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| Fältnamn | Indikatorer | Metadata |
|---|---|---|
| 000 | 14340naa a2201825 4500 | |
| 001 | oai:DiVA.org:uu-470347 | |
| 003 | SwePub | |
| 008 | 220324s2022 | |||||||||||000 ||eng| | |
| 009 | oai:DiVA.org:kth-310076 | |
| 009 | oai:DiVA.org:su-203237 | |
| 009 | oai:prod.swepub.kib.ki.se:148956713 | |
| 009 | oai:lup.lub.lu.se:7e0eea0f-45be-41ba-8a0e-cc9ce8ca6504 | |
| 024 | 7 | a https://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-4703472 URI |
| 024 | 7 | a https://doi.org/10.1038/s43018-022-00331-y2 DOI |
| 024 | 7 | a https://urn.kb.se/resolve?urn=urn:nbn:se:kth:diva-3100762 URI |
| 024 | 7 | a https://urn.kb.se/resolve?urn=urn:nbn:se:su:diva-2032372 URI |
| 024 | 7 | a http://kipublications.ki.se/Default.aspx?queryparsed=id:1489567132 URI |
| 024 | 7 | a https://lup.lub.lu.se/record/7e0eea0f-45be-41ba-8a0e-cc9ce8ca65042 URI |
| 040 | a (SwePub)uud (SwePub)kthd (SwePub)sud (SwePub)kid (SwePub)lu | |
| 041 | a engb eng | |
| 042 | 9 SwePub | |
| 072 | 7 | a ref2 swepub-contenttype |
| 072 | 7 | a art2 swepub-publicationtype |
| 100 | 1 | a Bonagas, Nadillyu Karolinska Institutet4 aut |
| 245 | 1 0 | a Pharmacological targeting of MTHFD2 suppresses acute myeloid leukemia by inducing thymidine depletion and replication stress |
| 264 | c 2022-02-28 | |
| 264 | 1 | b Springer Science and Business Media LLC,c 2022 |
| 338 | a electronic2 rdacarrier | |
| 500 | a QC 20220321 | |
| 520 | a The folate metabolism enzyme MTHFD2 (methylenetetrahydrofolate dehydrogenase/cyclohydrolase) is consistently overexpressed in cancer but its roles are not fully characterized, and current candidate inhibitors have limited potency for clinical development. In the present study, we demonstrate a role for MTHFD2 in DNA replication and genomic stability in cancer cells, and perform a drug screen to identify potent and selective nanomolar MTHFD2 inhibitors; protein cocrystal structures demonstrated binding to the active site of MTHFD2 and target engagement. MTHFD2 inhibitors reduced replication fork speed and induced replication stress followed by S-phase arrest and apoptosis of acute myeloid leukemia cells in vitro and in vivo, with a therapeutic window spanning four orders of magnitude compared with nontumorigenic cells. Mechanistically, MTHFD2 inhibitors prevented thymidine production leading to misincorporation of uracil into DNA and replication stress. Overall, these results demonstrate a functional link between MTHFD2-dependent cancer metabolism and replication stress that can be exploited therapeutically with this new class of inhibitors. Helleday and colleagues describe a nanomolar MTHFD2 inhibitor that causes replication stress and DNA damage accumulation in cancer cells via thymidine depletion, demonstrating a potential therapeutic strategy in AML tumors in vivo. | |
