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Page 1
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: berglund uw. 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.
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: berglund uw. 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.
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: berglund uw. Nature. 2014 Apr 10;508(7495):215-21. doi: 10.1038/nature13181. Epub 2014 Apr 2. Nature. 2014. PMID: 24695224
Discovery of the First Potent and Selective Inhibitors of Human dCTP Pyrophosphatase 1.
Llona-Minguez S, Höglund A, Jacques SA, Johansson L, Calderón-Montaño JM, Claesson M, Loseva O, Valerie NCK, Lundbäck T, Piedrafita J, Maga G, Crespan E, Meijer L, Morón EB, Baranczewski P, Hagbjörk AL, Svensson R, Wiita E, Almlöf I, Visnes T, Jeppsson F, Sigmundsson K, Jensen AJ, Artursson P, Jemth AS, Stenmark P, Berglund UW, Scobie M, Helleday T. Llona-Minguez S, et al. Among authors: berglund uw. J Med Chem. 2016 Feb 11;59(3):1140-1148. doi: 10.1021/acs.jmedchem.5b01741. Epub 2016 Jan 27. J Med Chem. 2016. PMID: 26771665 Free PMC article.
Small-molecule inhibitor of OGG1 suppresses proinflammatory gene expression and inflammation.
Visnes T, Cázares-Körner A, Hao W, Wallner O, Masuyer G, Loseva O, Mortusewicz O, Wiita E, Sarno A, Manoilov A, Astorga-Wells J, Jemth AS, Pan L, Sanjiv K, Karsten S, Gokturk C, Grube M, Homan EJ, Hanna BMF, Paulin CBJ, Pham T, Rasti A, Berglund UW, von Nicolai C, Benitez-Buelga C, Koolmeister T, Ivanic D, Iliev P, Scobie M, Krokan HE, Baranczewski P, Artursson P, Altun M, Jensen AJ, Kalderén C, Ba X, Zubarev RA, Stenmark P, Boldogh I, Helleday T. Visnes T, et al. Among authors: berglund uw. Science. 2018 Nov 16;362(6416):834-839. doi: 10.1126/science.aar8048. Science. 2018. PMID: 30442810 Free PMC article.
NUDT15-mediated hydrolysis limits the efficacy of anti-HCMV drug ganciclovir.
Zhang SM, Rehling D, Jemth AS, Throup A, Landázuri N, Almlöf I, Göttmann M, Valerie NCK, Borhade SR, Wakchaure P, Page BDG, Desroses M, Homan EJ, Scobie M, Rudd SG, Berglund UW, Söderberg-Nauclér C, Stenmark P, Helleday T. Zhang SM, et al. Among authors: berglund uw. Cell Chem Biol. 2021 Dec 16;28(12):1693-1702.e6. doi: 10.1016/j.chembiol.2021.06.001. Epub 2021 Jun 29. Cell Chem Biol. 2021. PMID: 34192523 Free article.
Small-molecule activation of OGG1 increases oxidative DNA damage repair by gaining a new function.
Michel M, Benítez-Buelga C, Calvo PA, Hanna BMF, Mortusewicz O, Masuyer G, Davies J, Wallner O, Sanjiv K, Albers JJ, Castañeda-Zegarra S, Jemth AS, Visnes T, Sastre-Perona A, Danda AN, Homan EJ, Marimuthu K, Zhenjun Z, Chi CN, Sarno A, Wiita E, von Nicolai C, Komor AJ, Rajagopal V, Müller S, Hank EC, Varga M, Scaletti ER, Pandey M, Karsten S, Haslene-Hox H, Loevenich S, Marttila P, Rasti A, Mamonov K, Ortis F, Schömberg F, Loseva O, Stewart J, D'Arcy-Evans N, Koolmeister T, Henriksson M, Michel D, de Ory A, Acero L, Calvete O, Scobie M, Hertweck C, Vilotijevic I, Kalderén C, Osorio A, Perona R, Stolz A, Stenmark P, Berglund UW, de Vega M, Helleday T. Michel M, et al. Among authors: berglund uw. Science. 2022 Jun 24;376(6600):1471-1476. doi: 10.1126/science.abf8980. Epub 2022 Jun 23. Science. 2022. PMID: 35737787
Targeting OGG1 arrests cancer cell proliferation by inducing replication stress.
Visnes T, Benítez-Buelga C, Cázares-Körner A, Sanjiv K, Hanna BMF, Mortusewicz O, Rajagopal V, Albers JJ, Hagey DW, Bekkhus T, Eshtad S, Baquero JM, Masuyer G, Wallner O, Müller S, Pham T, Göktürk C, Rasti A, Suman S, Torres-Ruiz R, Sarno A, Wiita E, Homan EJ, Karsten S, Marimuthu K, Michel M, Koolmeister T, Scobie M, Loseva O, Almlöf I, Unterlass JE, Pettke A, Boström J, Pandey M, Gad H, Herr P, Jemth AS, El Andaloussi S, Kalderén C, Rodriguez-Perales S, Benítez J, Krokan HE, Altun M, Stenmark P, Berglund UW, Helleday T. Visnes T, et al. Among authors: berglund uw. Nucleic Acids Res. 2020 Dec 2;48(21):12234-12251. doi: 10.1093/nar/gkaa1048. Nucleic Acids Res. 2020. PMID: 33211885 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: berglund uw. 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.
38 results