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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: stauffer f. 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.
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: stauffer f. 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. 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.
Identification of NVP-CLR457 as an Orally Bioavailable Non-CNS-Penetrant pan-Class IA Phosphoinositol-3-Kinase Inhibitor.
Fairhurst RA, Furet P, Imbach-Weese P, Stauffer F, Rueeger H, McCarthy C, Ripoche S, Oswald S, Arnaud B, Jary A, Maira M, Schnell C, Guthy DA, Wartmann M, Kiffe M, Desrayaud S, Blasco F, Widmer T, Seiler F, Gutmann S, Knapp M, Caravatti G. Fairhurst RA, et al. Among authors: stauffer f. J Med Chem. 2022 Jun 23;65(12):8345-8379. doi: 10.1021/acs.jmedchem.2c00267. Epub 2022 May 2. J Med Chem. 2022. PMID: 35500094
Blocking the PI3K/PKB pathway in tumor cells.
Stauffer F, Holzer P, García-Echeverría C. Stauffer F, et al. Curr Med Chem Anticancer Agents. 2005 Sep;5(5):449-62. doi: 10.2174/1568011054866937. Curr Med Chem Anticancer Agents. 2005. PMID: 16178772 Review.
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: stauffer f. Oncotarget. 2020 Mar 17;11(11):956-968. doi: 10.18632/oncotarget.27493. eCollection 2020 Mar 17. Oncotarget. 2020. PMID: 32215184 Free PMC article.
Discovery and Pharmacological Characterization of Novel Quinazoline-Based PI3K Delta-Selective Inhibitors.
Hoegenauer K, Soldermann N, Stauffer F, Furet P, Graveleau N, Smith AB, Hebach C, Hollingworth GJ, Lewis I, Gutmann S, Rummel G, Knapp M, Wolf RM, Blanz J, Feifel R, Burkhart C, Zécri F. Hoegenauer K, et al. Among authors: stauffer f. ACS Med Chem Lett. 2016 Jun 2;7(8):762-7. doi: 10.1021/acsmedchemlett.6b00119. eCollection 2016 Aug 11. ACS Med Chem Lett. 2016. PMID: 27563400 Free PMC article.
123 results