| 650 | 7 | a MEDICIN OCH HÄLSOVETENSKAPx Klinisk medicinx Cancer och onkologi0 (SwePub)302032 hsv//swe |
| 650 | 7 | a MEDICAL AND HEALTH SCIENCESx Clinical Medicinex Cancer and Oncology0 (SwePub)302032 hsv//eng |
| 650 | 7 | a NATURVETENSKAPx Biologix Cellbiologi0 (SwePub)106042 hsv//swe |
| 650 | 7 | a NATURAL SCIENCESx Biological Sciencesx Cell Biology0 (SwePub)106042 hsv//eng |
| 653 | a enzyme | |
| 653 | a enzyme inhibitor | |
| 653 | a LY345899 | |
| 653 | a methylenetetrahydrofolate dehydrogenase/cyclohydrolase | |
| 653 | a resazurin | |
| 653 | a small interfering RNA | |
| 653 | a TH7299 | |
| 653 | a TH9028 | |
| 653 | a TH9619 | |
| 653 | a thymidine | |
| 653 | a unclassified drug | |
| 653 | a uracil | |
| 653 | a acute myeloid leukemia | |
| 653 | a apoptosis assay | |
| 653 | a Article | |
| 653 | a cancer growth | |
| 653 | a cell culture | |
| 653 | a cell cycle assay | |
| 653 | a cell viability assay | |
| 653 | a chemical structure | |
| 653 | a colony formation | |
| 653 | a comet assay | |
| 653 | a confocal microscopy | |
| 653 | a crystal structure | |
| 653 | a crystallography | |
| 653 | a DNA damage | |
| 653 | a DNA replication | |
| 653 | a EC50 | |
| 653 | a flow cytometry | |
| 653 | a gene knockdown | |
| 653 | a genomic instability | |
| 653 | a high throughput screening | |
| 653 | a human | |
| 653 | a human cell | |
| 653 | a IC50 | |
| 653 | a physical chemistry | |
| 653 | a plasmid | |
| 653 | a RNA interference | |
| 653 | a S phase cell cycle checkpoint | |
| 653 | a surface plasmon resonance | |
| 653 | a tumor metabolism | |
| 653 | a Western blotting | |
| 700 | 1 | a Gustafsson, Nina M. S.u Karolinska Institutet4 aut |
| 700 | 1 | a Henriksson, Martinu Karolinska Institutet4 aut |
| 700 | 1 | a Marttila, Petrau Karolinska Inst, Dept Oncol Pathol, Sci Life Lab, Solna, Sweden.4 aut |
| 700 | 1 | a Gustafsson, Robert,d 1988-u Stockholms universitet,Institutionen för biokemi och biofysik,Stockholm Univ, Dept Biochem & Biophys, Stockholm, Sweden.4 aut0 (Swepub:su)rogu0454 |
| 700 | 1 | a Wiita, Eliseeu Karolinska Institutet4 aut |
| 700 | 1 | a Borhade, Sanjayu Karolinska Inst, Dept Oncol Pathol, Sci Life Lab, Solna, Sweden.4 aut |
| 700 | 1 | a Green, Alanna C.u Univ Sheffield, Med Sch, Dept Oncol & Metab, Weston Pk Canc Ctr, Sheffield, S Yorkshire, England.4 aut |
| 700 | 1 | a Vallin, Karl S. A.u Karolinska Institutet4 aut |
| 700 | 1 | a Sarno, Antoniou Karolinska Institutet4 aut |
| 700 | 1 | a Svensson, Richardu Uppsala universitet,Institutionen för farmaci,Science for Life Laboratory, SciLifeLab4 aut0 (Swepub:uu)ricsv977 |
| 700 | 1 | a Gokturk, Camillau Karolinska Inst, Dept Oncol Pathol, Sci Life Lab, Solna, Sweden.4 aut |
| 700 | 1 | a Pham, Thereseu Karolinska Institutet4 aut |
| 700 | 1 | a Jemth, Ann-Sofieu Karolinska Inst, Dept Oncol Pathol, Sci Life Lab, Solna, Sweden.4 aut |
