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Year
Paper
2023

Discovery of Molecular Glue Degraders via Isogenic Morphological Profiling

Amanda Ng, Fabian Offensperger, Jose A Cisneros, Natalie S Scholes, Monika Malik, Ludovica Villanti, Andrea Rukavina, Evandro Ferrada, J Thomas Hannich, Anna Koren, Stefan Kubicek, Giulio Superti-Furga, Georg E Winter.
ACS Chem Biol. 2023 Dec 15;18(12):2464-2473. doi: 10.1021/acschembio.3c00598. Epub 2023 Nov 21.
Abstract: https://pubmed.ncbi.nlm.nih.gov/38098458/
2023

2,4-Dichlorophenoxyacetic Acid Induces Degeneration of mDA Neurons In Vitro

Tamara Russ, Lennart Enders, Julia M Zbiegly, Phani Sankar Potru, Johannes Wurm, Björn Spittau.
Biomedicines. 2023 Oct 24;11(11):2882. doi: 10.3390/biomedicines11112882.
Abstract: https://pubmed.ncbi.nlm.nih.gov/38001883/
2023

A conformation-locking inhibitor of SLC15A4 with TASL proteostatic anti-inflammatory activity

Andras Boeszoermenyi, Léa Bernaleau, Xudong Chen, Felix Kartnig, Min Xie, Haobo Zhang, Sensen Zhang, Maeva Delacrétaz, Anna Koren, Ann-Katrin Hopp, Vojtech Dvorak, Stefan Kubicek, Daniel Aletaha, Maojun Yang, Manuele Rebsamen, Leonhard X Heinz, Giulio Superti-Furga.
Nat Commun. 2023 Oct 20;14(1):6626. doi: 10.1038/s41467-023-42070-3.
Abstract: https://pubmed.ncbi.nlm.nih.gov/37863876/
2023

Pharmacological perturbation of the phase-separating protein SMNDC1

Lennart Enders, Marton Siklos, Jan Borggräfe, Stefan Gaussmann, Anna Koren, Monika Malik, Tatjana Tomek, Michael Schuster, Jiří Reiniš, Elisa Hahn, Andrea Rukavina, Andreas Reicher, Tamara Casteels, Christoph Bock, Georg E Winter, J Thomas Hannich, Michael Sattler, Stefan Kubicek.
Nat Commun. 2023 Aug 16;14(1):4504. doi: 10.1038/s41467-023-40124-0.
Abstract: https://pubmed.ncbi.nlm.nih.gov/37587144/
2022

Metabolic modulation of transcription: The role of one-carbon metabolism

Jung-Ming G Lin, Savvas Kourtis, Ritobrata Ghose, Natalia Pardo Lorente, Stefan Kubicek, Sara Sdelci.
Cell Chem Biol. 2022 Dec 1:S2451-9456(22)00415-9. doi: 10.1016/j.chembiol.2022.11.009. Online ahead of print.
Abstract: https://pubmed.ncbi.nlm.nih.gov/36513079/
2022

SMNDC1 links chromatin remodeling and splicing to regulate pancreatic hormone expression

Tamara Casteels, Simon Bajew, Jiří Reiniš, Lennart Enders, Michael Schuster, Frédéric Fontaine, André C Müller, Bridget K Wagner, Christoph Bock, Stefan Kubicek.
Cell Rep. 2022 Aug 30;40(9):111288. doi: 10.1016/j.celrep.2022.111288.
Abstract: https://pubmed.ncbi.nlm.nih.gov/36044849/
2022

A toolbox for class I HDACs reveals isoform specific roles in gene regulation and protein acetylation

Lena Hess, Verena Moos, Arnel A Lauber, Wolfgang Reiter, Michael Schuster, Natascha Hartl, Daniel Lackner, Thorina Boenke, Anna Koren, Paloma M Guzzardo, Brigitte Gundacker, Anna Riegler, Petra Vician, Claudia Miccolo, Susanna Leiter, Mahesh B Chandrasekharan, Terezia Vcelkova, Andrea Tanzer, Jun Qi Jun, James Bradner, Gerald Brosch, Markus Hartl, Christoph Bock, Tilmann Bürckstümmer, Stefan Kubicek, Susanna Chiocca, Srividya Bhaskara, Christian Seiser.
PLoS Genet. 2022 Aug 22;18(8):e1010376. doi: 10.1371/journal.pgen.1010376. eCollection 2022 Aug.
Abstract: https://pubmed.ncbi.nlm.nih.gov/35994477/
2022

Molecular and Pharmacological Bladder Cancer Therapy Screening: Discovery of Clofarabine as a Highly Active Compound

Iris E Ertl, Ursula Lemberger, Dafina Ilijazi, Melanie R Hassler, Andreas Bruchbacher, Robert Brettner, Hannah Kronabitter, Michael Gutmann, Petra Vician, Gerhard Zeitler, Anna Koren, Charles-Hugues Lardeau, Thomas Mohr, Andrea Haitel, Eva Compérat, André Oszwald, Gabriel Wasinger, Thomas Clozel, Olivier Elemento, Stefan Kubicek, Walter Berger, Shahrokh F Shariat.
Eur Urol. 2022 Sep;82(3):261-270. doi: 10.1016/j.eururo.2022.03.009. Epub 2022 Apr 4.
Abstract: https://pubmed.ncbi.nlm.nih.gov/35393162/
2022

Oncogenic TYK2P760L kinase is effectively targeted by combinatorial TYK2, mTOR and CDK4/6 kinase blockade

