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447 results

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Page 1
Discovery of GSK8612, a Highly Selective and Potent TBK1 Inhibitor.
Thomson DW, Poeckel D, Zinn N, Rau C, Strohmer K, Wagner AJ, Graves AP, Perrin J, Bantscheff M, Duempelfeld B, Kasparcova V, Ramanjulu JM, Pesiridis GS, Muelbaier M, Bergamini G. Thomson DW, et al. Among authors: rau c. ACS Med Chem Lett. 2019 Mar 11;10(5):780-785. doi: 10.1021/acsmedchemlett.9b00027. eCollection 2019 May 9. ACS Med Chem Lett. 2019. PMID: 31097999 Free PMC article.
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: rau c. 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
Identifying drug targets in tissues and whole blood with thermal-shift profiling.
Perrin J, Werner T, Kurzawa N, Rutkowska A, Childs DD, Kalxdorf M, Poeckel D, Stonehouse E, Strohmer K, Heller B, Thomson DW, Krause J, Becher I, Eberl HC, Vappiani J, Sevin DC, Rau CE, Franken H, Huber W, Faelth-Savitski M, Savitski MM, Bantscheff M, Bergamini G. Perrin J, et al. Among authors: rau ce. Nat Biotechnol. 2020 Mar;38(3):303-308. doi: 10.1038/s41587-019-0388-4. Epub 2020 Jan 20. Nat Biotechnol. 2020. PMID: 31959954
Optimization of Orally Bioavailable PI3Kδ Inhibitors and Identification of Vps34 as a Key Selectivity Target.
Henley ZA, Amour A, Barton N, Bantscheff M, Bergamini G, Bertrand SM, Convery M, Down K, Dümpelfeld B, Edwards CD, Grandi P, Gore PM, Keeling S, Livia S, Mallett D, Maxwell A, Price M, Rau C, Reinhard FBM, Rowedder J, Rowland P, Taylor JA, Thomas DA, Hessel EM, Hamblin JN. Henley ZA, et al. Among authors: rau c. J Med Chem. 2020 Jan 23;63(2):638-655. doi: 10.1021/acs.jmedchem.9b01585. Epub 2020 Jan 8. J Med Chem. 2020. PMID: 31855425
A selective inhibitor reveals PI3Kγ dependence of T(H)17 cell differentiation.
Bergamini G, Bell K, Shimamura S, Werner T, Cansfield A, Müller K, Perrin J, Rau C, Ellard K, Hopf C, Doce C, Leggate D, Mangano R, Mathieson T, O'Mahony A, Plavec I, Rharbaoui F, Reinhard F, Savitski MM, Ramsden N, Hirsch E, Drewes G, Rausch O, Bantscheff M, Neubauer G. Bergamini G, et al. Among authors: rau c. Nat Chem Biol. 2012 Apr 29;8(6):576-82. doi: 10.1038/nchembio.957. Nat Chem Biol. 2012. PMID: 22544264
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: rau c. Nat Biotechnol. 2007 Sep;25(9):1035-44. doi: 10.1038/nbt1328. Epub 2007 Aug 26. Nat Biotechnol. 2007. PMID: 17721511
Structure-Based Optimization of Naphthyridones into Potent ATAD2 Bromodomain Inhibitors.
Bamborough P, Chung CW, Furze RC, Grandi P, Michon AM, Sheppard RJ, Barnett H, Diallo H, Dixon DP, Douault C, Jones EJ, Karamshi B, Mitchell DJ, Prinjha RK, Rau C, Watson RJ, Werner T, Demont EH. Bamborough P, et al. Among authors: rau c. J Med Chem. 2015 Aug 13;58(15):6151-78. doi: 10.1021/acs.jmedchem.5b00773. Epub 2015 Jul 31. J Med Chem. 2015. PMID: 26230603
447 results