| 700 | 1 | a Loseva, Olgau Karolinska Inst, Dept Oncol Pathol, Sci Life Lab, Solna, Sweden.4 aut |
| 700 | 1 | a Cookson, Victoriau Univ Sheffield, Med Sch, Dept Oncol & Metab, Weston Pk Canc Ctr, Sheffield, S Yorkshire, England.4 aut |
| 700 | 1 | a Kiweler, Nicoleu Luxembourg Inst Hlth, Dept Oncol, Canc Metab Grp, Luxembourg, Luxembourg.4 aut |
| 700 | 1 | a Sandberg, Larsu Stockholms universitet,Science for Life Laboratory (SciLifeLab),Institutionen för organisk kemi,Stockholm Univ, Dept Organ Chem, Sci Life Lab, Drug Discovery & Dev Platform, Solna, Sweden.4 aut0 (Swepub:su)lasa3159 |
| 700 | 1 | a Rasti, Azitau Karolinska Inst, Dept Oncol Pathol, Sci Life Lab, Solna, Sweden.4 aut |
| 700 | 1 | a Unterlass, Judith E.u Karolinska Inst, Dept Oncol Pathol, Sci Life Lab, Solna, Sweden.4 aut |
| 700 | 1 | a Haraldsson, Martinu Karolinska Institutet4 aut |
| 700 | 1 | a Andersson, Yasminu KTH,Läkemedelsutveckling,Science for Life Laboratory, SciLifeLab,Royal Inst Technol, Sch Engn Sci Chem Biotechnol & Hlth, Sci Life Lab, Drug Discovery & Dev Platform, Solna, Sweden.4 aut0 (Swepub:kth)u1io9xl7 |
| 700 | 1 | a Scaletti, Emma R.u Stockholm University,Lunds universitet,Stockholms universitet,Institutionen för biokemi och biofysik,Lund University, Sweden,Stockholm Univ, Dept Biochem & Biophys, Stockholm, Sweden.;Lund Univ, Dept Expt Med Sci, Lund, Sweden.,Strukturell biokemi,Forskargrupper vid Lunds universitet,Structural Biochemistry,Lund University Research Groups4 aut0 (Swepub:lu)em4772sc |
| 700 | 1 | a Bengtsson, Christofferu Stockholms universitet,Science for Life Laboratory (SciLifeLab),Institutionen för organisk kemi,Stockholm Univ, Dept Organ Chem, Sci Life Lab, Drug Discovery & Dev Platform, Solna, Sweden.4 aut0 (Swepub:su)chben |
| 700 | 1 | a Jarvius, Malinu Uppsala universitet,Cancerfarmakologi och beräkningsmedicin,Science for Life Laboratory, SciLifeLab4 aut0 (Swepub:uu)maemi734 |
| 700 | 1 | a Sanjiv, Kumaru Karolinska Inst, Dept Oncol Pathol, Sci Life Lab, Solna, Sweden.4 aut |
| 700 | 1 | a Abdurakhmanov, Eldar,d 1977-u Uppsala universitet,Biokemi,Science for Life Laboratory, SciLifeLab4 aut0 (Swepub:uu)eldab338 |
| 700 | 1 | a Pudelko, Lindau Karolinska Inst, Dept Oncol Pathol, Sci Life Lab, Solna, Sweden.4 aut |
| 700 | 1 | a Kunz, Benu Karolinska Inst, Dept Oncol Pathol, Sci Life Lab, Solna, Sweden.4 aut |
| 700 | 1 | a Desroses, Matthieuu Karolinska Inst, Dept Oncol Pathol, Sci Life Lab, Solna, Sweden.4 aut |
| 700 | 1 | a Iliev, Petaru Karolinska Institutet4 aut |
| 700 | 1 | a Färnegårdh, Katarinau Stockholms universitet,Science for Life Laboratory (SciLifeLab),Institutionen för organisk kemi,Stockholm Univ, Dept Organ Chem, Sci Life Lab, Drug Discovery & Dev Platform, Solna, Sweden.4 aut0 (Swepub:su)kfr |
| 700 | 1 | a Kramer, Andreasu Goethe Univ, Inst Pharmaceut Chem, Frankfurt, Germany.4 aut |
