Structure-guided design of a selective BCL-X(L) inhibitor.

  title={Structure-guided design of a selective BCL-X(L) inhibitor.},
  author={Guillaume Lessene and Peter E. Czabotar and Brad E Sleebs and Kerry Zobel and Kym N. Lowes and Jerry M. Adams and Jonathan B. Baell and Peter M. Colman and Kurt D Deshayes and Wayne J. Fairbrother and John A. Flygare and Paul A Gibbons and Wilhelmus J A Kersten and Sanji Kulasegaram and Rebecca M. Moss and John P. Parisot and Brian J Smith and Ian P. Street and Hong Yang and David C S Huang and Keith G Watson},
  journal={Nature chemical biology},
  volume={9 6},
The prosurvival BCL-2 family protein BCL-X(L) is often overexpressed in solid tumors and renders malignant tumor cells resistant to anticancer therapeutics. Enhancing apoptotic responses by inhibiting BCL-X(L) will most likely have widespread utility in cancer treatment and, instead of inhibiting multiple prosurvival BCL-2 family members, a BCL-X(L)-selective inhibitor would be expected to minimize the toxicity to normal tissues. We describe the use of a high-throughput screen to discover a new… CONTINUE READING
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