Katharina Woess, Sabine Macho-Maschler, Dorette S Van Ingen Schenau, Miriam Butler, Caroline Lassnig, Daniel Valcanover, Andrea Poelzl, Katrin Meissl, Barbara Maurer, Tania Brandstoetter, Claus Vogl, Anna Koren, Stefan Kubicek, Anna Orlova, Richard Moriggl, Birgit Strobl, Veronika Sexl, Frank N Van Leeuwen, Roland P Kuiper, Mathias Mueller.
Haematologica. 2022 Jan 13. doi: 10.3324/haematol.2021.279848. Online ahead of print.
Abstract: https://pubmed.ncbi.nlm.nih.gov/35021603/
Year
Paper
2021
Grosche S, Marenholz I, Esparza-Gordillo J, Arnau-Soler A, Pairo-Castineira E, Rüschendorf F, Ahluwalia TS, Almqvist C, Arnold A; Australian Asthma Genetics Consortium (AAGC), Baurecht H, Bisgaard H, Bønnelykke K, Brown SJ, Bustamante M, Curtin JA, Custovic A, Dharmage SC, Esplugues A, Falchi M, Fernandez-Orth D, Ferreira MAR, Franke A, Gerdes S, Gieger C, Hakonarson H, Holt PG, Homuth G, Hubner N, Hysi PG, Jarvelin MR, Karlsson R, Koppelman GH, Lau S, Lutz M, Magnusson PKE, Marks GB, Müller-Nurasyid M, Nöthen MM, Paternoster L, Pennell CE, Peters A, Rawlik K, Robertson CF, Rodriguez E, Sebert S, Simpson A, Sleiman PMA, Standl M, Stölzl D, Strauch K, Szwajda A, Tenesa A, Thompson PJ, Ullemar V, Visconti A, Vonk JM, Wang CA, Weidinger S, Wielscher M, Worth CL, Xu CJ, Lee YA. Rare variant analysis in eczema identifies exonic variants in DUSP1, NOTCH4 and SLC9A4. Nat Commun. 2021 Nov 16;12(1):6618. doi: 10.1038/s41467-021-26783-x.
Abstract: https://pubmed.ncbi.nlm.nih.gov/34785669/
2021
Bolomsky A, Miettinen JJ, Malyutina A, Besse A, Huber J, Fellinger S, Breid H, Parsons A, Klavins K, Hannich JT, Kubicek S, Caers J, Hübl W, Schreder M, Zojer N, Driessen C, Tang J, Besse L, Heckman CA, Ludwig H. Heterogeneous modulation of Bcl-2 family members and drug efflux mediate MCL-1 inhibitor resistance in multiple myeloma. Blood Adv. 2021 Oct 26;5(20):4125-4139. doi: 10.1182/bloodadvances.2020003826.
Abstract: https://pubmed.ncbi.nlm.nih.gov/34478517/
2021
Casteels T, Zhang Y, Frogne T, Sturtzel C, Lardeau CH, Sen I, Liu X, Hong S, Pauler FM, Penz T, Brandstetter M, Barbieux C, Berishvili E, Heuser T, Bock C, Riedel CG, Meyer D, Distel M, Hecksher-Sørensen J, Li J, Kubicek S. An inhibitor-mediated beta-cell dedifferentiation model reveals distinct roles for FoxO1 in glucagon repression and insulin maturation. Mol Metab. 2021 Dec;54:101329. doi: 10.1016/j.molmet.2021.101329. Epub 2021 Aug 25.
Abstract: https://pubmed.ncbi.nlm.nih.gov/34454092/
2021
Cadena Del Castillo CE, Hannich JT, Kaech A, Chiyoda H, Brewer J, Fukuyama M, Færgeman NJ, Riezman H, Spang A. Patched regulates lipid homeostasis by controlling cellular cholesterol levels. Nat Commun. 2021 Aug 12;12(1):4898. doi: 10.1038/s41467-021-24995-9.
Abstract: https://pubmed.ncbi.nlm.nih.gov/34385431/
2021
Baumgartner M, Lang M, Holley H, Crepaz D, Hausmann B, Pjevac P, Moser D, Haller F, Hof F, Beer A, Orgler E, Frick A, Khare V, Evstatiev R, Strohmaier S, Primas C, Dolak W, Köcher T, Klavins K, Rath T, Neurath MF, Berry D, Makristathis A, Muttenthaler M, Gasche C. Mucosal Biofilms Are an Endoscopic Feature of Irritable Bowel Syndrome and Ulcerative Colitis. Gastroenterology. 2021 Oct;161(4):1245-1256.e20. doi: 10.1053/j.gastro.2021.06.024.2021 Jun 17.
Abstract: https://pubmed.ncbi.nlm.nih.gov/34146566/
2021
Amaya-García F, Caldera M, Koren A, Kubicek S, Menche J, Unterlass MM. Green Hydrothermal Synthesis of Fluorescent 2,3-Diarylquinoxalines and Large-Scale Computational Comparison to Existing Alternatives. ChemSusChem. 2021 Apr 22;14(8):1780. doi: 10.1002/cssc.202100607.
Abstract: https://pubmed.ncbi.nlm.nih.gov/33855809/ _blank
2021
Subtelna I, Kryshchyshyn-Dylevych A, Jia R, Lelyukh M, Ringler A, Kubicek S, Zagrijtschuk O, Kralovics R, Lesyk R. 5-Arylidene-2-(4-hydroxyphenyl)aminothiazol-4(5H)-ones with selective inhibitory activity against some leukemia cell lines. Arch Pharm (Weinheim). 2021 Apr;354(4):e2000342. doi: 10.1002/ardp.202000342. Epub 2020 Nov 25.
Abstract: https://pubmed.ncbi.nlm.nih.gov/33241558/
2021
