Identification and evaluation of small-molecule inhibitors against the dNTPase SAMHD1 via a comprehensive screening funnel

Authors: Zhang, Si Min ^{1, ∗}, Paulin, Cynthia B.J. ^{1, 4}, Shu, Huazhang ¹, Yagüe-Capilla, Miriam ¹, Michel, Maurice ¹, Marttila, Petra ¹, Ortis, Florian ¹, Bwanika, Henri Colyn ¹, Dirks, Christopher ¹, Venkatram, Rajagopal Papagudi ^{1, 5}, Wiita, Elisée ¹, Jemth, Ann-Sofie ¹, Almlöf, Ingrid ¹, Loseva, Olga ¹, Hormann, Femke M. ¹, Koolmeister, Tobias ¹, Linde, Erika ^{1, 6}, Lee, Sun ^{1, 7}, Llona-Minguez, Sabin ^{1, 8}, Haraldsson, Martin ², Axelsson, Hanna ², Strömberg, Kia ^{1, 9}, Homan, Evert J. ¹, Scobie, Martin ¹, Lundbäck, Thomas ^{2, 10}, Helleday, Thomas ^{1, 3}, Rudd, Sean G. ^{1, 11, ∗∗}

Source: In iScience 16 February 2024 27(2)

Inhibition of MYC translation through targeting of the newly identified PHB-eIF4F complex as a therapeutic strategy in CLL

Authors: Largeot, Anne, Klapp, Vanessa, Viry, Elodie, Gonder, Susanne, Fernandez Botana, Iria, Blomme, Arnaud, Benzarti, Mohaned, Pierson, Sandrine, Duculty, Chloé, Marttila, Petra, Wierz, Marina, Gargiulo, Ernesto, Pagano, Giulia, An, Ning, El Hachem, Najla, Perez Hernandez, Daniel, Chakraborty, Supriya, Ysebaert, Loïc, François, Jean-Hugues, Cortez Clemente, Susan, Berchem, Guy, Efremov, Dimitar G., Dittmar, Gunnar, Szpakowska, Martyna, Chevigné, Andy, Nazarov, Petr V., Helleday, Thomas, Close, Pierre, Meiser, Johannes, Stamatopoulos, Basile, Désaubry, Laurent, Paggetti, Jérôme, Moussay, Etienne

Source: In Blood 29 June 2023 141(26):3166-3183

NUDT1 promotes the accumulation and longevity of CD103+ TRM cells in primary biliary cholangitis

Authors: Huang, Bingyuan, Lyu, Zhuwan, Qian, Qiwei, Chen, Yong, Zhang, Jun, Li, Bo, Li, Yikang, Liang, Jubo, Liu, Qiaoyan, Li, You, Chen, Ruiling, Lian, Min, Xiao, Xiao, Miao, Qi, Wang, Qixia, Fang, Jingyuan, Lian, Zhexiong, Li, Yanmei, Tang, Ruqi, Helleday, Thomas, Gershwin, M. Eric, You, Zhengrui, Ma, Xiong

Source: In Journal of Hepatology November 2022 77(5):1311-1324

Defects in 8-oxo-guanine repair pathway cause high frequency of C > A substitutions in neuroblastoma

Authors: van den Boogaard, Marlinde L., Oka, Rurika, Hakkert, Anne, Schild, Linda, Ebus, Marli E., van Gerven, Michael R., Zwijnenburg, Danny A., Molenaar, Piet, Hoyng, Lieke L., Dolman, M. Emmy M., Essing, Anke H. W., Koopmans, Bianca, Helleday, Thomas, Drost, Jarno, van Boxtel, Ruben, Versteeg, Rogier, Koster, Jan, Molenaar, Jan J.

Source: Proceedings of the National Academy of Sciences of the United States of America, 2021 Sep 01. 118(36), 1-9.

Access URL: https://www.jstor.org/stable/27075431

Targeting the DNA damage response and repair in cancer through nucleotide metabolism

Authors: Helleday, Thomas, Rudd, Sean G.

