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Mechanism and inhibition of the papain-like protease, PLpro, of SARS-CoV-2.
Klemm T, Ebert G, Calleja DJ, Allison CC, Richardson LW, Bernardini JP, Lu BG, Kuchel NW, Grohmann C, Shibata Y, Gan ZY, Cooney JP, Doerflinger M, Au AE, Blackmore TR, van der Heden van Noort GJ, Geurink PP, Ovaa H, Newman J, Riboldi-Tunnicliffe A, Czabotar PE, Mitchell JP, Feltham R, Lechtenberg BC, Lowes KN, Dewson G, Pellegrini M, Lessene G, Komander D. Klemm T, et al. Among authors: lowes kn. EMBO J. 2020 Sep 15;39(18):e106275. doi: 10.15252/embj.2020106275. Epub 2020 Aug 26. EMBO J. 2020. PMID: 32845033 Free PMC article.
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. J Med Chem. 2011 Mar 24;54(6):1914-26. doi: 10.1021/jm101596e. Epub 2011 Mar 2. J Med Chem. 2011. PMID: 21366295
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: lowes kn. Nat Chem Biol. 2013 Jun;9(6):390-7. doi: 10.1038/nchembio.1246. Epub 2013 Apr 21. Nat Chem Biol. 2013. PMID: 23603658
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: lowes kn. J Med Chem. 2013 Jul 11;56(13):5514-40. doi: 10.1021/jm400556w. Epub 2013 Jun 26. J Med Chem. 2013. PMID: 23767404
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: lowes kn. 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.
A small molecule interacts with VDAC2 to block mouse BAK-driven apoptosis.
van Delft MF, Chappaz S, Khakham Y, Bui CT, Debrincat MA, Lowes KN, Brouwer JM, Grohmann C, Sharp PP, Dagley LF, Li L, McArthur K, Luo MX, Chin HS, Fairlie WD, Lee EF, Segal D, Duflocq S, Lessene R, Bernard S, Peilleron L, Nguyen T, Miles C, Wan SS, Lane RM, Wardak A, Lackovic K, Colman PM, Sandow JJ, Webb AI, Czabotar PE, Dewson G, Watson KG, Huang DCS, Lessene G, Kile BT. van Delft MF, et al. Among authors: lowes kn. Nat Chem Biol. 2019 Nov;15(11):1057-1066. doi: 10.1038/s41589-019-0365-8. Epub 2019 Oct 7. Nat Chem Biol. 2019. PMID: 31591564
Basis for drug selectivity of plasmepsin IX and X inhibition in Plasmodium falciparum and vivax.
Hodder AN, Christensen J, Scally S, Triglia T, Ngo A, Birkinshaw RW, Bailey B, Favuzza P, Dietrich MH, Tham WH, Czabotar PE, Lowes K, Guo Z, Murgolo N, Lera Ruiz M, McCauley JA, Sleebs BE, Olsen D, Cowman AF. Hodder AN, et al. Structure. 2022 Jul 7;30(7):947-961.e6. doi: 10.1016/j.str.2022.03.018. Epub 2022 Apr 22. Structure. 2022. PMID: 35460613 Free article.
Insights Into Drug Repurposing, as Well as Specificity and Compound Properties of Piperidine-Based SARS-CoV-2 PLpro Inhibitors.
Calleja DJ, Kuchel N, Lu BGC, Birkinshaw RW, Klemm T, Doerflinger M, Cooney JP, Mackiewicz L, Au AE, Yap YQ, Blackmore TR, Katneni K, Crighton E, Newman J, Jarman KE, Call MJ, Lechtenberg BC, Czabotar PE, Pellegrini M, Charman SA, Lowes KN, Mitchell JP, Nachbur U, Lessene G, Komander D. Calleja DJ, et al. Among authors: lowes kn. Front Chem. 2022 Apr 12;10:861209. doi: 10.3389/fchem.2022.861209. eCollection 2022. Front Chem. 2022. PMID: 35494659 Free PMC article.
36 results