Swoboda A, Soukup R, Eckel O, Kinslechner K, Wingelhofer B, Schörghofer D, Sternberg C, Pham HTT, Vallianou M, Horvath J, Stoiber D, Kenner L, Larue L, Poli V, Beermann F, Yokota T, Kubicek S, Krausgruber T, Rendeiro AF, Bock C, Zenz R, Kovacic B, Aberger F, Hengstschläger M, Petzelbauer P, Mikula M, Moriggl R. STAT3 promotes melanoma metastasis by CEBP-induced repression of the MITF pathway. Oncogene. 2021 Feb;40(6):1091-1105. doi: 10.1038/s41388-020-01584-6. Epub 2020 Dec 15.
Abstract: https://pubmed.ncbi.nlm.nih.gov/33323974/
2021
Schick S, Grosche S, Kohl KE, Drpic D, Jaeger MG, Marella NC, Imrichova H, Lin JG, Hofstätter G, Schuster M, Rendeiro AF, Koren A, Petronczki M, Bock C, Müller AC, Winter GE, Kubicek S. Acute BAF perturbation causes immediate changes in chromatin accessibility. Nat Genet. 2021 Mar;53(3):269-278. doi: 10.1038/s41588-021-00777-3. Epub 2021 Feb 8.
Abstract: https://pubmed.ncbi.nlm.nih.gov/33558760/
2021
Valent P, Orfao A, Kubicek S, Staber P, Haferlach T, Deininger M, Kollmann K, Lion T, Virgolini I, Winter G, Hantschel O, Kenner L, Zuber J, Grebien F, Moriggl R, Hoermann G, Hermine O, Andreeff M, Bock C, Mughal T, Constantinescu SN, Kralovics R, Sexl V, Skoda R, Superti-Furga G, Jäger U. Precision Medicine in Hematology 2021: Definitions, Tools, Perspectives, and Open Questions. Hemasphere. 2021 Feb 17;5(3):e536. doi: 10.1097/HS9.0000000000000536. eCollection 2021 Mar.
Abstract: https://pubmed.ncbi.nlm.nih.gov/33623882/
2021
Mayor-Ruiz C, Bauer S, Brand M, Kozicka Z, Siklos M, Imrichova H, Kaltheuner IH, Hahn E, Seiler K, Koren A, Petzold G, Fellner M, Bock C, Müller AC, Zuber J, Geyer M, Thomä NH, Kubicek S, Winter GE. Publisher Correction: Rational discovery of molecular glue degraders via scalable chemical profiling. Nat Chem Biol. 2021 Mar;17(3):361. doi: 10.1038/s41589-021-00735-4.
Abstract: https://pubmed.ncbi.nlm.nih.gov/33452497/
2021
Jia R, Balligand T, Atamanyuk V, Nivarthi H, Xu E, Kutzner L, Weinzierl J, Nedelec A, Kubicek S, Lesyk R, Zagrijtschuk O, Constantinescu SN, Kralovics R. Hematoxylin binds to mutant calreticulin and disrupts its abnormal interaction with thrombopoietin receptor. Blood. 2021 Apr 8;137(14):1920-1931. doi: 10.1182/blood.2020006264.
Abstract: https://pubmed.ncbi.nlm.nih.gov/33202418/
2020
Ferreira MAR, Vonk JM, Baurecht H, Marenholz I, Tian C, Hoffman JD, Helmer Q, Tillander A, Ullemar V, Lu Y, Grosche S, Rüschendorf F, Granell R, Brumpton BM, Fritsche LG, Bhatta L, Gabrielsen ME, Nielsen JB, Zhou W, Hveem K, Langhammer A, Holmen OL, Løset M, Abecasis GR, Willer CJ, Emami NC, Cavazos TB, Witte JS, Szwajda A; 23andMe Research Team; collaborators of the SHARE study, Hinds DA, Hübner N, Weidinger S, Magnusson PK, Jorgenson E, Karlsson R, Paternoster L, Boomsma DI, Almqvist C, Lee YA, Koppelman GH. Age-of-onset information helps identify 76 genetic variants associated with allergic disease. PLoS Genet. 2020 Jun 30;16(6):e1008725. doi: 10.1371/journal.pgen.1008725.
Abstract: https://pubmed.ncbi.nlm.nih.gov/32603359/
2020
Mayor-Ruiz C, Bauer S, Brand M, Kozicka Z, Siklos M, Imrichova H, Kaltheuner IH, Hahn E, Seiler K, Koren A, Petzold G, Fellner M, Bock C, Müller AC, Zuber J, Geyer M, Thomä NH, Kubicek S, Winter GE. Rational discovery of molecular glue degraders via scalable chemical profiling. Nat Chem Biol. 2020 Nov;16(11):1199-1207. doi: 10.1038/s41589-020-0594-x. Epub 2020 Aug 3. Erratum in: Nat Chem Biol. 2021 Mar;17(3):361.
Abstract: https://pubmed.ncbi.nlm.nih.gov/32747809/
2020
Subtelna I, Kryshchyshyn-Dylevych A, Jia R, Lelyukh M, Ringler A, Kubicek S, Zagrijtschuk O, Kralovics R, Lesyk R. 5-Arylidene-2-(4-hydroxyphenyl)aminothiazol-4(5H)-ones with selective inhibitory activity against some leukemia cell lines. Arch Pharm (Weinheim). 2021 Apr;354(4):e2000342. doi: 10.1002/ardp.202000342. Epub 2020 Nov 25.
Abstract: https://pubmed.ncbi.nlm.nih.gov/33241558/
2020
Swoboda A, Soukup R, Eckel O, Kinslechner K, Wingelhofer B, Schörghofer D, Sternberg C, Pham HTT, Vallianou M, Horvath J, Stoiber D, Kenner L, Larue L, Poli V, Beermann F, Yokota T, Kubicek S, Krausgruber T, Rendeiro AF, Bock C, Zenz R, Kovacic B, Aberger F, Hengstschläger M, Petzelbauer P, Mikula M, Moriggl R. STAT3 promotes melanoma metastasis by CEBP-induced repression of the MITF pathway. Oncogene. 2021 Feb;40(6):1091-1105. doi: 10.1038/s41388-020-01584-6. Epub 2020 Dec 15.
Abstract: https://pubmed.ncbi.nlm.nih.gov/33323974/
2020