Source: Molecular oncology. 16(21):3792-3810

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100163915240.0x000001&indx=1&recIds=ETOCvdc_100163915240.0x000001

MutT Homolog 1 Inhibitor Karonudib Attenuates Autoimmune Hepatitis by Inhibiting DNA Repair in Activated T Cells

Authors: Chen, Yong, Hua, Xiangwei, Huang, Bingyuan, Karsten, Stella, You, Zhengrui, Li, Bo, Li, You, Li, Yikang, Liang, Jubo, Zhang, Jun, Wei, Yiran, Chen, Ruiling, Lyu, Zhuwan, Xiao, Xiao, Lian, Min, Wei, Jue, Fang, Jingyuan, Miao, Qi, Wang, Qixia, Berglung, Ulrika Warpman, Tang, Ruqi, Helleday, Thomas, Ma, Xiong

Source: Hepatology communications. 6(5):1016-1031

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100148394750.0x000001&indx=1&recIds=ETOCvdc_100148394750.0x000001

Nudix hydrolase 18 catalyzes the hydrolysis of active triphosphate metabolites of the antivirals remdesivir, ribavirin, and molnupiravir

Authors: Jemth, Ann-Sofie, Scaletti, Emma Rose, Homan, Evert, Stenmark, Pål, Helleday, Thomas, Michel, Maurice

Source: In Journal of Biological Chemistry August 2022 298(8)

NUDT15-mediated hydrolysis limits the efficacy of anti-HCMV drug ganciclovir

Authors: Zhang, Si Min, Rehling, Daniel, Jemth, Ann-Sofie, Throup, Adam, Landázuri, Natalia, Almlöf, Ingrid, Göttmann, Mona, Valerie, Nicholas C.K., Borhade, Sanjay R., Wakchaure, Prasad, Page, Brent D.G., Desroses, Matthieu, Homan, Evert J., Scobie, Martin, Rudd, Sean G., Berglund, Ulrika Warpman, Söderberg-Nauclér, Cecilia, Stenmark, Pål, Helleday, Thomas

Source: In Cell Chemical Biology 16 December 2021 28(12):1693-1702

MTH1 Inhibitors for the Treatment of Psoriasis

Authors: Bivik Eding, Cecilia, Köhler, Ines, Verma, Deepti, Sjögren, Florence, Bamberg, Claudia, Karsten, Stella, Pham, Therese, Scobie, Martin, Helleday, Thomas, Warpman Berglund, Ulrika, Enerbäck, Charlotta

Source: In Journal of Investigative Dermatology August 2021 141(8):2037-2048

Crystal structures of NUDT15 variants enabled by a potent inhibitor reveal the structural basis for thiopurine sensitivity

Authors: Rehling, Daniel, Zhang, Si Min, Jemth, Ann-Sofie, Koolmeister, Tobias, Throup, Adam, Wallner, Olov, Scaletti, Emma, Moriyama, Takaya, Nishii, Rina, Davies, Jonathan, Desroses, Matthieu, Rudd, Sean G., Scobie, Martin, Homan, Evert, Berglund, Ulrika Warpman, Yang, Jun J., Helleday, Thomas, Stenmark, Pål

Source: In Journal of Biological Chemistry January-June 2021 296

Kinetic and structural characterization of NUDT15 and NUDT18 as catalysts of isoprene pyrophosphate hydrolysis.

Authors: Scaletti, Emma R., Unterlass, Judith E., Almlöf, Ingrid, Koolmeister, Tobias, Vallin, Karl S., Kapsitidou, Despina, Tsuber, Viktoriia, Helleday, Thomas, Stenmark, Pål, Jemth, Ann‐Sofie

Source: FEBS Journal; Oct2024, Vol. 291 Issue 19, p4301-4322, 22p

Subject Terms: CELL membranes, PYROPHOSPHATES, ISOPRENYLATION, ISOPRENE, HYDROLASES

Ex vivo assessment of targeted therapies in a rare metastatic epithelial–myoepithelial carcinoma

Authors: Mäkelä, Rami, Arjonen, Antti, Suryo Rahmanto, Aldwin, Härmä, Ville, Lehtiö, Janne, Kuopio, Teijo, Helleday, Thomas, Sangfelt, Olle, Kononen, Juha, Rantala, Juha K.

