Research Publications


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
ACS Med Chem Lett
Journal Article
Because of the promise of BCL-2 antagonists in combating chronic lymphocytic leukemia (CLL) and non-Hodgkin's lymphoma (NHL), interest in additional selective antagonists of antiapoptotic proteins has grown. Beginning with a series of selective, potent BCL-XL antagonists containing an undesirable hydrazone functionality, in silico design and X-ray crystallography were utilized to develop alternative scaffolds that retained the selectivity and potency of the starting compounds.
Chemical Biology; Structural Biology
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Creation Date 2014-06-23 08:42:21 Last Modified 2015-03-26 02:49:24