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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: watson k. J Med Chem. 2013 Jul 11;56(13):5514-40. doi: 10.1021/jm400556w. Epub 2013 Jun 26. J Med Chem. 2013. PMID: 23767404
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: watson kg. Nat Chem Biol. 2013 Jun;9(6):390-7. doi: 10.1038/nchembio.1246. Epub 2013 Apr 21. Nat Chem Biol. 2013. PMID: 23603658
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: watson kg. 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 a Potent and Selective BCL-XL Inhibitor with in Vivo Activity.
Tao ZF, Hasvold L, Wang L, Wang X, Petros AM, Park CH, Boghaert ER, Catron ND, Chen J, Colman PM, Czabotar PE, Deshayes K, Fairbrother WJ, Flygare JA, Hymowitz SG, Jin S, Judge RA, Koehler MF, Kovar PJ, Lessene G, Mitten MJ, Ndubaku CO, Nimmer P, Purkey HE, Oleksijew A, Phillips DC, Sleebs BE, Smith BJ, Smith ML, Tahir SK, Watson KG, Xiao Y, Xue J, Zhang H, Zobel K, Rosenberg SH, Tse C, Leverson JD, Elmore SW, Souers AJ. Tao ZF, et al. Among authors: watson kg. ACS Med Chem Lett. 2014 Aug 26;5(10):1088-93. doi: 10.1021/ml5001867. eCollection 2014 Oct 9. ACS Med Chem Lett. 2014. PMID: 25313317 Free PMC 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: watson kg. 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
1,973 results