| 700 | 1 | a Garg, Neeraju Uppsala universitet,Science for Life Laboratory, SciLifeLab4 aut |
| 700 | 1 | a Michel, Mauriceu Karolinska Institutet4 aut |
| 700 | 1 | a Häggblad, Sarau Stockholms universitet,Science for Life Laboratory (SciLifeLab),Institutionen för biokemi och biofysik,Stockholm Univ, Dept Biochem & Biophys, Sci Life Lab, Biochem & Cellular Screening Facil, Solna, Sweden.4 aut0 (Swepub:su)sah |
| 700 | 1 | a Jarvius, Malinu Uppsala universitet,Cancerfarmakologi och beräkningsmedicin,Science for Life Laboratory, SciLifeLab4 aut0 (Swepub:uu)maemi734 |
| 700 | 1 | a Kalderen, Christinau Karolinska Inst, Dept Oncol Pathol, Sci Life Lab, Solna, Sweden.4 aut |
| 700 | 1 | a Jensen, Amanda Bogedahlu Karolinska Inst, Dept Oncol Pathol, Sci Life Lab, Solna, Sweden.4 aut |
| 700 | 1 | a Almlof, Ingridu Karolinska Institutet4 aut |
| 700 | 1 | a Karsten, Stellau Karolinska Institutet4 aut |
| 700 | 1 | a Zhang, Si Minu Karolinska Inst, Dept Oncol Pathol, Sci Life Lab, Solna, Sweden.4 aut |
| 700 | 1 | a Häggblad, Mariau Stockholms universitet,Science for Life Laboratory (SciLifeLab),Institutionen för biokemi och biofysik,Stockholm Univ, Dept Biochem & Biophys, Sci Life Lab, Biochem & Cellular Screening Facil, Solna, Sweden.4 aut0 (Swepub:su)maha7002 |
| 700 | 1 | a Eriksson, Andersu Karolinska Inst, Karolinska High Throughput Ctr, Dept Biosci & Nutr, Huddinge, Sweden.4 aut |
| 700 | 1 | a Liu, Jianpingu Karolinska Inst, Karolinska High Throughput Ctr, Dept Biosci & Nutr, Huddinge, Sweden.4 aut |
| 700 | 1 | a Glinghammar, Bjornu Karolinska Inst, Dept Med Biochem & Biophys, Sci Life Lab, Drug Discovery & Dev Platform, Solna, Sweden.4 aut |
| 700 | 1 | a Nekhotiaeva, Nataliau Karolinska Inst, Karolinska High Throughput Ctr, Dept Biosci & Nutr, Huddinge, Sweden.4 aut |
| 700 | 1 | a Klingegård, Fredriku Stockholms universitet,Science for Life Laboratory (SciLifeLab),Institutionen för organisk kemi,Stockholm Univ, Dept Organ Chem, Sci Life Lab, Drug Discovery & Dev Platform, Solna, Sweden.4 aut0 (Swepub:su)fthor |
| 700 | 1 | a Koolmeister, Tobiasu Karolinska Institutet4 aut |
| 700 | 1 | a Martens, Ulfu Stockholms universitet,Science for Life Laboratory (SciLifeLab),Institutionen för biokemi och biofysik,Stockholm Univ, Dept Biochem & Biophys, Sci Life Lab, Biochem & Cellular Screening Facil, Solna, Sweden.4 aut0 (Swepub:su)ulma3535 |
| 700 | 1 | a Llona-Minguez, Sabinu Karolinska Inst, Dept Oncol Pathol, Sci Life Lab, Solna, Sweden.4 aut |
| 700 | 1 | a Moulson, Ruthu Karolinska Inst, Dept Oncol Pathol, Sci Life Lab, Solna, Sweden.4 aut |
| 700 | 1 | a Nordström, Helena,d 1974-u Uppsala universitet,Biokemi4 aut0 (Swepub:uu)henor020 |
| 700 | 1 | a Parrow, Vendelau Uppsala universitet,Cancerfarmakologi och beräkningsmedicin4 aut0 (Swepub:uu)venpa974 |
