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Page 1
Polo-like Kinase 1 Inhibition as a Therapeutic Approach to Selectively Target BRCA1-Deficient Cancer Cells by Synthetic Lethality Induction.
Carbajosa S, Pansa MF, Paviolo NS, Castellaro AM, Andino DL, Nigra AD, García IA, Racca AC, Rodriguez-Berdini L, Angiolini V, Guantay L, Villafañez F, Federico MB, Rodríguez-Baili MC, Caputto BL, Drewes G, Madauss KP, Gloger I, Fernandez E, Gil GA, Bocco JL, Gottifredi V, Soria G. Carbajosa S, et al. Among authors: drewes g. Clin Cancer Res. 2019 Jul 1;25(13):4049-4062. doi: 10.1158/1078-0432.CCR-18-3516. Epub 2019 Mar 19. Clin Cancer Res. 2019. PMID: 30890549
Hsp90 inhibition differentially destabilises MAP kinase and TGF-beta signalling components in cancer cells revealed by kinase-targeted chemoproteomics.
Haupt A, Joberty G, Bantscheff M, Fröhlich H, Stehr H, Schweiger MR, Fischer A, Kerick M, Boerno ST, Dahl A, Lappe M, Lehrach H, Gonzalez C, Drewes G, Lange BM. Haupt A, et al. Among authors: drewes g. BMC Cancer. 2012 Jan 25;12:38. doi: 10.1186/1471-2407-12-38. BMC Cancer. 2012. PMID: 22277058 Free PMC article.
The commonly used PI3-kinase probe LY294002 is an inhibitor of BET bromodomains.
Dittmann A, Werner T, Chung CW, Savitski MM, Fälth Savitski M, Grandi P, Hopf C, Lindon M, Neubauer G, Prinjha RK, Bantscheff M, Drewes G. Dittmann A, et al. Among authors: drewes g. ACS Chem Biol. 2014 Feb 21;9(2):495-502. doi: 10.1021/cb400789e. Epub 2013 Dec 10. ACS Chem Biol. 2014. PMID: 24533473
Discovery of a Highly Selective Tankyrase Inhibitor Displaying Growth Inhibition Effects against a Diverse Range of Tumor Derived Cell Lines.
Thomson DW, Wagner AJ, Bantscheff M, Benson RE, Dittus L, Duempelfeld B, Drewes G, Krause J, Moore JT, Mueller K, Poeckel D, Rau C, Salzer E, Shewchuk L, Hopf C, Emery JG, Muelbaier M. Thomson DW, et al. Among authors: drewes g. J Med Chem. 2017 Jul 13;60(13):5455-5471. doi: 10.1021/acs.jmedchem.7b00137. Epub 2017 Jun 27. J Med Chem. 2017. PMID: 28591512
Quantitative chemical proteomics reveals mechanisms of action of clinical ABL kinase inhibitors.
Bantscheff M, Eberhard D, Abraham Y, Bastuck S, Boesche M, Hobson S, Mathieson T, Perrin J, Raida M, Rau C, Reader V, Sweetman G, Bauer A, Bouwmeester T, Hopf C, Kruse U, Neubauer G, Ramsden N, Rick J, Kuster B, Drewes G. Bantscheff M, et al. Among authors: drewes g. Nat Biotechnol. 2007 Sep;25(9):1035-44. doi: 10.1038/nbt1328. Epub 2007 Aug 26. Nat Biotechnol. 2007. PMID: 17721511
Recurrent mutations, including NPM1c, activate a BRD4-dependent core transcriptional program in acute myeloid leukemia.
Dawson MA, Gudgin EJ, Horton SJ, Giotopoulos G, Meduri E, Robson S, Cannizzaro E, Osaki H, Wiese M, Putwain S, Fong CY, Grove C, Craig J, Dittmann A, Lugo D, Jeffrey P, Drewes G, Lee K, Bullinger L, Prinjha RK, Kouzarides T, Vassiliou GS, Huntly BJ. Dawson MA, et al. Among authors: drewes g. Leukemia. 2014 Feb;28(2):311-20. doi: 10.1038/leu.2013.338. Epub 2013 Nov 13. Leukemia. 2014. PMID: 24220271 Free PMC article.
High-throughput screening of the Plasmodium falciparum cGMP-dependent protein kinase identified a thiazole scaffold which kills erythrocytic and sexual stage parasites.
Penzo M, de Las Heras-Dueña L, Mata-Cantero L, Diaz-Hernandez B, Vazquez-Muñiz MJ, Ghidelli-Disse S, Drewes G, Fernandez-Alvaro E, Baker DA. Penzo M, et al. Among authors: drewes g. Sci Rep. 2019 May 7;9(1):7005. doi: 10.1038/s41598-019-42801-x. Sci Rep. 2019. PMID: 31065005 Free PMC article.
New IDH1 mutant inhibitors for treatment of acute myeloid leukemia.
Okoye-Okafor UC, Bartholdy B, Cartier J, Gao EN, Pietrak B, Rendina AR, Rominger C, Quinn C, Smallwood A, Wiggall KJ, Reif AJ, Schmidt SJ, Qi H, Zhao H, Joberty G, Faelth-Savitski M, Bantscheff M, Drewes G, Duraiswami C, Brady P, Groy A, Narayanagari SR, Antony-Debre I, Mitchell K, Wang HR, Kao YR, Christopeit M, Carvajal L, Barreyro L, Paietta E, Makishima H, Will B, Concha N, Adams ND, Schwartz B, McCabe MT, Maciejewski J, Verma A, Steidl U. Okoye-Okafor UC, et al. Among authors: drewes g. Nat Chem Biol. 2015 Nov;11(11):878-86. doi: 10.1038/nchembio.1930. Epub 2015 Oct 5. Nat Chem Biol. 2015. PMID: 26436839 Free PMC article.
115 results