Reicher A, Koren A, Kubicek S. Pooled protein tagging, cellular imaging, and in situ sequencing for monitoring drug action in real time. Genome Res. 2020 Dec;30(12):1846-1855. doi: 10.1101/gr.261503.120. Epub 2020 Nov 17.
Abstract: https://pubmed.ncbi.nlm.nih.gov/33203764/
2020
Maurer B, Nivarthi H, Wingelhofer B, Pham HTT, Schlederer M, Suske T, Grausenburger R, Schiefer AI, Prchal-Murphy M, Chen D, Winkler S, Merkel O, Kornauth C, Hofbauer M, Hochgatterer B, Hoermann G, Hoelbl-Kovacic A, Prochazkova J, Lobello C, Cumaraswamy AA, Latzka J, Kitzwögerer M, Chott A, Janikova A, Pospíšilova Š, Loizou JI, Kubicek S, Valent P, Kolbe T, Grebien F, Kenner L, Gunning PT, Kralovics R, Herling M, Müller M, Rülicke T, Sexl V, Moriggl R. High activation of STAT5A drives peripheral T-cell lymphoma and leukemia. Haematologica. 2020 Jan 31;105(2):435-447. doi: 10.3324/haematol.2019.216986.
Abstract: https://www.ncbi.nlm.nih.gov/pubmed/31123029
2020
Marquina-Sanchez B, Fortelny N, Farlik M, Vieira A, Collombat P, Bock C, Kubicek S. Single-cell RNA-seq with spike-in cells enables accurate quantification of cell-specific drug effects in pancreatic islets. Genome Biol. 2020 May 6;21(1):106. doi: 10.1186/s13059-020-02006-2.
Abstract: https://www.ncbi.nlm.nih.gov/pubmed/32375897
2020
Girardi E, César-Razquin A, Lindinger S, Papakostas K, Konecka J, Hemmerich J, Kickinger S, Kartnig F, Gürtl B, Klavins K, Sedlyarov V, Ingles-Prieto A, Fiume G, Koren A, Lardeau CH, Kumaran Kandasamy R, Kubicek S, Ecker GF, Superti-Furga G. A widespread role for SLC transmembrane transporters in resistance to cytotoxic drugs. Nat Chem Biol. 2020 Apr;16(4):469-478. doi: 10.1038/s41589-020-0483-3. Epub 2020 Mar 9.
Abstract: https://www.ncbi.nlm.nih.gov/pubmed/32152546
2019
Schick S, Rendeiro AF, Runggatscher K, Ringler A, Boidol B, Hinkel M, Májek P, Vulliard L, Penz T, Parapatics K, Schmidl C, Menche J, Boehmelt G, Petronczki M, Müller AC, Bock C, Kubicek S. Systematic characterization of BAF mutations provides insights into intracomplex synthetic lethalities in human cancers. Nat Genet. 2019;51(9):1399–1410. doi:10.1038/s41588-019-0477-9
Abstract: https://pubmed.ncbi.nlm.nih.gov/31427792/
2019
Chien J, Wolf FW, Grosche S, Yosef N, Garriga G, Mörck C. The Enigmatic Canal-Associated Neurons Regulate Caenorhabditis elegans Larval Development Through a cAMP Signaling Pathway. Genetics. 2019 Dec;213(4):1465-1478. doi: 10.1534/genetics.119.302628.
Abstract: https://pubmed.ncbi.nlm.nih.gov/31619445/
2019
Chen Y, Coussanes G, Souris C, Aillard P, Kaldre D, Runggatscher K, Kubicek S, Di Mauro G, Maryasin B, Maulide N. A Domino 10-Step Total Synthesis of FR252921 and Its Analogues, Complex Macrocyclic Immunosuppressants. J Am Chem Soc. 2019 Sep 4;141(35):13772-13777. doi: 10.1021/jacs.9b07185.
Abstract: https://pubmed.ncbi.nlm.nih.gov/31436963/
2019
Caldera M, Müller F, Kaltenbrunner I, Licciardello MP, Lardeau CH, Kubicek S, Menche J. Mapping the perturbome network of cellular perturbations. Nat Commun. 2019 Nov 13;10(1):5140. doi: 10.1038/s41467-019-13058-9.
Abstract: https://pubmed.ncbi.nlm.nih.gov/31723137/
2019
Staber PB, Herling M, Bellido M, Jacobsen ED, Davids MS, Kadia TM, Shustov A,Tournilhac O, Bachy E, Zaja F, Porkka K, Hoermann G, Simonitsch I, Haferlach C,Kubicek S, Mayerhoefer M, Hopfinger G, Jaeger U, Dearden C. Consensus criteria for diagnosis, staging, and treatment response assessment of T-cell prolymphocytic leukemia (T-PLL). Blood. 2019 Jul 10. pii: blood.2019000402. doi: 10.1182/blood.2019000402. [Epub ahead of print]
Abstract: https://www.ncbi.nlm.nih.gov/pubmed/31292114
2019
Sdelci S, Rendeiro AF, Rathert P, You W, Lin JG, Ringler A, Hofstätter G,Moll HP, Gürtl B, Farlik M, Schick S, Klepsch F, Oldach M, Buphamalai P,Schischlik F, Májek P, Parapatics K, Schmidl C, Schuster M, Penz T, Buckley DL,Hudecz O, Imre R, Wang SY, Maric HM, Kralovics R, Bennett KL, Müller AC, MechtlerK, Menche J, Bradner JE, Winter GE, Klavins K, Casanova E, Bock C, Zuber J,Kubicek S. MTHFD1 interaction with BRD4 links folate metabolism to transcriptional regulation. Nat Genet. 2019 Jun;51(6):990-998. doi:10.1038/s41588-019-0413-z. Epub 2019 May 27.
Abstract: https://www.ncbi.nlm.nih.gov/pubmed/31133746
2019