| 700 | 1 | a Dahllund, Leifu KTH,Läkemedelsutveckling,Science for Life Laboratory, SciLifeLab,Royal Inst Technol, Sch Engn Sci Chem Biotechnol & Hlth, Sci Life Lab, Drug Discovery & Dev Platform, Solna, Sweden.4 aut0 (Swepub:kth)u1t0erdm |
| 700 | 1 | a Sjoberg, Birgeru Karolinska Institutet4 aut |
| 700 | 1 | a Vargas, Irene L.u Karolinska Inst, Dept Oncol Pathol, Sci Life Lab, Solna, Sweden.4 aut |
| 700 | 1 | a Vo, Duy Ducu Uppsala Univ, Dept Med Chem, Sci Life Lab, Uppsala, Sweden.4 aut |
| 700 | 1 | a Wannberg, Johanu Uppsala universitet,Science for Life Laboratory, SciLifeLab,Preparativ läkemedelskemi4 aut0 (Swepub:uu)jowan133 |
| 700 | 1 | a Knapp, Stefanu Goethe Univ, Inst Pharmaceut Chem, Frankfurt, Germany.4 aut |
| 700 | 1 | a Krokan, Hans E.u Norwegian Univ Sci & Technol, Dept Canc Res & Mol Med, Trondheim, Norway.4 aut |
| 700 | 1 | a Arvidsson, Per, Iu Karolinska Inst, Dept Med Biochem & Biophys, Sci Life Lab, Drug Discovery & Dev Platform, Solna, Sweden.4 aut |
| 700 | 1 | a Scobie, Martinu Karolinska Inst, Dept Oncol Pathol, Sci Life Lab, Solna, Sweden.4 aut |
| 700 | 1 | a Meiser, Johannesu Luxembourg Inst Hlth, Dept Oncol, Canc Metab Grp, Luxembourg, Luxembourg.4 aut |
| 700 | 1 | a Stenmark, Pålu Stockholm University,Lunds universitet,Stockholms universitet,Institutionen för biokemi och biofysik,Lund University, Sweden,Stockholm Univ, Dept Biochem & Biophys, Stockholm, Sweden.;Lund Univ, Dept Expt Med Sci, Lund, Sweden.,Strukturell biokemi,Forskargrupper vid Lunds universitet,LUCC: Lunds universitets cancercentrum,Övriga starka forskningsmiljöer,Structural Biochemistry,Lund University Research Groups,LUCC: Lund University Cancer Centre,Other Strong Research Environments4 aut0 (Swepub:lu)pa4463st |
| 700 | 1 | a Berglund, Ulrika Warpmanu Karolinska Institutet4 aut |
| 700 | 1 | a Homan, Evert J.u Karolinska Institutet4 aut |
| 700 | 1 | a Helleday, Thomasu Karolinska Institutet,University of Sheffield4 aut |
| 710 | 2 | a Karolinska Institutetb Karolinska Inst, Dept Oncol Pathol, Sci Life Lab, Solna, Sweden.4 org |
| 710 | 2 | a et al. |
| 773 | 0 | t NATURE CANCERd : Springer Science and Business Media LLCg 3:2, s. 156-q 3:2<156-x 2662-1347 |
| 856 | 4 | u https://doi.org/10.1038/s43018-022-00331-yy Fulltext |
| 856 | 4 | u https://uu.diva-portal.org/smash/get/diva2:1646786/FULLTEXT01.pdfx primaryx Raw objecty fulltext:print |
| 856 | 4 | u http://dx.doi.org/10.1038/s43018-022-00331-yx freey FULLTEXT |
| 856 | 4 8 | u https://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-470347 |
| 856 | 4 8 | u https://doi.org/10.1038/s43018-022-00331-y |
| 856 | 4 8 | u https://urn.kb.se/resolve?urn=urn:nbn:se:kth:diva-310076 |
| 856 | 4 8 | u https://urn.kb.se/resolve?urn=urn:nbn:se:su:diva-203237 |
| 856 | 4 8 | u http://kipublications.ki.se/Default.aspx?queryparsed=id:148956713 |
| 856 | 4 8 | u https://lup.lub.lu.se/record/7e0eea0f-45be-41ba-8a0e-cc9ce8ca6504 |
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