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Page 1
The VEGFR/PDGFR tyrosine kinase inhibitor, ABT-869, blocks necroptosis by targeting RIPK1 kinase.
Pierotti CL, Jacobsen AV, Grohmann C, Dempsey RK, Etemadi N, Hildebrand JM, Fitzgibbon C, Young SN, Davies KA, Kersten WJA, Silke J, Lowes KN, Jousset Sabroux H, Huang DCS, van Delft MF, Murphy JM, Lessene G. Pierotti CL, et al. Among authors: kersten wja. Biochem J. 2023 May 15;480(9):665-684. doi: 10.1042/BCJ20230035. Biochem J. 2023. PMID: 37115711 Free PMC article.
Potent Inhibition of Necroptosis by Simultaneously Targeting Multiple Effectors of the Pathway.
Pierotti CL, Tanzer MC, Jacobsen AV, Hildebrand JM, Garnier JM, Sharma P, Lucet IS, Cowan AD, Kersten WJA, Luo MX, Liang LY, Fitzgibbon C, Garnish SE, Hempel A, Nachbur U, Huang DCS, Czabotar PE, Silke J, van Delft MF, Murphy JM, Lessene G. Pierotti CL, et al. Among authors: kersten wja. ACS Chem Biol. 2020 Oct 16;15(10):2702-2713. doi: 10.1021/acschembio.0c00482. Epub 2020 Sep 22. ACS Chem Biol. 2020. PMID: 32902249
Viral MLKL Homologs Subvert Necroptotic Cell Death by Sequestering Cellular RIPK3.
Petrie EJ, Sandow JJ, Lehmann WIL, Liang LY, Coursier D, Young SN, Kersten WJA, Fitzgibbon C, Samson AL, Jacobsen AV, Lowes KN, Au AE, Jousset Sabroux H, Lalaoui N, Webb AI, Lessene G, Manning G, Lucet IS, Murphy JM. Petrie EJ, et al. Among authors: kersten wja. Cell Rep. 2019 Sep 24;28(13):3309-3319.e5. doi: 10.1016/j.celrep.2019.08.055. Cell Rep. 2019. PMID: 31553902 Free article.
Conformational switching of the pseudokinase domain promotes human MLKL tetramerization and cell death by necroptosis.
Petrie EJ, Sandow JJ, Jacobsen AV, Smith BJ, Griffin MDW, Lucet IS, Dai W, Young SN, Tanzer MC, Wardak A, Liang LY, Cowan AD, Hildebrand JM, Kersten WJA, Lessene G, Silke J, Czabotar PE, Webb AI, Murphy JM. Petrie EJ, et al. Among authors: kersten wja. Nat Commun. 2018 Jun 21;9(1):2422. doi: 10.1038/s41467-018-04714-7. Nat Commun. 2018. PMID: 29930286 Free PMC article.
Structure-Guided Rescaffolding of Selective Antagonists of BCL-XL.
Koehler MF, Bergeron P, Choo EF, Lau K, Ndubaku C, Dudley D, Gibbons P, Sleebs BE, Rye CS, Nikolakopoulos G, Bui C, Kulasegaram S, Kersten WJ, Smith BJ, Czabotar PE, Colman PM, Huang DC, Baell JB, Watson KG, Hasvold L, Tao ZF, Wang L, Souers AJ, Elmore SW, Flygare JA, Fairbrother WJ, Lessene G. Koehler MF, et al. Among authors: kersten wj. ACS Med Chem Lett. 2014 Mar 21;5(6):662-7. doi: 10.1021/ml500030p. eCollection 2014 Jun 12. ACS Med Chem Lett. 2014. PMID: 24944740 Free PMC article.
Discovery of potent and selective benzothiazole hydrazone inhibitors of Bcl-XL.
Sleebs BE, Kersten WJ, Kulasegaram S, Nikolakopoulos G, Hatzis E, Moss RM, Parisot JP, Yang H, Czabotar PE, Fairlie WD, Lee EF, Adams JM, Chen L, van Delft MF, Lowes KN, Wei A, Huang DC, Colman PM, Street IP, Baell JB, Watson K, Lessene G. Sleebs BE, et al. Among authors: kersten wj. J Med Chem. 2013 Jul 11;56(13):5514-40. doi: 10.1021/jm400556w. Epub 2013 Jun 26. J Med Chem. 2013. PMID: 23767404
Characterization of the novel broad-spectrum kinase inhibitor CTx-0294885 as an affinity reagent for mass spectrometry-based kinome profiling.
Zhang L, Holmes IP, Hochgräfe F, Walker SR, Ali NA, Humphrey ES, Wu J, de Silva M, Kersten WJ, Connor T, Falk H, Allan L, Street IP, Bentley JD, Pilling PA, Monahan BJ, Peat TS, Daly RJ. Zhang L, et al. Among authors: kersten wj. J Proteome Res. 2013 Jul 5;12(7):3104-16. doi: 10.1021/pr3008495. Epub 2013 Jun 25. J Proteome Res. 2013. PMID: 23692254
Structure-guided design of a selective BCL-X(L) inhibitor.
Lessene G, Czabotar PE, Sleebs BE, Zobel K, Lowes KN, Adams JM, Baell JB, Colman PM, Deshayes K, Fairbrother WJ, Flygare JA, Gibbons P, Kersten WJ, Kulasegaram S, Moss RM, Parisot JP, Smith BJ, Street IP, Yang H, Huang DC, Watson KG. Lessene G, et al. Among authors: kersten wj. Nat Chem Biol. 2013 Jun;9(6):390-7. doi: 10.1038/nchembio.1246. Epub 2013 Apr 21. Nat Chem Biol. 2013. PMID: 23603658
Quinazoline sulfonamides as dual binders of the proteins B-cell lymphoma 2 and B-cell lymphoma extra long with potent proapoptotic cell-based activity.
Sleebs BE, Czabotar PE, Fairbrother WJ, Fairlie WD, Flygare JA, Huang DC, Kersten WJ, Koehler MF, Lessene G, Lowes K, Parisot JP, Smith BJ, Smith ML, Souers AJ, Street IP, Yang H, Baell JB. Sleebs BE, et al. Among authors: kersten wj. J Med Chem. 2011 Mar 24;54(6):1914-26. doi: 10.1021/jm101596e. Epub 2011 Mar 2. J Med Chem. 2011. PMID: 21366295