Schmidl C, Vladimer GI, Rendeiro AF, Schnabl S, Krausgruber T, Taubert C,Krall N, Pemovska T, Araghi M, Snijder B, Hubmann R, Ringler A, Runggatscher K,Demirtas D, de la Fuente OL, Hilgarth M, Skrabs C, Porpaczy E, Gruber M, HoermannG, Kubicek S, Staber PB, Shehata M, Superti-Furga G, Jäger U, Bock C. Combined chemosensitivity and chromatin profiling prioritizes drug combinations in CLL. Nat Chem Biol. 2019 Mar;15(3):232-240. doi: 10.1038/s41589-018-0205-2. Epub 2019 Jan 28.
Abstract: https://www.ncbi.nlm.nih.gov/pubmed/30692684
2019
Owusu M, Bannauer P, Ferreira da Silva J, Mourikis TP, Jones A, Májek P,Caldera M, Wiedner M, Lardeau CH, Mueller AC, Menche J, Kubicek S, Ciccarelli FD,Loizou JI. Mapping the Human Kinome in Response to DNA Damage. Cell Rep. 2019 Jan15;26(3):555-563.e6. doi: 10.1016/j.celrep.2018.12.087.
Abstract: https://www.ncbi.nlm.nih.gov/pubmed/30650350
2019
Moik F, Riedl JM, Winder T, Terbuch A, Rossmann CH, Szkandera J, Bauernhofer T, Kasparek AK, Schaberl-Moser R, Reicher A, Prinz F, Pichler M, Stöger H, Stotz M, Gerger A, Posch F. Benefit of second-line systemic chemotherapy for advanced biliary tract cancer: A propensity score analysis. Sci Rep. 2019 Apr 3;9(1):5548.doi: 10.1038/s41598-019-42069-1.
Abstract: https://www.ncbi.nlm.nih.gov/pubmed/30944390
2019
Maurer B, Nivarthi H, Wingelhofer B, Pham HTT, Schlederer M, Suske T,Grausenburger R, Schiefer AI, Prchal-Murphy M, Chen D, Winkler S, Merkel O,Kornauth C, Hofbauer M, Hochgatterer B, Hoermann G, Hoelbl-Kovacic A, ProchazkovaJ, Lobello C, Cumaraswamy AA, Latzka J, Kitzwögerer M, Chott A, Janikova A,Pospíšilova Š, Loizou JI, Kubicek S, Valent P, Kolbe T, Grebien F, Kenner L,Gunning PT, Kralovics R, Herling M, Müller M, Rülicke T, Sexl V, Moriggl R. High activation of STAT5A drives peripheral T-cell lymphoma and leukemia.Haematologica. 2019 May 23. pii: haematol.2019.216986. doi:10.3324/haematol.2019.216986. [Epub ahead of print]
Abstract: https://www.ncbi.nlm.nih.gov/pubmed/31123029
2019
Kosack L, Wingelhofer B, Popa A, Orlova A, Agerer B, Vilagos B, Majek P,Parapatics K, Lercher A, Ringler A, Klughammer J, Smyth M, Khamina K, Baazim H,de Araujo ED, Rosa DA, Park J, Tin G, Ahmar S, Gunning PT, Bock C, Siddle HV,Woods GM, Kubicek S, Murchison EP, Bennett KL, Moriggl R, Bergthaler A. The ERBB-STAT3 Axis Drives Tasmanian Devil Facial Tumor Disease. Cancer Cell. 2019Jan 14;35(1):125-139.e9. doi: 10.1016/j.ccell.2018.11.018.
Abstract: https://www.ncbi.nlm.nih.gov/pubmed/30645971
2018
Saulnier-Blache JS, Wilson R, Klavins K, Graham D, Alesutan I, Kastenmüller G, Wang-Sattler R, Adamski J, Roden M, Rathmann W, Seissler J, Meisinger C, Koenig W, Thiery J, Suhre K, Peters A, Kuro-O M, Lang F, Dallmann G, Delles C, Voelkl J, Waldenberger M, Bascands JL, Klein J, Schanstra JP. Ldlr(-)(/)(-) and ApoE(-)(/)(-) mice better mimic the human metabolite signature of increased carotid intima media thickness compared to other animal models of cardiovascular disease. Atherosclerosis. 2018 Sep;276:140-147. doi: 10.1016/j.atherosclerosis.2018.07.024. Epub 2018 Jul 21.
Abstract: https://www.ncbi.nlm.nih.gov/pubmed/30059845
2018
Brown M, Johnson LA, Leone DA, Majek P, Vaahtomeri K, Senfter D, Bukosza N, Schachner H, Asfour G, Langer B, Hauschild R, Parapatics K, Hong YK, Bennett KL, Kain R, Detmar M, Sixt M, Jackson DG, Kerjaschki D. Lymphatic exosomes promote dendritic cell migration along guidance cues. J Cell Biol. 2018 Jun 4;217(6):2205-2221. doi: 10.1083/jcb.201612051. Epub 2018 Apr 12.
Abstract: https://www.ncbi.nlm.nih.gov/pubmed/29650776
2018
Wingelhofer B, Maurer B, Heyes EC, Cumaraswamy AA, Berger-Becvar A, de Araujo ED, Orlova A, Freund P, Ruge F, Park J, Tin G, Ahmar S, Lardeau CH, Sadovnik I, Bajusz D, Keserű GM, Grebien F, Kubicek S, Valent P, Gunning PT, Moriggl R. Pharmacologic inhibition of STAT5 in acute myeloid leukemia. Leukemia. 2018 May;32(5):1135-1146. doi: 10.1038/s41375-017-0005-9. Epub 2018 Feb 2.
Abstract: https://www.ncbi.nlm.nih.gov/pubmed/29472718
2018
Bellutti F, Tigan AS, Nebenfuehr S, Dolezal M, Zojer M, Grausenburger R, Hartenberger S, Kollmann S, Doma E, Prchal-Murphy M, Uras IZ, Höllein A, Neuberg DS, Ebert BL, Ringler A, Mueller AC, Loizou JI, Hinds PW, Vogl C, Heller G, Kubicek S, Zuber J, Malumbres M, Farlik M, Villunger A, Kollmann K, Sexl V. CDK6 antagonizes p53-induced responses during tumorigenesis. Cancer Discov. 2018 Jun 13. pii: CD-17-0912. doi: 10.1158/2159-8290.CD-17-0912. [Epub ahead of print]
