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The MCL1 inhibitor S63845 is tolerable and effective in diverse cancer models.
Kotschy A, Szlavik Z, Murray J, Davidson J, Maragno AL, Le Toumelin-Braizat G, Chanrion M, Kelly GL, Gong JN, Moujalled DM, Bruno A, Csekei M, Paczal A, Szabo ZB, Sipos S, Radics G, Proszenyak A, Balint B, Ondi L, Blasko G, Robertson A, Surgenor A, Dokurno P, Chen I, Matassova N, Smith J, Pedder C, Graham C, Studeny A, Lysiak-Auvity G, Girard AM, Gravé F, Segal D, Riffkin CD, Pomilio G, Galbraith LC, Aubrey BJ, Brennan MS, Herold MJ, Chang C, Guasconi G, Cauquil N, Melchiore F, Guigal-Stephan N, Lockhart B, Colland F, Hickman JA, Roberts AW, Huang DC, Wei AH, Strasser A, Lessene G, Geneste O. Kotschy A, et al. Among authors: lessene g. Nature. 2016 Oct 27;538(7626):477-482. doi: 10.1038/nature19830. Epub 2016 Oct 19. Nature. 2016. PMID: 27760111
BCL-2 family antagonists for cancer therapy.
Lessene G, Czabotar PE, Colman PM. Lessene G, et al. Nat Rev Drug Discov. 2008 Dec;7(12):989-1000. doi: 10.1038/nrd2658. Nat Rev Drug Discov. 2008. PMID: 19043450 Review.
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: lessene g. 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. 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: lessene g. J Med Chem. 2013 Jul 11;56(13):5514-40. doi: 10.1021/jm400556w. Epub 2013 Jun 26. J Med Chem. 2013. PMID: 23767404
Simplified silvestrol analogues with potent cytotoxic activity.
Hawkins BC, Lindqvist LM, Nhu D, Sharp PP, Segal D, Powell AK, Campbell M, Ryan E, Chambers JM, White JM, Rizzacasa MA, Lessene G, Huang DC, Burns CJ. Hawkins BC, et al. Among authors: lessene g. ChemMedChem. 2014 Jul;9(7):1556-66. doi: 10.1002/cmdc.201400024. Epub 2014 Mar 27. ChemMedChem. 2014. PMID: 24677741
Apoptotic caspases suppress mtDNA-induced STING-mediated type I IFN production.
White MJ, McArthur K, Metcalf D, Lane RM, Cambier JC, Herold MJ, van Delft MF, Bedoui S, Lessene G, Ritchie ME, Huang DC, Kile BT. White MJ, et al. Among authors: lessene g. Cell. 2014 Dec 18;159(7):1549-62. doi: 10.1016/j.cell.2014.11.036. Cell. 2014. PMID: 25525874 Free PMC article.
A RIPK2 inhibitor delays NOD signalling events yet prevents inflammatory cytokine production.
Nachbur U, Stafford CA, Bankovacki A, Zhan Y, Lindqvist LM, Fiil BK, Khakham Y, Ko HJ, Sandow JJ, Falk H, Holien JK, Chau D, Hildebrand J, Vince JE, Sharp PP, Webb AI, Jackman KA, Mühlen S, Kennedy CL, Lowes KN, Murphy JM, Gyrd-Hansen M, Parker MW, Hartland EL, Lew AM, Huang DC, Lessene G, Silke J. Nachbur U, et al. Among authors: lessene g. Nat Commun. 2015 Mar 17;6:6442. doi: 10.1038/ncomms7442. Nat Commun. 2015. PMID: 25778803 Free article.
86 results