Source: In Neoplasia September 2020 22(9):390-398

Crystal structures of human PAICS reveal substrate and product binding of an emerging cancer target

Authors: Škerlová, Jana, Unterlass, Judith, Göttmann, Mona, Marttila, Petra, Homan, Evert, Helleday, Thomas, Jemth, Ann-Sofie ^*, Stenmark, Pål ^*

Source: In Journal of Biological Chemistry 14 August 2020 295(33):11656-11668

MutT homologue 1 (MTH1) removes N6-methyl-dATP from the dNTP pool

Authors: Scaletti, Emma Rose, Vallin, Karl S., Bräutigam, Lars, Sarno, Antonio ^**, Warpman Berglund, Ulrika, Helleday, Thomas, Stenmark, Pål, Jemth, Ann-Sofie

Source: In Journal of Biological Chemistry 10 April 2020 295(15):4761-4772

Cell Cycle Profiling Reveals Protein Oscillation, Phosphorylation, and Localization Dynamics

Authors: Herr, Patrick ^{‡, §, ‡‡}, Boström, Johan ^{¶, ‡‡}, Rullman, Eric ^¶, Rudd, Sean G. ^‡, Vesterlund, Mattias ^‡, Lehtiö, Janne ^‡, Helleday, Thomas ^{‡, §}, Maddalo, Gianluca ^‖, Altun, Mikael ^{¶, **}

Source: In Molecular & Cellular Proteomics April 2020 19(4):608-623

Synthesis of Substituted Indazole Acetic Acids by N−N Bond Forming Reactions

Authors: Odell, Luke R., Skillinghaug, Bobo, Matt, Christof, Wu, Peng, Koolmeister, Tobias, Desroses, Matthieu, Llona‐Minguez, Sabin, Wallner, Olov, Helleday, Thomas, Scobie, Martin

Source: European journal of organic chemistry. 26(29)

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100190847164.0x000001&indx=1&recIds=ETOCvdc_100190847164.0x000001

Front Cover: Synthesis of Substituted Indazole Acetic Acids by N−N Bond Forming Reactions (Eur. J. Org. Chem. 29/2023)

Authors: Odell, Luke R., Skillinghaug, Bobo, Matt, Christof, Wu, Peng, Koolmeister, Tobias, Desroses, Matthieu, Llona‐Minguez, Sabin, Wallner, Olov, Helleday, Thomas, Scobie, Martin

Source: European journal of organic chemistry. 26(29)

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100190847283.0x000001&indx=1&recIds=ETOCvdc_100190847283.0x000001

Front Cover: Optimization of N‐Piperidinyl‐Benzimidazolone Derivatives as Potent and Selective Inhibitors of 8‐Oxo‐Guanine DNA Glycosylase 1 (ChemMedChem 1/2023)

Authors: 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, Benítez‐Buelga, Carlos, Davies, Jonathan, Scobie, Martin, Warpman Berglund, Ulrika, Kalderén, Christina, Stenmark, Pål, Helleday, Thomas, Michel, Maurice

Source: ChemMedChem. 18(1)

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100171665615.0x000001&indx=1&recIds=ETOCvdc_100171665615.0x000001

Optimization of N‐Piperidinyl‐Benzimidazolone Derivatives as Potent and Selective Inhibitors of 8‐Oxo‐Guanine DNA Glycosylase 1

Authors: 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, Benítez‐Buelga, Carlos, Davies, Jonathan, Scobie, Martin, Warpman Berglund, Ulrika, Kalderén, Christina, Stenmark, Pål, Helleday, Thomas, Michel, Maurice

Source: ChemMedChem. 18(1)

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100171665481.0x000001&indx=1&recIds=ETOCvdc_100171665481.0x000001

TH1579, MTH1 inhibitor, delays tumour growth and inhibits metastases development in osteosarcoma model

Authors: Moukengue, Brice, Brown, Hannah K, Charrier, Céline, Battaglia, Séverine, Baud'huin, Marc, Quillard, Thibaut, Pham, Therese M, Pateras, Ioannis S, Gorgoulis, Vassilis G, Helleday, Thomas, Heymann, Dominique, Berglund, Ulrika Warpman, Ory, Benjamin, Lamoureux, Francois

Source: In EBioMedicine March 2020 53