Abstract: https://www.ncbi.nlm.nih.gov/pubmed/29899063
2017
Mazouzi A, Battistini F, Moser SC, Ferreira da Silva J, Wiedner M, Owusu M, Lardeau CH, Ringler A, Weil B, Neesen J, Orozco M, Kubicek S, Loizou JI. Repair of UV-Induced DNA Damage Independent of Nucleotide Excision Repair Is Masked by MUTYH. Mol Cell. 2017 Nov 16;68(4):797-807.e7. doi: 10.1016/j.molcel.2017.10.021
Abstract: http://www.cell.com/molecular-cell/comments/S1097-2765(17)30796-7
2017
Uras IZ, Scheicher RM, Kollmann K, Glösmann M, Prchal-Murphy M, Tigan AS, Fux DA, Altamura S, Neves J, Muckenthaler MU, Bennett KL, Kubicek S, Hinds PW, von Lindern M, Sexl V. Cdk6 contributes to cytoskeletal stability in erythroid cells. Haematologica. 2017 Jun;102(6):995-1005. doi: 10.3324/haematol.2016.159947. Epub 2017 Mar 2.
Abstract: https://www.ncbi.nlm.nih.gov/pubmed/28255017
2017
Valent P, Herndlhofer S, Schneeweiß M, Boidol B, Ringler A, Kubicek S, Gleixner KV, Hoermann G, Hadzijusufovic E, Müllauer L, Sperr WR, Superti-Furga G, Mannhalter C. TKI rotation-induced persistent deep molecular response in multi-resistant blast crisis of Ph+ CML. Oncotarget. 2017 Apr 4;8(14):23061-23072. doi: 10.18632/oncotarget.15481.
Abstract: https://www.ncbi.nlm.nih.gov/pubmed/28416739
2017
Vladimer GI, Snijder B, Krall N, Bigenzahn JW, Huber KVM, Lardeau CH, Sanjiv K, Ringler A, Berglund UW, Sabler M, de la Fuente OL, Knöbl P, Kubicek S, Helleday T, Jäger U, Superti-Furga G. Global survey of the immunomodulatory potential of common drugs. Nat Chem Biol. 2017 Jun;13(6):681-690. doi: 10.1038/nchembio.2360. Epub 2017 Apr 24.
Abstract: https://www.ncbi.nlm.nih.gov/pubmed/28437395
2017
Licciardello MP, Ringler A, Markt P, Klepsch F, Lardeau CH, Sdelci S, Schirghuber E, Müller AC, Caldera M, Wagner A, Herzog R, Penz T, Schuster M, Boidol B, Dürnberger G, Folkvaljon Y, Stattin P, Ivanov V, Colinge J, Bock C, Kratochwill K, Menche J, Bennett KL, Kubicek S. A combinatorial screen of the CLOUD uncovers a synergy targeting the androgen receptor. Nat Chem Biol. 2017 Jul;13(7):771-778. doi: 10.1038/nchembio.2382. Epub 2017 May 22.
Abstract: https://www.ncbi.nlm.nih.gov/pubmed/28530711
2017
Malenczyk K, Girach F, Szodorai E, Storm P, Segerstolpe Å, Tortoriello G, Schnell R, Mulder J, Romanov RA, Borók E, Piscitelli F, Di Marzo V, Szabó G, Sandberg R, Kubicek S, Lubec G, Hökfelt T, Wagner L, Groop L, Harkany T. A TRPV1-to-secretagogin regulatory axis controls pancreatic β-cell survival by modulating protein turnover. EMBO J. 2017 Jul 14;36(14):2107-2125. doi: 10.15252/embj.201695347. Epub 2017 Jun 21.
Abstract: https://www.ncbi.nlm.nih.gov/pubmed/28637794
2017
Kostrhon S, Kontaxis G, Kaufmann T, Schirghuber E, Kubicek S, Konrat R, Slade D. A histone-mimicking interdomain linker in a multidomain protein modulates multivalent histone binding. J Biol Chem. 2017 Oct 27;292(43):17643-17657. doi: 10.1074/jbc.M117.801464. Epub 2017 Sep 1.
Abstract: https://www.ncbi.nlm.nih.gov/pubmed/28864776
2017
Boidol B, Kornauth C, van der Kouwe E, Prutsch N, Kazianka L, Gültekin S, Hoermann G, Mayerhoefer ME, Hopfinger G, Hauswirth A, Panny M, Aretin MB, Hilgarth B, Sperr WR, Valent P, Simonitsch-Klupp I, Moriggl R, Merkel O, Kenner L, Jäger U, Kubicek S, Staber PB. First in human response of BCL-2 inhibitor venetoclax in T-cell prolymphocytic leukemia. Blood. 2017 Sep 27. pii: blood-2017-05-785683. doi: 10.1182/blood-2017-05-785683. [Epub ahead of print]
Abstract: https://www.ncbi.nlm.nih.gov/pubmed/28972014
2016
Li J, Casteels T, Frogne T, Ingvorsen C, Honoré C, Courtney M, Huber KVM, Schmitner N, Kimmel RA, Romanov RA, Sturtzel C, Lardeau CH, Klughammer J, Farlik M, Sdelci S, Vieira A, Avolio F, Briand F, Baburin I, Májek P, Pauler FM, Penz T, Stukalov A, Gridling M, Parapatics K, Barbieux C, Berishvili E, Spittler A, Colinge J, Bennett KL, Hering S, Sulpice T, Bock C, Distel M, Harkany T, Meyer D, Superti-Furga G, Collombat P, Hecksher-Sørensen J, and Kubicek S. Artemisinins Target GABAA Receptor Signaling and Impair α Cell Identity, Cell 2017 Jan 12 (epub ahead of print 2016 Dec 1);168(1), 86-100. doi:10.1016/j.cell.2016.11.010.Abstract: http://www.cell.com/cell/abstract/S0092-8674(16)31531-8
