• Computational and Experimental Druggability Assessment of Human DNA Glycosylases 

      Michel, M; Visnes, Torkild; Homan, Evert; Seashore-Ludlow, Brinton; Hedenström, Mattias; Wiita, Elisee; Vallin, K; Paulin, Cynthia BJ; Zhang, Jiaxi; Wallner, Olov; Scobie, Martin; Schmidt, A.; Jenmalm-Jensen, Annika; Warpman Berglund, Ulrika; Helleday, Thomas (Peer reviewed; Journal article, 2019)
      Due to a polar or even charged binding interface, DNA-binding proteins are considered extraordinarily difficult targets for development of small-molecule ligands and only a handful of proteins have been targeted successfully ...
    • Optimization of N-Piperidinyl-Benzimidazolone Derivatives as Potent and Selective Inhibitors of 8-Oxo-Guanine DNA Glycosylase 1 

      Wallner, Olov; Cázares-Körner, Armando; Scaletti, Emma Rose; Masuyer, Geoffrey; Bekkhus, Tove; Visnes, Torkild; Mamonov, Kirill; Ortis, Florian; Lundbäck, Thomas; Volkova, Maria; Koolmeister, Tobias; Wiita, Elisée; Loseva, Olga; Pandey, Monica; Homan, Evert J.; Benítez-Buelga, Carlos; Davies, Jonathan; Scobie, Martin; Warpman Berglund, Ulrika; Kalderén, Christina; Stenmark, Pål; Helleday, Thomas; Michel, Maurice (Peer reviewed; Journal article, 2022)
      8-oxo Guanine DNA Glycosylase 1 is the initiating enzyme within base excision repair and removes oxidized guanines from damaged DNA. Since unrepaired 8-oxoG could lead to G : C→T : A transversion, base removal is of utmost ...
    • Small molecule inhibitor of OGG1 blocks oxidative DNA damage repair at telomeres and potentiates methotrexate anticancer effects 

      Baquero, Juan Miguel; Benitez-Buelga, Carlos; Rajagopal, Varshni; Zhenjun, Zhao; Torres-Ruiz, Raúl; Müller, Sarah; Hanna, Bishoy Magdi Fekry; Loseva, Olga; Wallner, Olov; Michel, Maurice; Rodriguez-Perales, Sandra; Gad, Helge; Visnes, Torkild; Helleday, Thomas; Benitez, Javier; Osario, Ana (Peer reviewed; Journal article, 2021)
      The most common oxidative DNA lesion is 8-oxoguanine which is mainly recognized and excised by the 8-oxoG DNA glycosylase 1 (OGG1), initiating the base excision repair (BER) pathway. Telomeres are particularly sensitive ...
    • Small-molecule inhibitor of OGG1 suppresses proinflammatory gene expression and inflammation 

      Visnes, Torkild; Armando, Cazares-Körner; Wenjing, Hao; Wallner, Olov; Masuyer, Geoffrey; Loseva, Olga; Mortusewicz, Oliver; Wiita, Elisee; Sarno, Antonio; Manoilov, Aleksandr; Astorga-Wells, Juan; Jemth, Ann-Sofie; Pan, Lang; Sanjiv, Kumar; Karsten, Stella; Gokturk, Camilla; Grube, Maurice; Evert J, Homan; Hanna, Bishoy Magdi Fekry; Cynthia, Paulin BJ; pham, Therese; Rasti, Azita; Warpman Berglund, Ulrika; von Nikolai, Catharina; Benitez-Buelga, Carlos; Koolmeister, Tobias; Ivanic, Dag; Iliev, Petar; Scobie, Martin; Krokan, Hans Einar; Baranczewski, Pawel; Artursson, Per; Altun, Mikael; Jenmalm-Jensen, Annika; Kalderen, Christina; Xueqing, Ba; Zubarev, Roman A.; Stenmark, Pål; Boldogh, Istvan; Helleday, Thomas (Journal article; Peer reviewed, 2018)
      The onset of inflammation is associated with reactive oxygen species and oxidative damage to macromolecules like 7,8-dihydro-8-oxoguanine (8-oxoG) in DNA. Because 8-oxoguanine DNA glycosylase 1 (OGG1) binds 8-oxoG and ...
    • Targeting OGG1 arrests cancer cell proliferation by inducing replication stress 

      Visnes, Torkild; Benitez-Buelga, Carlos; Cázares-Körner, Armando; Sanjiv, Kumar; Hanna, Bishoy M F; Mortusewicz, Oliver; Rajagopal, Varshni; Albers, Julian J.; Hagey, Daniel W.; Bekkhus, Tove; Eshtad, Saeed; Baquero, Juan Miguel; Masuyer, Geoffrey; Wallner, Olov; Müller, Sarah; Pham, Therese; Gokturk, Camilla; Rasti, Azita; Suman, Sharda; Torres-Ruiz, Raúl; Sarno, Antonio; Wiita, Elisée; Homan, Evert; Karsten, Stella; Marimuthu, Karthick; Michel, M; Koolmeister, Tobias; Scobie, Martin; Loseva, Olga; Almlöf, Ingrid; Unterlass, Judith Edda; Pettke, Aleksandra; Boström, Johan; Pandey, Monica; Gad, Helge; Herr, Patrick; Jemth, Ann-Sofie; El Andaloussi, Samir; Kalderén, Christina; Rodriguez-Perales, Sandra; Benítez, Javier; Krokan, Hans Einar; Altun, Mikael; Stenmark, Pål; Berglund, Ulrika Warpman; Helleday, Thomas (Peer reviewed; Journal article, 2020)
      Abstract Altered oncogene expression in cancer cells causes loss of redox homeostasis resulting in oxidative DNA damage, e.g. 8-oxoguanine (8-oxoG), repaired by base excision repair (BER). PARP1 coordinates BER and relies ...
    • Targeting OGG1 arrests cancer cell proliferation by inducing replication stress 

      Visnes, Torkild; Benitez-Buelga, Carlos; Cázares-Körner, Armando; Sanjiv, Kumar; Hanna, Bishoy M F; Mortusewicz, Oliver; Rajagopal, Varshni; Albers, Julian J.; Hagey, Daniel W.; Bekkhus, Tove; Eshtad, Saeed; Baquero, Juan Miguel; Masuyer, Geoffrey; Wallner, Olov; Müller, Sarah; Pham, Therese; Gokturk, Camilla; Rasti, Azita; Suman, Sharda; Torres-Ruiz, Raúl; Sarno, Antonio; Wiita, Elisée; Homan, Evert; Karsten, Stella; Marimuthu, Karthick; Michel, M; Koolmeister, Tobias; Scobie, Martin; Loseva, Olga; Almlöf, Ingrid; Unterlass, Judith Edda; Pettke, Aleksandra; Boström, Johan; Pandey, Monica; Gad, Helge; Herr, Patrick; Jemth, Ann-Sofie; El Andaloussi, Samir; Kalderén, Christina; Rodriguez-Perales, Sandra; Benítez, Javier; Krokan, Hans Einar; Altun, Mikael; Stenmark, Pål; Berglund, Ulrika Warpman; Helleday, Thomas (Peer reviewed; Journal article, 2020)
      Abstract Altered oncogene expression in cancer cells causes loss of redox homeostasis resulting in oxidative DNA damage, e.g. 8-oxoguanine (8-oxoG), repaired by base excision repair (BER). PARP1 coordinates BER and relies ...