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Page 1
Discovery of Novel Allosteric EGFR L858R Inhibitors for the Treatment of Non-Small-Cell Lung Cancer as a Single Agent or in Combination with Osimertinib.
Obst-Sander U, Ricci A, Kuhn B, Friess T, Koldewey P, Kuglstatter A, Hewings D, Goergler A, Steiner S, Rueher D, Imhoff MP, Raschetti N, Marty HP, Dietzig A, Rynn C, Ehler A, Burger D, Kornacker M, Schaffland JP, Herting F, Pao W, Bischoff JR, Martoglio B, Alice Nagel Y, Jaeschke G. Obst-Sander U, et al. Among authors: hewings d. J Med Chem. 2022 Oct 13;65(19):13052-13073. doi: 10.1021/acs.jmedchem.2c00893. Epub 2022 Sep 30. J Med Chem. 2022. PMID: 36178776
Preclinical Characterization of a Next-Generation Brain Permeable, Paradox Breaker BRAF Inhibitor.
Wichmann J, Rynn C, Friess T, Petrig-Schaffland J, Kornacker M, Handl C, Emmenegger J, Eckmann J, Herting F, Frances N, Hunziker D, Krummenacher D, Rüttinger D, Ribeiro A, Bacac M, Brigo A, Hewings DS, Dummer R, Levesque MP, Schnetzler G, Martoglio B, Bischoff JR, Pettazzoni P. Wichmann J, et al. Among authors: hewings ds. Clin Cancer Res. 2022 Feb 15;28(4):770-780. doi: 10.1158/1078-0432.CCR-21-2761. Clin Cancer Res. 2022. PMID: 34782366
BET bromodomain ligands: Probing the WPF shelf to improve BRD4 bromodomain affinity and metabolic stability.
Jennings LE, Schiedel M, Hewings DS, Picaud S, Laurin CMC, Bruno PA, Bluck JP, Scorah AR, See L, Reynolds JK, Moroglu M, Mistry IN, Hicks A, Guzanov P, Clayton J, Evans CNG, Stazi G, Biggin PC, Mapp AK, Hammond EM, Humphreys PG, Filippakopoulos P, Conway SJ. Jennings LE, et al. Among authors: hewings ds. Bioorg Med Chem. 2018 Jul 15;26(11):2937-2957. doi: 10.1016/j.bmc.2018.05.003. Epub 2018 May 15. Bioorg Med Chem. 2018. PMID: 29776834 Free article.
3,5-dimethylisoxazoles act as acetyl-lysine-mimetic bromodomain ligands.
Hewings DS, Wang M, Philpott M, Fedorov O, Uttarkar S, Filippakopoulos P, Picaud S, Vuppusetty C, Marsden B, Knapp S, Conway SJ, Heightman TD. Hewings DS, et al. J Med Chem. 2011 Oct 13;54(19):6761-70. doi: 10.1021/jm200640v. Epub 2011 Sep 6. J Med Chem. 2011. PMID: 21851057 Free PMC article.
Optimization of 3,5-dimethylisoxazole derivatives as potent bromodomain ligands.
Hewings DS, Fedorov O, Filippakopoulos P, Martin S, Picaud S, Tumber A, Wells C, Olcina MM, Freeman K, Gill A, Ritchie AJ, Sheppard DW, Russell AJ, Hammond EM, Knapp S, Brennan PE, Conway SJ. Hewings DS, et al. J Med Chem. 2013 Apr 25;56(8):3217-27. doi: 10.1021/jm301588r. Epub 2013 Apr 5. J Med Chem. 2013. PMID: 23517011 Free PMC article.
Small molecule inhibitors of bromodomain-acetyl-lysine interactions.
Brand M, Measures AR, Wilson BG, Cortopassi WA, Alexander R, Höss M, Hewings DS, Rooney TP, Paton RS, Conway SJ. Brand M, et al. ACS Chem Biol. 2015 Jan 16;10(1):22-39. doi: 10.1021/cb500996u. ACS Chem Biol. 2015. PMID: 25549280 Review.
Isoxazole-Derived Amino Acids are Bromodomain-Binding Acetyl-Lysine Mimics: Incorporation into Histone H4 Peptides and Histone H3.
Sekirnik Née Measures AR, Hewings DS, Theodoulou NH, Jursins L, Lewendon KR, Jennings LE, Rooney TP, Heightman TD, Conway SJ. Sekirnik Née Measures AR, et al. Among authors: hewings ds. Angew Chem Int Ed Engl. 2016 Jul 11;55(29):8353-7. doi: 10.1002/anie.201602908. Epub 2016 Jun 6. Angew Chem Int Ed Engl. 2016. PMID: 27264992 Free PMC article.
18 results