2016
Guryanova OA, Shank K, Spitzer B, Luciani L, Koche RP, Garrett-Bakelman FE, Ganzel C, Durham BH, Mohanty A, Hoermann G, Rivera SA, Chramiec AG, Pronier E, Bastian L, Keller MD, Tovbin D, Loizou E, Weinstein AR, Gonzalez AR, Lieu YK, Rowe JM, Pastore F, McKenney AS, Krivtsov AV, Sperr WR, Cross JR, Mason CE, Tallman MS, Arcila ME, Abdel-Wahab O, Armstrong SA, Kubicek S, Staber PB, Gönen M, Paietta EM, Melnick AM, Nimer SD, Mukherjee S, Levine RL. DNMT3A mutations promote anthracycline resistance in acute myeloid leukemia via impaired nucleosome remodeling. Nat Med. 2016 Dec;22(12):1488-1495. doi: 10.1038/nm.4210.
Abstract: http://www.nature.com/nm/journal/v22/n12/full/nm.4210.html
2016
Vitko D, Májek P, Schirghuber E, Kubicek S, Bennett KL. FASIL-MS: An Integrated Proteomic and Bioinformatic Workflow To Universally Quantitate In Vivo-Acetylated Positional Isomers. J Proteome Res. 2016 Aug 5;15(8):2579-94. doi: 10.1021/acs.jproteome.6b00130.
Abstract: http://www.ncbi.nlm.nih.gov/pubmed/27302567
2016
Uras IZ, Walter GJ, Scheicher R, Bellutti F, Prchal-Murphy M, Tigan AS, Valent P, Heidel FH, Kubicek S, Scholl C, Fröhling S, Sexl V. Palbociclib treatment of FLT3-ITD+ AML cells uncovers a kinase-dependent transcriptional regulation of FLT3 and PIM1 by CDK6. Blood. 2016 Apr 20. pii: blood-2015-11-683581.
Abstract: http://www.ncbi.nlm.nih.gov/pubmed/27099147
2016
Sdelci S, Lardeau CH, Tallant C, Klepsch F, Klaiber B, Bennett J, Rathert P, Schuster M, Penz T, Fedorov O, Superti-Furga G, Bock C, Zuber J, Huber KV, Knapp S, Müller S, Kubicek S. Mapping the chemical chromatin reactivation landscape identifies BRD4-TAF1 cross-talk. Nat Chem Biol. 2016 May 9. doi: 10.1038/nchembio.2080.
Abstract: http://www.ncbi.nlm.nih.gov/pubmed/27159579
2016
Licciardello MP, Kubicek S. Pharmacological treats for SUMO addicts. Pharmacol Res. 2016 Jan 24. pii: S1043-6618(16)30009-3. doi: 10.1016/j.phrs.2016.01.004.
Abstract: http://www.ncbi.nlm.nih.gov/pubmed/26816086
2016
Englinger B, Lötsch D, Pirker C, Mohr T, van Schoonhoven S, Boidol B, Lardeau CH, Spitzwieser M, Szabó P, Heffeter P, Lang I, Cichna-Markl M, Grasl-Kraupp B, Marian B, Grusch M, Kubicek S, Szakács G, Berger W. Acquired nintedanib resistance in FGFR1-driven small cell lung cancer: role of endothelin-A receptor-activated ABCB1 expression. Oncotarget. 2016 Jun 29. doi: 10.18632/oncotarget.10324.
Abstract: http://www.ncbi.nlm.nih.gov/pubmed/27367030
2015
Licciardello MP, Müllner MK, Dürnberger G, Kerzendorfer C, Boidol B, Trefzer C, Sdelci S, Berg T, Penz T, Schuster M, Bock C, Kralovics R, Superti-Furga G, Colinge J, Nijman SM, Kubicek S. NOTCH1 activation in breast cancer confers sensitivity to inhibition of SUMOylation. Oncogene. 2015 Jul;34(29):3780-90. doi: 10.1038/onc.2014.319. Epub 2014 Sep 29.
Abstract: http://www.ncbi.nlm.nih.gov/pubmed/25263445
2015
Li J, Klughammer J, Farlik M, Penz T, Spittler A, Barbieux C, Berishvili E, Bock C, Kubicek S. Single-cell transcriptomes reveal characteristic features of human pancreatic islet cell types. EMBO Rep. 2016 Feb. Epub 2015 Dec 21.
Abstract: https://www.ncbi.nlm.nih.gov/pubmed/26691212
2015
Herzog VA, Lempradl A, Trupke J, Okulski H, Altmutter C, Ruge F, Boidol B, Kubicek S, Schmauss G, Aumayr K, Ruf M, Pospisilik A, Dimond A, Senergin HB, Vargas ML, Simon JA, Ringrose L. A strand-specific switch in noncoding transcription switches the function of a Polycomb/Trithorax response element. Nat Genet. 2014 Sep;46(9):973-81. doi: 10.1038/ng.3058. Epub 2014 Aug 10.
Abstract: http://www.ncbi.nlm.nih.gov/pubmed/25108384
2015
Bentires-Alj M, Rajan A, van Harten W, van Luenen HG, Kubicek S, Andersen JB, Saarela J, Cook SJ, Van Minnebruggen G, Roman-Roman S, Maurer C, Erler JT, Bertero MG. Stimulating translational research: several European life science institutions put their heads together. Trends Mol Med. 2015 Sep;21(9):525-7. doi: 10.1016/j.molmed.2015.07.002. Epub 2015 Aug 5.
Abstract: http://www.ncbi.nlm.nih.gov/pubmed/26254816
2015
Muellner MK, Mair B, Ibrahim Y, Kerzendorfer C, Lechtermann H, Trefzer C, Klepsch F, Müller AC, Leitner E, Macho-Maschler S, Superti-Furga G, Bennett KL, Baselga J, Rix U, Kubicek S, Colinge J, Serra V, Nijman SM. Targeting a cell state common to triple-negative breast cancers. Mol Syst Biol. 2015 Feb 19;11(1):789. doi: 10.15252/msb.20145664.
