiser J. Green AC, et al. Among authors: wiita e. Nat Metab. 2023 Apr;5(4):642-659. doi: 10.1038/s42255-023-00771-5. Epub 2023 Apr 3. Nat Metab. 2023. PMID: 37012496 Free PMC article.
Pharmacological targeting of MTHFD2 suppresses acute myeloid leukemia by inducing thymidine depletion and replication stress.
Bonagas N, Gustafsson NMS, Henriksson M, Marttila P, Gustafsson R, Wiita E, Borhade S, Green AC, Vallin KSA, Sarno A, Svensson R, Göktürk C, Pham T, Jemth AS, Loseva O, Cookson V, Kiweler N, Sandberg L, Rasti A, Unterlass JE, Haraldsson M, Andersson Y, Scaletti ER, Bengtsson C, Paulin CBJ, Sanjiv K, Abdurakhmanov E, Pudelko L, Kunz B, Desroses M, Iliev P, Färnegårdh K, Krämer A, Garg N, Michel M, Häggblad S, Jarvius M, Kalderén C, Jensen AB, Almlöf I, Karsten S, Zhang SM, Häggblad M, Eriksson A, Liu J, Glinghammar B, Nekhotiaeva N, Klingegård F, Koolmeister T, Martens U, Llona-Minguez S, Moulson R, Nordström H, Parrow V, Dahllund L, Sjöberg B, Vargas IL, Vo DD, Wannberg J, Knapp S, Krokan HE, Arvidsson PI, Scobie M, Meiser J, Stenmark P, Berglund UW, Homan EJ, Helleday T. Bonagas N, et al. Among authors: wiita e. Nat Cancer. 2022 Feb;3(2):156-172. doi: 10.1038/s43018-022-00331-y. Epub 2022 Feb 28. Nat Cancer. 2022. PMID: 35228749 Free PMC 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: wiita e. Nature. 2014 Apr 10;508(7495):215-21. doi: 10.1038/nature13181. Epub 2014 Apr 2. Nature. 2014. PMID: 24695224
Crystal Structure of the Emerging Cancer Target MTHFD2 in Complex with a Substrate-Based Inhibitor.
Gustafsson R, Jemth AS, Gustafsson NM, Färnegårdh K, Loseva O, Wiita E, Bonagas N, Dahllund L, Llona-Minguez S, Häggblad M, Henriksson M, Andersson Y, Homan E, Helleday T, Stenmark P. Gustafsson R, et al. Among authors: wiita e. Cancer Res. 2017 Feb 15;77(4):937-948. doi: 10.1158/0008-5472.CAN-16-1476. Epub 2016 Nov 29. Cancer Res. 2017. PMID: 27899380
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: wiita e. Oncotarget. 2017 Apr 4;8(14):23713-23726. doi: 10.18632/oncotarget.15785. Oncotarget. 2017. PMID: 28423595 Free PMC article.
Targeting PFKFB3 radiosensitizes cancer cells and suppresses homologous recombination.
Gustafsson NMS, Färnegårdh K, Bonagas N, Ninou AH, Groth P, Wiita E, Jönsson M, Hallberg K, Lehto J, Pennisi R, Martinsson J, Norström C, Hollers J, Schultz J, Andersson M, Markova N, Marttila P, Kim B, Norin M, Olin T, Helleday T. Gustafsson NMS, et al. Among authors: wiita e. Nat Commun. 2018 Sep 24;9(1):3872. doi: 10.1038/s41467-018-06287-x. Nat Commun. 2018. PMID: 30250201 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: wiita e. 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.
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: wiita e. Ann Oncol. 2016 Dec;27(12):2275-2283. doi: 10.1093/annonc/mdw429. Epub 2016 Nov 8. Ann Oncol. 2016. PMID: 27827301 Free article.
Identification of Triazolothiadiazoles as Potent Inhibitors of the dCTP Pyrophosphatase 1.
Llona-Minguez S, Höglund A, Wiita E, Almlöf I, Mateus A, Calderón-Montaño JM, Cazares-Körner C, Homan E, Loseva O, Baranczewski P, Jemth AS, Häggblad M, Martens U, Lundgren B, Artursson P, Lundbäck T, Jenmalm Jensen A, Warpman Berglund U, Scobie M, Helleday T. Llona-Minguez S, et al. Among authors: wiita e. J Med Chem. 2017 Mar 9;60(5):2148-2154. doi: 10.1021/acs.jmedchem.6b01786. Epub 2017 Feb 15. J Med Chem. 2017. PMID: 28145708
30 results