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Discovery of Novel Dot1L Inhibitors through a Structure-Based Fragmentation Approach.
Chen C, Zhu H, Stauffer F, Caravatti G, Vollmer S, Machauer R, Holzer P, Möbitz H, Scheufler C, Klumpp M, Tiedt R, Beyer KS, Calkins K, Guthy D, Kiffe M, Zhang J, Gaul C. Chen C, et al. Among authors: tiedt r. ACS Med Chem Lett. 2016 Jun 1;7(8):735-40. doi: 10.1021/acsmedchemlett.6b00167. eCollection 2016 Aug 11. ACS Med Chem Lett. 2016. PMID: 27563395 Free PMC article.
Complementary activities of DOT1L and Menin inhibitors in MLL-rearranged leukemia.
Dafflon C, Craig VJ, Méreau H, Gräsel J, Schacher Engstler B, Hoffman G, Nigsch F, Gaulis S, Barys L, Ito M, Aguadé-Gorgorió J, Bornhauser B, Bourquin JP, Proske A, Stork-Fux C, Murakami M, Sellers WR, Hofmann F, Schwaller J, Tiedt R. Dafflon C, et al. Among authors: tiedt r. Leukemia. 2017 Jun;31(6):1269-1277. doi: 10.1038/leu.2016.327. Epub 2016 Nov 14. Leukemia. 2017. PMID: 27840424
Discovery of Potent, Selective, and Structurally Novel Dot1L Inhibitors by a Fragment Linking Approach.
Möbitz H, Machauer R, Holzer P, Vaupel A, Stauffer F, Ragot C, Caravatti G, Scheufler C, Fernandez C, Hommel U, Tiedt R, Beyer KS, Chen C, Zhu H, Gaul C. Möbitz H, et al. Among authors: tiedt r. ACS Med Chem Lett. 2017 Feb 14;8(3):338-343. doi: 10.1021/acsmedchemlett.6b00519. eCollection 2017 Mar 9. ACS Med Chem Lett. 2017. PMID: 28337327 Free PMC article.
New Potent DOT1L Inhibitors for in Vivo Evaluation in Mouse.
Stauffer F, Weiss A, Scheufler C, Möbitz H, Ragot C, Beyer KS, Calkins K, Guthy D, Kiffe M, Van Eerdenbrugh B, Tiedt R, Gaul C. Stauffer F, et al. Among authors: tiedt r. ACS Med Chem Lett. 2019 Dec 4;10(12):1655-1660. doi: 10.1021/acsmedchemlett.9b00452. eCollection 2019 Dec 12. ACS Med Chem Lett. 2019. PMID: 31857842 Free PMC article.
DOT1L inhibition is lethal for multiple myeloma due to perturbation of the endoplasmic reticulum stress pathway.
Dafflon C, Gaulis S, Barys L, Kapur K, Cornacchione V, Schukur L, Bergling S, Traggiai E, Jansky S, Hellmann L, Engstler BS, Kerr G, de Weck A, Ruddy DA, Naumann U, Stauffer F, Gaul C, Lin Y, Billy E, Weiss A, Hofmann F, Ito M, Tiedt R. Dafflon C, et al. Among authors: tiedt r. Oncotarget. 2020 Mar 17;11(11):956-968. doi: 10.18632/oncotarget.27493. eCollection 2020 Mar 17. Oncotarget. 2020. PMID: 32215184 Free PMC article.
BET bromodomain inhibitors regulate keratinocyte plasticity.
Schutzius G, Kolter C, Bergling S, Tortelli F, Fuchs F, Renner S, Guagnano V, Cotesta S, Rueeger H, Faller M, Bouchez L, Salathe A, Nigsch F, Richards SM, Louis M, Gruber V, Aebi A, Turner J, Grandjean F, Li J, Dimitri C, Thomas JR, Schirle M, Blank J, Drueckes P, Vaupel A, Tiedt R, Manley PW, Klopp J, Hemmig R, Zink F, Leroy N, Carbone W, Roma G, Keller CG, Dales N, Beyerbach A, Zimmerlin A, Bonenfant D, Terranova R, Berwick A, Sahambi S, Reynolds A, Jennings LL, Ruffner H, Tarsa P, Bouwmeester T, Driver V, Frederiksen M, Lohmann F, Kirkland S. Schutzius G, et al. Among authors: tiedt r. Nat Chem Biol. 2021 Mar;17(3):280-290. doi: 10.1038/s41589-020-00716-z. Epub 2021 Jan 18. Nat Chem Biol. 2021. PMID: 33462494
A drug resistance screen using a selective MET inhibitor reveals a spectrum of mutations that partially overlap with activating mutations found in cancer patients.
Tiedt R, Degenkolbe E, Furet P, Appleton BA, Wagner S, Schoepfer J, Buck E, Ruddy DA, Monahan JE, Jones MD, Blank J, Haasen D, Drueckes P, Wartmann M, McCarthy C, Sellers WR, Hofmann F. Tiedt R, et al. Cancer Res. 2011 Aug 1;71(15):5255-64. doi: 10.1158/0008-5472.CAN-10-4433. Epub 2011 Jun 22. Cancer Res. 2011. PMID: 21697284
Rescue screens with secreted proteins reveal compensatory potential of receptor tyrosine kinases in driving cancer growth.
Harbinski F, Craig VJ, Sanghavi S, Jeffery D, Liu L, Sheppard KA, Wagner S, Stamm C, Buness A, Chatenay-Rivauday C, Yao Y, He F, Lu CX, Guagnano V, Metz T, Finan PM, Hofmann F, Sellers WR, Porter JA, Myer VE, Graus-Porta D, Wilson CJ, Buckler A, Tiedt R. Harbinski F, et al. Among authors: tiedt r. Cancer Discov. 2012 Oct;2(10):948-59. doi: 10.1158/2159-8290.CD-12-0237. Epub 2012 Aug 8. Cancer Discov. 2012. PMID: 22874768
37 results