Abstract: http://www.ncbi.nlm.nih.gov/pubmed/25699542
2014
Herzog VA, Lempradl A, Trupke J, Okulski H, Altmutter C, Ruge F, Boidol B, Kubicek S, Schmauss G, Aumayr K, Ruf M, Pospisilik A, Dimond A, Senergin HB, Vargas ML, Simon JA, Ringrose L. A strand-specific switch in noncoding transcription switches the function of a Polycomb/Trithorax response element. Nat Genet. 2014 Sep;46(9):973-81. doi: 10.1038/ng.3058. Epub 2014 Aug 10.
Abstract: http://www.ncbi.nlm.nih.gov/pubmed/25108384
2014
Choudhary A, Hu He K, Mertins P, Udeshi ND, Dančík V, Fomina-Yadlin D, Kubicek S, Clemons PA, Schreiber SL, Carr SA, Wagner BK. Quantitative-proteomic comparison of alpha and Beta cells to uncover novel targets for lineage reprogramming. PLoS One. 2014 Apr 23;9(4):e95194. doi: 10.1371/journal.pone.0095194.
Abstract: http://www.plosone.org/article/info%3Adoi%2F10.1371%2Fjournal.pone.0095194
2014
Berger A, Hoelbl-Kovacic A, Bourgeais J, Hoefling L, Warsch W, Grundschober E, Uras IZ, Menzl I, Putz EM, Hoermann G, Schuster C, Fajmann S, Leitner E, Kubicek S, Moriggl R, Gouilleux F, Sexl V. PAK-dependent STAT5 serine phosphorylation is required for BCR-ABL-induced leukemogenesis. Leukemia. 2014 Mar;28(3):629-41. doi: 10.1038/leu.2013.351. Epub 2013 Nov 22.
Abstract: http://www.ncbi.nlm.nih.gov/pubmed/24263804
2014
Mair B, Kubicek S, Nijman SM. Exploiting epigenetic vulnerabilities for cancer therapeutics. Trends Pharmacol Sci. 2014 Mar;35(3):136-145. doi: 10.1016/j.tips.2014.01.001. Epub 2014 Feb 12. Review.
Abstract: http://www.ncbi.nlm.nih.gov/pubmed/24529765
2014
Dancík V, Carrel H, Bodycombe NE, Seiler KP, Fomina-Yadlin D, Kubicek ST, Hartwell K, Shamji AF, Wagner BK, Clemons PA. Connecting Small Molecules with Similar Assay Performance Profiles Leads to New Biological Hypotheses. J Biomol Screen. 2014 Jan 24;19(5):771-781. [Epub ahead of print]
Abstract: http://www.ncbi.nlm.nih.gov/pubmed/24464433
2013
Berger A, Hoelbl-Kovacic A, Bourgeais J, Hoefling L, Warsch W, Grundschober E, Uras IZ, Menzl I, Putz EM, Hoermann G, Schuster C, Fajmann S, Leitner E, Kubicek S, Moriggl R, Gouilleux F, Sexl V. PAK-dependent STAT5 serine phosphorylation is required for BCR-ABL-induced leukemogenesis. Leukemia. 2013 Nov 22. doi: 10.1038/leu.2013.351. [Epub ahead of print]
Abstract: http://www.ncbi.nlm.nih.gov/pubmed/24263804
2012
Yuan Y, Wang Q, Paulk J, Kubicek S, Kemp MM, Adams DJ, Shamji AF, Wagner BK, Schreiber SL. A small-molecule probe of the histone methyltransferase G9a induces cellular senescence in pancreatic adenocarcinoma. ACS Chem Biol. 2012 Jul 20;7(7):1152-7.
Abstract: http://www.ncbi.nlm.nih.gov/pubmed/22536950
2012
Kubicek S, Gilbert JC, Fomina-Yadlin D, Gitlin AD, Yuan Y, Wagner FF, Holson EB, Luo T, Lewis TA, Taylor B, Gupta S, Shamji A, Wagner BK, Clemons PA, Schreiber S.L. Chromatin-targeting small molecules cause class-specific transcriptional changes in pancreatic endocrine cells. PNAS 2012 Apr 3;109(14):5364-9.
Abstract: http://www.ncbi.nlm.nih.gov/pubmed/22434908
2012
Frogne T, Sylvestersen KB, Kubicek S, Nielsen ML, Hecksher-Sørensen J. Pdx1 is post-translationally modified in vivo and serine 61 is the principal site of phosphorylation. PLoS One. 2012;7(4):e35233.
Abstract: http://www.ncbi.nlm.nih.gov/pubmed/22509401
2012
Fomina-Yadlin D, Kubicek S, Vetere A, Hu He K, Schreiber SL, Wagner BK. GW8510 increases insulin expression in pancreatic alpha cells through activation of p53 transcriptional activity. PLOS one7(1): e28808.
Abstract: http://www.ncbi.nlm.nih.gov/pubmed/22242153
2011
Luo X, Liu Y, Kubicek S, Myllyharju J, Tumber A, Ng S, Che KH, Podoll J, Heightman TD, Oppermann U, Schreiber SL, Wang X. A selective inhibitor and probe of the cellular functions of Jumonji C domain-containing histone demethylases. J Am Chem Soc. 2011 Jun 22;133(24):9451-6.
Abstract: http://www.ncbi.nlm.nih.gov/pubmed/21585201
2010
O’Sullivan RJ, Kubicek S, Schreiber SL, Karlseder J. Reduced histone biosynthesis and chromatin changes arising from a damage signal at telomeres. Nat Struct Mol Biol. 2010 Oct;17(10):1218-25. Epub 2010 Oct 3.
Abstract: http://www.ncbi.nlm.nih.gov/pubmed/20890289